Search Result
Results for "
benzodiazepine receptors
" in MedChemExpress (MCE) Product Catalog:
8
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-100369A
-
|
GABA Receptor
|
Neurological Disease
|
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively .
|
-
-
- HY-105791
-
|
GABA Receptor
|
Inflammation/Immunology
|
Sulazepam, a benzodiazepine, is a selective ovarian cancer G protein-coupled receptor (OGR1) agonist. Sulazepam has anticonvulsive action and has the potential for airway hyperresponsiveness (AHR) research .
|
-
-
- HY-101059
-
|
GABA Receptor
|
Neurological Disease
|
FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .
|
-
-
- HY-19945
-
|
GABA Receptor
|
Neurological Disease
|
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
|
-
-
- HY-111194
-
-
-
- HY-118259
-
-
-
- HY-168363
-
WE-973
|
GABA Receptor
|
Neurological Disease
|
Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats .
|
-
-
- HY-119605
-
|
GABA Receptor
|
Neurological Disease
|
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects .
|
-
-
- HY-100369AR
-
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
DMCM (hydrochloride) (Standard) is the analytical standard of DMCM (hydrochloride). This product is intended for research and analytical applications. DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively .
|
-
-
- HY-101059R
-
|
GABA Receptor
Reference Standards
|
Neurological Disease
|
FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27. This product is intended for research and analytical applications. FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .
|
-
-
- HY-103476
-
|
GABA Receptor
|
Neurological Disease
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
-
- HY-100248
-
-
-
- HY-103476R
-
|
GABA Receptor
|
Neurological Disease
|
Ro15-4513 (Standard) is the analytical standard of Ro15-4513. This product is intended for research and analytical applications. Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
-
- HY-19065
-
-
-
- HY-19250
-
-
-
- HY-W749797
-
|
GABA Receptor
|
Neurological Disease
|
Nitrazolam is a benzodiazepine compound, that may exhibit CNS depressant properties as traditional benzodiazepines, including sedation, hypnosis, anxiolysis, and anticonvulsant effects, by acting on GABA receptors .
|
-
-
- HY-B0009
-
-
-
- HY-U00033
-
|
Endogenous Metabolite
|
Neurological Disease
|
Iomazenil is a benzodiazepine receptor antagonist with partial inverse agonist activity. Iomazenil can assess the binding potential of central benzodiazepine receptors in the cerebral cortex and may reflect neuronal function in viable tissue. Iomazenil use is associated with improved cognitive function in adult patients with ischemic cerebral pathology after indirect revascularization surgery. Iomazenil demonstrated restoration of benzodiazepine receptor binding potential in the affected hemisphere after surgery on brain SPECT imaging .
|
-
-
- HY-19308
-
-
-
- HY-106316
-
|
GABA Receptor
|
Neurological Disease
|
CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures .
|
-
-
- HY-100924
-
|
GABA Receptor
|
Neurological Disease
|
β-CCB is a ligand for benzodiazepine receptor, which inhibits the binding of [ 3H]flunitrazepam and ethyl (3-[ 3H]carboline-3-carboxylate to benzodiazepine receptors, with Ki of 3-4 nM. β-CCB exhibits proconvulsant and anxiogenic effects .
|
-
-
- HY-124225
-
-
-
- HY-118308
-
-
-
- HY-100140
-
-
-
- HY-N6648
-
|
GABA Receptor
|
Neurological Disease
|
Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
|
-
-
- HY-100140A
-
PK-8165 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity .
|
-
-
- HY-116813
-
-
-
- HY-100291
-
-
-
- HY-169651
-
|
GABA Receptor
|
Neurological Disease
|
GABA-IN-4 (Compound 17) is a N-(indol-3-ylglyoxylyl)benzylamine derivative. GABA-IN-4 exhibits high affinity for the benzodiazepine receptor (BzR) (binding site in GABAA receptor complex) with Ki value of 67 nM. Benzodiazepines are widely used as antianxiety, sedative-hypnotic and anticonvulsant agents .
|
-
-
- HY-106635
-
RP31264
|
GABA Receptor
|
Neurological Disease
|
Suriclone (RP31264) is a GABA receptor agonist. Suriclone is an anxiolytic agent with a high affinity for the benzodiazepine receptors. Suriclone has oral activity .
|
-
-
- HY-110399
-
-
-
- HY-106851
-
FG 10571; PNU 78875
|
GABA Receptor
|
Neurological Disease
|
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .
|
-
-
- HY-111481
-
MS 4101; Ro 7-6102
|
GABA Receptor
|
Neurological Disease
|
Flutazolam (MS 4101; Ro 7-6102) is a medicine acts on benzodiazepine receptors of the brain and relieves anxiety or tension.
|
-
-
- HY-124467
-
-
-
- HY-U00215
-
|
GABA Receptor
|
Neurological Disease
|
Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the benzodiazepine receptor.
|
-
-
- HY-139145
-
Trimethylopropane phosphate
|
GABA Receptor
|
Neurological Disease
|
Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
|
-
-
- HY-129090
-
-
-
- HY-167658
-
-
-
- HY-103225
-
SB-737552 phosphate
|
GABA Receptor
|
Neurological Disease
|
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.
|
-
-
- HY-121877
-
Valmethamide
|
GABA Receptor
|
Neurological Disease
|
Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors .
|
-
-
- HY-106917
-
Ro 41-3696
|
GABA Receptor
|
Neurological Disease
|
Lirequinil (Ro 41-3696) is an orally active partial agonist of the benzodiazepine (BDZ) receptor. Lirequinil has the effect of promoting sleep .
|
-
-
- HY-14953
-
AWD 131-138
|
GABA Receptor
|
Neurological Disease
|
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
|
-
-
- HY-A0198
-
U 41123
|
GABA Receptor
|
Neurological Disease
|
Adinazolam (U 41123) is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities .
|
-
-
- HY-W705371
-
|
Drug Metabolite
GABA Receptor
|
Others
|
α-Hydroxy etizolam is the primary metabolite of Etizolam, possessing nearly identical pharmacological potency and high affinity for benzodiazepine receptors as Etizolam .
|
-
-
- HY-138014
-
|
GABA Receptor
|
Neurological Disease
|
Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders .
|
-
-
- HY-114685
-
SB-737552 free base
|
GABA Receptor
|
Neurological Disease
|
S-8510 free base is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.
|
-
-
- HY-A0198A
-
U 41123F mesylate
|
GABA Receptor
|
Neurological Disease
|
Adinazolam (U 41123F) mesylate is a triazolobenzodiazepine. Adinazolam mesylate binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam mesylate has dual anxiolytic and antidepressant activities .
|
-
-
- HY-W634748
-
Bromonordiazepam
|
GABA Receptor
|
Neurological Disease
|
Desalkylgidazepam is a benzodiazepine compound and Gidazepam (HY-U00315) metabolite. Desalkylgidazepam can activate GABA A receptor and translocator protein (TSPO) .
|
-
-
- HY-B0009R
-
|
GABA Receptor
|
Neurological Disease
|
Flumazenil (Standard) is the analytical standard of Flumazenil. This product is intended for research and analytical applications. Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
|
-
-
- HY-B0548
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist.
Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder .
|
-
- HY-100140R
-
PK-8165 (Standard)
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
Pipequaline (Standard) is the analytical standard of Pipequaline. This product is intended for research and analytical applications. Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity .
|
-
- HY-19371
-
|
GABA Receptor
|
Neurological Disease
|
Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
|
-
- HY-19082
-
|
GABA Receptor
|
Neurological Disease
|
Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders .
|
-
- HY-B0548A
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-15527
-
AC-5216; XBD-173
|
Antibiotic
|
Neurological Disease
Metabolic Disease
|
Emapunil (AC-5216), an orally active and selective TSPO (a mitochondrial benzodiazepine receptor) ligand, produces anti-anxiety and antidepressant-like effects in various animal models .
|
-
- HY-121116
-
|
GABA Receptor
|
Neurological Disease
|
CGS 8216, a benzodiazepine receptor antagonist, inhibits 3H-flunitrazepam ( 3H-FLU) binding to rat synaptosomal membranes in vitro at subnanomolar concentrations .
|
-
- HY-19006
-
|
GABA Receptor
|
Neurological Disease
|
ZK-91296 is a GABA receptor agonist with anxiolytic activity. ZK-91296 can reduce anxiety in animals without causing sedation. ZK-91296 may have pharmacological selectivity for interaction with specific types of benzodiazepine receptors .
|
-
- HY-139145S
-
Trimethylopropane phosphate-13C3
|
GABA Receptor
|
Neurological Disease
|
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
|
-
- HY-114706
-
MDL-26479
|
GABA Receptor
|
Neurological Disease
|
Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on GABAA ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases .
|
-
- HY-106025
-
AC-3933
|
GABA Receptor
|
Neurological Disease
|
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively .
|
-
- HY-121877S
-
|
Isotope-Labeled Compounds
GABA Receptor
|
Neurological Disease
|
Valnoctamide-d5 is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors .
|
-
- HY-131941
-
|
GABA Receptor
|
Neurological Disease
|
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
|
-
- HY-105056
-
Ro 16-6028
|
GABA Receptor
|
Neurological Disease
|
Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
|
-
- HY-B0548AS2
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine-d8 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-B0548AS1
-
Vistaril-d4' dihydrochloride; Atarax-dd4' dihydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-U00199A
-
(S)-N-Desmethyl zopiclone; SEP-174559
|
GABA Receptor
nAChR
iGluR
|
Neurological Disease
|
(S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABAA receptor and inhibits nACh and NMDA receptors .
|
-
- HY-B0548R
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine (Standard) is the analytical standard of Hydroxyzine. This product is intended for research and analytical applications. Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder .
|
-
- HY-B0548AR
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine (dihydrochloride) (Standard) is the analytical standard of Hydroxyzine (dihydrochloride). This product is intended for research and analytical applications. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-A0198S
-
U 41123-d5
|
Isotope-Labeled Compounds
GABA Receptor
|
Neurological Disease
|
Adinazolam-d5 (U 41123-d5) is a deuterium labeled Adinazolam (HY-A0198). Adinazolam is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities .
|
-
- HY-17617
-
Z-360
|
Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
|
Neurological Disease
Cancer
|
Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
|
-
- HY-103505
-
|
GABA Receptor
|
Neurological Disease
|
CL 218872 is an orally active and selective ligand for the benzodiazepine receptor subtype BZ1. CL 218872 exhibits anxiolytic, sedative and anticonvulsant activities. CL 218872 can be used in researches of anxiety related disorders and epilepsy .
|
-
- HY-128174
-
Beta-CCM; Ro 22-7497
|
GABA Receptor
|
Neurological Disease
|
β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and proconvulsant effects. β-CCM enhances emotional reactivity and reduces vulnerability to interference in spatial working memory tasks. β-CCM can be used for research on anxiety-related disorders .
|
-
- HY-16579
-
HOE 36-801 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-16579A
-
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-14575
-
Z-360 hemicalcium
|
Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
|
Neurological Disease
Cancer
|
Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain .
|
-
- HY-105115
-
ZK 112119
|
GABA Receptor
|
Neurological Disease
|
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research .
|
-
- HY-123249
-
|
GABA Receptor
|
Neurological Disease
|
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16579AS2
-
|
GABA Receptor
|
Neurological Disease
|
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-103511
-
|
GABA Receptor
|
Neurological Disease
|
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion .
|
-
- HY-108035
-
MR04A3
|
GABA Receptor
|
Neurological Disease
|
(-)-JM-1232 (MR04A3) targets GABA A receptors and exerts its analgesic effects by binding to the benzodiazepine binding site of GABA A receptors. (-)-JM-1232 demonstrates potent analgesic effects in mice against acute thermal stimuli, mechanically induced pain, and visceral pain, with CI50 values of 2.96, 3.06, and 2.27 mg/kg, respectively. (-)-JM-1232 can be used in research related to pain and analgesia .
|
-
- HY-137494
-
|
GABA Receptor
|
Neurological Disease
|
Ethyl β-carboline-3-carboxylate (fl-CCE) is a ligand and short-acting antagonist of benzodiazepine receptors. Ethyl β-carboline-3-carboxylate did not affect cerebellar cGMP levels when used alone, but when taken together with Diazepam, it significantly inhibited the cGMP levels that were upregulated by Diazepam .
|
-
- HY-16579AR
-
|
GABA Receptor
|
Neurological Disease
|
Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-N8852
-
6-MeOF
|
GABA Receptor
|
Neurological Disease
|
6-Methoxyflavanone (6-MeOF) is an orally active flavonoid compound. 6-Methoxyflavanone has anxiolytic properties. 6-Methoxyflavanone targets unique sites on GABA-A receptors, different from traditional benzodiazepines. 6-Methoxyflavanone can be used to study anxiety disorders. 6-Methoxyflavanone readily crosses the blood brain barrier (BBB) .
|
-
- HY-Y0265
-
Indoline-2,3-dione
|
Monoamine Oxidase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
|
-
- HY-N1951
-
Rosmariquinone
|
GABA Receptor
Apoptosis
Carboxylesterase (CES)
SARS-CoV
|
Neurological Disease
Cancer
|
Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro) .
|
-
- HY-100991
-
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .
|
-
- HY-101392
-
Harmane
1 Publications Verification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-101392A
-
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-103521
-
|
GABA Receptor
|
Neurological Disease
|
Anxiolytic/nonsedative agent-1 (compound 2b) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo .
|
-
- HY-W394903R
-
|
JAK
Drug Metabolite
|
Cancer
|
Isatin (Standard) is the analytical standard of Isatin. This product is intended for research and analytical applications. Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
|
-
- HY-Y0265R
-
|
Monoamine Oxidase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Isatin (Standard) is the analytical standard of Isatin. This product is intended for research and analytical applications. Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
|
-
- HY-103512
-
|
GABA Receptor
|
Neurological Disease
|
TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors .
|
-
- HY-100991R
-
ZK 39106 (Standard); LSU-65 (Standard)
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
FG 7142 (Standard) is the analytical standard of FG 7142. This product is intended for research and analytical applications. FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .
|
-
- HY-W700834
-
|
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
|
Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-W777360
-
|
Isotope-Labeled Compounds
Adrenergic Receptor
Monoamine Oxidase
nAChR
Opioid Receptor
Imidazoline Receptor
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-115857
-
|
GABA Receptor
|
Neurological Disease
|
SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
|
-
- HY-N7110
-
|
Akt
ERK
JNK
GABA Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
|
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N6648
-
-
-
- HY-110399
-
-
-
- HY-Y0265
-
-
-
- HY-N1951
-
-
-
- HY-101392
-
Harmane
1 Publications Verification
|
Alkaloids
Structural Classification
other families
Source classification
Pyridine Alkaloids
Plants
Indole Alkaloids
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
-
- HY-N7110
-
-
-
- HY-101392A
-
|
Apocynaceae
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Plants
Rauwolfia canescens
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
-
- HY-Y0265R
-
|
Alkaloids
Structural Classification
other families
Source classification
Plants
Indole Alkaloids
|
Monoamine Oxidase
Apoptosis
|
Isatin (Standard) is the analytical standard of Isatin. This product is intended for research and analytical applications. Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0548AS1
-
|
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
-
- HY-139145S
-
|
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
|
-
-
- HY-121877S
-
|
Valnoctamide-d5 is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors .
|
-
-
- HY-B0548AS2
-
|
Hydroxyzine-d8 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
-
- HY-A0198S
-
|
Adinazolam-d5 (U 41123-d5) is a deuterium labeled Adinazolam (HY-A0198). Adinazolam is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities .
|
-
-
- HY-16579AS2
-
|
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
-
- HY-W700834
-
|
Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
-
- HY-W777360
-
|
Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-103476
-
|
|
Azide
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-123249
-
|
|
Alkynes
|
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: