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Results for "

nAChRs partial agonist

" in MedChemExpress (MCE) Product Catalog:

42

Inhibitors & Agonists

4

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10

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10019
    Varenicline

    CP 526555

    		 nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline
  • HY-10020
    Varenicline Hydrochloride

    CP 526555 hydrochloride

    		 nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Hydrochloride
  • HY-10019A
    Varenicline dihydrochloride

    CP 526555 dihydrochloride

    		 nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline dihydrochloride
  • HY-10021
    Varenicline Tartrate

    CP 526555-18

    		 nAChR ERK p38 MAPK Others Neurological Disease Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Tartrate
  • HY-107680
    3-Pyr-Cytisine

    3-Pyr-Cyt

    		 nAChR Neurological Disease
    3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant .
    3-Pyr-Cytisine
  • HY-10020R
    Varenicline Hydrochloride (Standard)

    CP 526555 hydrochloride (Standard)

    		 Reference Standards nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (Hydrochloride) (Standard) is the analytical standard of Varenicline (Hydrochloride). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Hydrochloride (Standard)
  • HY-10019R
    Varenicline (Standard)

    CP 526555 (Standard)

    		 Reference Standards nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (Standard) is the analytical standard of Varenicline. This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline (Standard)
  • HY-10021R
    Varenicline Tartrate (Standard)

    CP 526555-18 (Standard)

    		 Reference Standards nAChR ERK p38 MAPK Others Neurological Disease
    Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Tartrate (Standard)
  • HY-10019AR
    Varenicline dihydrochloride (Standard)

    CP 526555 dihydrochloride (Standard)

    		 Reference Standards nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (dihydrochloride) (Standard) is the analytical standard of Varenicline (dihydrochloride). This product is intended for research and analytical applications. Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline dihydrochloride (Standard)
  • HY-10019S1
    Varenicline-15N,13C,d2

    CP 526555-15N,13C,d2

    		 nAChR Isotope-Labeled Compounds Neurological Disease Inflammation/Immunology Cancer
    Varenicline- 15N, 13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline-15N,13C,d2
  • HY-10019AS1
    Varenicline-d4 hydrochloride

    		Isotope-Labeled Compounds nAChR Inflammation/Immunology
    Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .
    Varenicline-d4 hydrochloride
  • HY-15430A
    Encenicline hydrochloride
    5 Publications Verification

    EVP-6124 hydrochloride

    		 nAChR Neurological Disease
    Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
    Encenicline hydrochloride
  • HY-15430
    Encenicline

    EVP-6124

    		 nAChR Neurological Disease
    Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
    Encenicline
  • HY-10019S2
    Varenicline-13C15N

    CP 526555-13C,15N

    		 Isotope-Labeled Compounds nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline- 13C 15N (CP 526555- 13C 15N) is 13C and 15N labeled Varenicline. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline-13C15N
  • HY-10020S
    Varenicline-15N3 hydrochloride

    CP 526555-15N3 Hydrochloride

    		 nAChR Isotope-Labeled Compounds Neurological Disease Inflammation/Immunology Cancer
    Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline-15N3 hydrochloride
  • HY-11053
    S 24795

    		nAChR Neurological Disease
    S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the research of aging-related memory disturbances .
    S 24795
  • HY-N0175
    Cytisinicline
    1 Publications Verification

    Cytisine; Sophorine; Baptitoxine

    		 nAChR Metabolic Disease Cancer
    Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
    Cytisinicline
  • HY-10063
    Ispronicline

    TC-1734; ACD3480

    		 nAChR Neurological Disease
    Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
    Ispronicline
  • HY-N0175R
    Cytisinicline (Standard)

    Cytisine (Standard); Sophorine (Standard); Baptitoxine (Standard)

    		 Reference Standards nAChR Metabolic Disease Cancer
    Cytisinicline (Standard) is the analytical standard of Cytisinicline. This product is intended for research and analytical applications. Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
    Cytisinicline (Standard)
  • HY-120609
    BMS-902483

    		nAChR Neurological Disease
    BMS-902483 is a quinuclidine-containing spirooxazolidine that is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). BMS-902483 improves cognitive ability in preclinical rodent models. .
    BMS-902483
  • HY-107671
    DMAB-anabaseine dihydrochloride

    		nAChR Neurological Disease
    DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an α4β2 nAChR antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects .
    DMAB-anabaseine dihydrochloride
  • HY-W743727
    Cytisine-d4

    		Isotope-Labeled Compounds nAChR Metabolic Disease
    Cytisine-d4 is the deuterium labeled Cytisinicline (HY-N0175). Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
    Cytisine-d4
  • HY-116507
    AZD0328

    		nAChR Neurological Disease
    AZD0328 is a selective α7 nAChR partial agonist. AZD0328 selectively enhances midbrain dopaminergic neuronal activity and enhances cortical dopamine levels in rats. AZD0328 improves cognitive performance .
    AZD0328
  • HY-19411
    SSR180711 hydrochloride

    		nAChR Neurological Disease
    SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus .
    SSR180711 hydrochloride
  • HY-10019S
    Varenicline-d4

    CP 526555-d4

    		 Isotope-Labeled Compounds nAChR Neurological Disease
    Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .
    Varenicline-d4
  • HY-115766S
    Anabaseine-d4

    		Isotope-Labeled Compounds nAChR Neurological Disease
    Anabaseine-d4 is the deuterium labeled Anabaseine (HY-115766). Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
    Anabaseine-d4
  • HY-115766R
    Anabaseine (Standard)

    		nAChR Neurological Disease
    Anabaseine (Standard) is the analytical standard of Anabaseine. This product is intended for research and analytical applications. Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
    Anabaseine (Standard)
  • HY-115766
    Anabaseine

    		nAChR Neurological Disease
    Anabaseine, a naturally occurring alkaloid toxin, is potent agonist of multiple nicotinic acetylcholine receptors (AChRs). Anabaseine stimulates the neuromuscular α12β1γδ or α12β1γɛ and α7 AChRs. Anabaseine is also a weak partial agonist at α4β2 nAChRs .
    Anabaseine
  • HY-138879
    CP-601927

    		nAChR Neurological Disease
    CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .
    CP-601927
  • HY-110142
    Thermopsidine

    CC4

    		 nAChR Neurological Disease
    Thermopsidine (CC4) is a selective partial agonist at α4β2/α6β2 nAChR with EC50 values of 2.2 μM target α4β2 .
    Thermopsidine
  • HY-14565
    Pozanicline

    ABT-089

    		 nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .
    Pozanicline
  • HY-19490A
    (S)-VQW-765

    (S)-AQW-051

    		 nAChR Neurological Disease
    (S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia .
    (S)-VQW-765
  • HY-108057
    Facinicline

    RG3487 free base

    		 nAChR 5-HT Receptor Neurological Disease
    Facinicline (RG3487) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
    Facinicline
  • HY-108057A
    Facinicline hydrochloride

    RG3487 hydrochloride

    		 nAChR 5-HT Receptor Neurological Disease
    Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
    Facinicline hydrochloride
  • HY-138879B
    CP-601932

    (1S,5R)-CP-601927

    		 nAChR Neurological Disease
    CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
    CP-601932
  • HY-W002112
    (±)-Nornicotine

    Nornicotine

    		 Endogenous Metabolite Drug Metabolite nAChR β-catenin Cardiovascular Disease Neurological Disease
    (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia .
    (±)-Nornicotine
  • HY-59201A
    A-582941 dihydrochloride

    		nAChR 5-HT Receptor Neurological Disease
    A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
    A-582941 dihydrochloride
  • HY-W002112S
    (±)-Nornicotine-d4

    		nAChR Isotope-Labeled Compounds Endogenous Metabolite Drug Metabolite β-catenin Cardiovascular Disease Neurological Disease
    (±)-Nornicotine-d4 is the deuterium labeled (±)-Nornicotine (HY-W002112). (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia .
    (±)-Nornicotine-d4
  • HY-W002112R
    (±)-Nornicotine (Standard)

    Nornicotine (Standard)

    		 Reference Standards Endogenous Metabolite Drug Metabolite nAChR β-catenin Cardiovascular Disease Neurological Disease
    (±)-Nornicotine (Standard) is the analytical standard of (±)-Nornicotine (HY-W002112). This product is intended for research and analytical applications. (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia .
    (±)-Nornicotine (Standard)
  • HY-W002112S1
    (±)-Nornicotine-d7

    		Isotope-Labeled Compounds Endogenous Metabolite Drug Metabolite nAChR β-catenin Cardiovascular Disease Neurological Disease
    (±)-Nornicotine-d7 is the deuterium labeled (±)-Nornicotine (HY-W002112). (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia .
    (±)-Nornicotine-d7
  • HY-136207
    TC-2559 difumarate

    		nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
    TC-2559 difumarate
  • HY-B0072S
    Tropisetron-d5

    SDZ-ICS-930-d5 free base

    		 Isotope-Labeled Compounds nAChR p38 MAPK 5-HT Receptor AP-1 NF-κB Nuclear Factor of activated T Cells (NFAT) JAK Neurological Disease Inflammation/Immunology Cancer
    Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects .
    Tropisetron-d5

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