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Results for "

muscarinic M1 receptor agonist

" in MedChemExpress (MCE) Product Catalog:

52

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-116480
    LY593093

    		mAChR Neurological Disease
    LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC50 of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research .
    LY593093
  • HY-100336
    AC260584
    1 Publications Verification

    		 mAChR Neurological Disease
    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
    AC260584
  • HY-U00230
    CDD0102

    CDD0102A

    		 mAChR Neurological Disease
    CDD0102 is a potent M1 Muscarinic receptor agonist.
    CDD0102
  • HY-U00230A
    CDD0102 hydrochloride

    		mAChR Neurological Disease
    CDD0102 Hydrochloride is a potent M1 Muscarinic receptor agonist.
    CDD0102 hydrochloride
  • HY-120418
    L-687306

    		mAChR Others
    L-687306 is a high affinity muscarinic M1 receptor partial agonist with activity as a partial agonist of M1 receptors in rat ganglia and as a high affinity competitive antagonist at guinea pig cardiac M2 and ileal M3 muscarinic receptors, useful for studying the receptor reserve of muscarinic receptors.
    L-687306
  • HY-U00038
    ENS-163 phosphate

    ENS 213-163; Sandoz ENS 163 phosphate; Thiopilocarpine phosphate

    		 mAChR Neurological Disease
    ENS-163 phosphate is a selective muscarinic M1 receptor agonist.
    ENS-163 phosphate
  • HY-119082A
    VU0029767

    		mAChR Others
    VU0029767 is an allosteric enhancer of the M1 muscarinic receptor with the activity to modulate M1 receptor activity. VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
    VU0029767
  • HY-119082
    (E/Z)-VU0029767

    		mAChR Others
    (E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
    (E/Z)-VU0029767
  • HY-B1789
    Telenzepine

    		mAChR Neurological Disease
    Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM) .
    Telenzepine
  • HY-118806
    AC-42

    		mAChR Neurological Disease
    AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
    AC-42
  • HY-106432A
    Sabcomeline hydrochloride

    SB-202026 hydrochloride; Memric hydrochloride

    		 mAChR Neurological Disease
    Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research .
    Sabcomeline hydrochloride
  • HY-106432
    Sabcomeline

    SB-202026; Memric

    		 mAChR Neurological Disease
    Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research .
    Sabcomeline
  • HY-118806A
    AC-42 hydrochloride

    		mAChR Neurological Disease
    AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .
    AC-42 hydrochloride
  • HY-105182
    Xanomeline
    5 Publications Verification

    LY-246708

    		 mAChR Neurological Disease
    Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
    Xanomeline
  • HY-15618
    MK-7622

    M1 receptor modulator

    		 mAChR Calcium Channel Neurological Disease
    MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC50 = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD) .
    MK-7622
  • HY-106949
    Tazomeline

    		mAChR Neurological Disease
    Tazomeline is a selective M1 muscarinic receptor agonist. Tazomeline inhibits twitch height in rabbit vas deferens(IC50= 0.001 nM). Tazomeline can be used for research of neuropsychiatric disorders .
    Tazomeline
  • HY-116586
    AF710B

    		Sigma Receptor Neurological Disease
    AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .
    AF710B
  • HY-120329
    Lu 26-046

    		mAChR Others
    Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
    Lu 26-046
  • HY-105182A
    Xanomeline tartrate
    5 Publications Verification

    LY 246708 tartrate

    		 mAChR Neurological Disease
    Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .
    Xanomeline tartrate
  • HY-118363
    Lu AE51090

    		mAChR Neurological Disease
    Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS) .
    Lu AE51090
  • HY-19752A
    VU0357017 hydrochloride

    CID-25010775

    		 mAChR Neurological Disease
    VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia .
    VU0357017 hydrochloride
  • HY-105182R
    Xanomeline (Standard)

    LY-246708 (Standard)

    		 Reference Standards mAChR Neurological Disease
    Xanomeline (Standard) is the analytical standard of Xanomeline. This product is intended for research and analytical applications. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
    Xanomeline (Standard)
  • HY-113616
    VU0364572

    		mAChR MARCKS Neurological Disease
    VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant .
    VU0364572
  • HY-105182S1
    Xanomeline-d3

    LY-246708-d3

    		 Isotope-Labeled Compounds mAChR Neurological Disease
    Xanomeline-d3 (LY-246708-d3) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
    Xanomeline-d3
  • HY-113616A
    VU0364572 TFA

    		MARCKS mAChR Neurological Disease
    VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant .
    VU0364572 TFA
  • HY-116586A
    (Rac)-AF710B

    		mAChR Sigma Receptor Neurological Disease
    (Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .
    (Rac)-AF710B
  • HY-14539B
    Clozapine dihydrochloride

    HF 1854 dihydrochloride

    		 Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor Neurological Disease Cancer
    Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
    Clozapine dihydrochloride
  • HY-14539
    Clozapine
    Maximum Cited Publications
    10 Publications Verification

    HF 1854

    		 Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor Neurological Disease Cancer
    Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
    Clozapine
  • HY-14539A
    Clozapine hydrochloride

    HF 1854 hydrochloride

    		 Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor Neurological Disease
    Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
    Clozapine hydrochloride
  • HY-76772
    Cevimeline hydrochloride hemihydrate
    2 Publications Verification

    SNI-2011; AF102B hydrochloride hemihydrate

    		 mAChR Neurological Disease Cancer
    Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
    Cevimeline hydrochloride hemihydrate
  • HY-70020B
    Cevimeline hydrochloride
    2 Publications Verification

    AF102B hydrochloride

    		 mAChR Neurological Disease Cancer
    Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
    Cevimeline hydrochloride
  • HY-105182AR
    Xanomeline tartrate (Standard)

    LY 246708 tartrate (Standard)

    		 Reference Standards mAChR Neurological Disease
    Xanomeline (tartrate) (Standard) is the analytical standard of Xanomeline (tartrate). This product is intended for research and analytical applications. Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .
    Xanomeline tartrate (Standard)
  • HY-70020
    Cevimeline
    2 Publications Verification

    AF102B

    		 mAChR Neurological Disease Cancer
    Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline can cross the blood-brain barrier (BBB) .
    Cevimeline
  • HY-14539R
    Clozapine (Standard)
    Maximum Cited Publications
    10 Publications Verification

    HF 1854 (Standard)

    		 Reference Standards Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor Neurological Disease
    Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
    Clozapine (Standard)
  • HY-107656
    PTAC oxalate

    		mAChR Neurological Disease
    PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .
    PTAC oxalate
  • HY-32067
    Aceclidine

    Quinuclidin-3-yl acetate

    		 mAChR Cardiovascular Disease Neurological Disease
    Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
    Aceclidine
  • HY-32067A
    Aceclidine hydrochloride

    Quinuclidin-3-yl acetate hydrochloride

    		 mAChR Neurological Disease
    Aceclidine (Quinuclidin-3-yl acetate) hydrochloride is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine hydrochloride is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine hydrochloride has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
    Aceclidine hydrochloride
  • HY-119333
    NNC 11-1607

    		mAChR Neurological Disease
    NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia .
    NNC 11-1607
  • HY-76772R
    Cevimeline hydrochloride hemihydrate (Standard)

    		mAChR Neurological Disease Cancer
    Cevimeline (hydrochloride hemihydrate) (Standard) is the analytical standard of Cevimeline (hydrochloride hemihydrate). This product is intended for research and analytical applications. Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
    Cevimeline hydrochloride hemihydrate (Standard)
  • HY-70020BR
    Cevimeline hydrochloride (Standard)

    		mAChR Neurological Disease Cancer
    Cevimeline (hydrochloride) (Standard) is the analytical standard of Cevimeline (hydrochloride). This product is intended for research and analytical applications. Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
    Cevimeline hydrochloride (Standard)
  • HY-14539S3
    Clozapine-d3

    HF 1854-d3

    		 Isotope-Labeled Compounds 5-HT Receptor Adrenergic Receptor Dopamine Receptor mAChR Neurological Disease Cancer
    Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
    Clozapine-d3
  • HY-107650
    Milameline hydrochloride

    CI 979 hydrochloride; RU 35926 hydrochloride

    		 mAChR Neurological Disease
    Milameline (CI 979; RU35926) hydrochloride is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydrochloride has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydrochloride has a higher affinity for sites [ 3H]CMD (IC50 = 20 nM), than [ 3H]QNB, (IC50 = 3059 nM). Milameline hydrochloride produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydrochloride can be used for the study of Alzheimer’s Disease .
    Milameline hydrochloride
  • HY-135460
    Milameline

    CI-979; RU35926

    		 mAChR Neurological Disease
    Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [ 3H]CMD (IC50 = 20 nM), than [ 3H]QNB, (IC50 = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease .
    Milameline
  • HY-107650A
    Milameline hydroiodide

    CI 979 hydroiodide; RU 35926 hydroiodide

    		 mAChR Neurological Disease
    Milameline (CI 979; RU35926) hydroiodide is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydroiodide has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydroiodide has a higher affinity for sites [ 3H]CMD (IC50 = 20 nM), than [ 3H]QNB, (IC50 = 3059 nM). Milameline hydroiodide produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydroiodide can be used for the study of Alzheimer’s Disease .
    Milameline hydroiodide
  • HY-N4157
    Isopteropodine

    		mAChR 5-HT Receptor Bacterial Neurological Disease
    Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
    Isopteropodine
  • HY-101341
    RS 67333 hydrochloride

    		5-HT Receptor Neurological Disease
    RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
    RS 67333 hydrochloride
  • HY-N4157R
    Isopteropodine (Standard)

    		Reference Standards mAChR 5-HT Receptor Bacterial Neurological Disease
    Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
    Isopteropodine (Standard)
  • HY-B0527A
    Amitriptyline hydrochloride
    5+ Cited Publications

    		 Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline hydrochloride
  • HY-B0527
    Amitriptyline
    5+ Cited Publications

    		 Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d6 hydrochloride

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