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Results for "

muscarinic M1 receptor agonist

" in MedChemExpress (MCE) Product Catalog:

標的別:	mAChR (65) 5-HT Receptor (13) Adrenergic Receptor (9) Amyloid-β (1) Apoptosis (4) Bacterial (2) Calcium Channel (3) Dopamine Receptor (5) Dopamine Transporter (4) Drug Isomer (1) ERK (1) Histamine Receptor (4) Isotope-Labeled Compounds (4) Ligands for E3 Ligase (1) MARCKS (2) Opioid Receptor (1) Potassium Channel (4) Protein Arginine Deiminase (1) Reference Standards (10) Serotonin Transporter (4) Sigma Receptor (2) Sodium Channel (4) Tau Protein (1) Trk Receptor (4)
研究分野別:	Cancer (9) Cardiovascular Disease (1) Endocrinology (4) Inflammation/Immunology (5) Neurological Disease (63)
クリックケミストリー:	Alkynes (1)

阻害剤およびアゴニスト

天然物

同位体標識化合物

クリックケミストリー

Targets Recommended: mAChR

製品番号	製品名	Target	研究分野	構造式

HY-14539

Clozapine Maximum Cited Publications 11 Publications Verification HF 1854; ZINC000019796155	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor Ligands for E3 Ligase	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 K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

HY-105182

Xanomeline 5+ Cited Publications 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 .

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 (K_i = 3.45 nM) and NET (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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 .

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 (K_i = 3.45 nM) and NET (K_i = 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 K_i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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 .

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) .

HY-105182A

Xanomeline tartrate 5+ Cited Publications 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 .

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 .

HY-122190

TAK-071	mAChR	Neurological Disease
TAK-071 is a novel, potent and highly selective **muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC₅₀** of TAK-071 M1R agonist activities is 520 nM .

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) .

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 .

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) .

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) .

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 .

HY-159829

Direclidine NBI-1117568; HTL-0016878	mAChR	Neurological Disease
Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .

HY-101341

RS 67333 hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
RS 67333 hydrochloride is a potent and selective *5-HT4 receptor* (5-HT4R)** partial agonist with a pK_i 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 .

HY-176710

PAD-PF2	Protein Arginine Deiminase Opioid Receptor mAChR	Neurological Disease Inflammation/Immunology Cancer
PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC₅₀ = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC₅₀ = 12.3 μM). The IC₅₀ values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca ²⁺-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .

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 .

HY-100336

AC260584 1 Publications Verification	mAChR	Neurological Disease
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC₅₀ of 7.6.

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) .

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 .

HY-14539A

Clozapine hydrochloride Maximum Cited Publications 11 Publications Verification 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 K_i of 75 nM. Clozapine hydrochloride inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is 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) .

HY-14539R

Clozapine (Standard) Maximum Cited Publications 11 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 K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

HY-116586

AF710B	Sigma Receptor mAChR ERK Amyloid-β Tau Protein	Neurological Disease
AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease .

HY-177410

Muscarinic M1 receptor agonist-1	mAChR	Neurological Disease
Muscarinic M1 receptor agonist-1 (Ex.1-21) is a **Muscarinic M1 receptor** agonist. Muscarinic M1 receptor agonist-1 can be used in the research of psychiatric disorders such as schizophrenia .

HY-B0527AR

Amitriptyline hydrochloride (Standard) 4 Publications Verification	Reference Standards 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 hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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.

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 .

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 .

HY-113970A

Nebracetam hydrochloride WEB 1881 FU hydrochloride	mAChR Calcium Channel	Neurological Disease
Nebracetam (WEB 1881 FU) hydrochloride is an orally active M₁ muscarinic receptor agonist. Nebracetam hydrochloride can induce an increase in intracellular Ca ²⁺ concentration, with an EC₅₀ value of 1.59 mM. Nebracetam hydrochloride exhibits neuroprotective activity and the ability to improve cognitive impairment. Nebracetam hydrochloride can be used in the research of neurological diseases such as Alzheimer's disease .

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 .

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 (K_i = 3.45 nM) and NET (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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.

HY-123852

PF-06764427	mAChR	Neurological Disease
PF-06764427 is a selective M1 muscarinic acetylcholine receptor positive allosteric modulator. PF-06764427 exhibits robust M1 agonist activity. PF-06764427 can be used in the research of Alzheimer's disease and schizophrenia .

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 EC₅₀*s 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 .

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 (K_i 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 .

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.

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 .

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 .

HY-19092

YM-796 dihydroxybutanedioate	mAChR	Neurological Disease
YM-796 dihydroxybutanedioate is a selective **muscarinic M₁ receptor** agonist. YM-796 dihydroxybutanedioate can improve cognitive impairment and reduce amyloid plaque deposition. YM-796 dihydroxybutanedioate can be used in the research of cognitive impairment diseases such as Alzheimer's disease .

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 .

HY-U00230

CDD0102 CDD0102A	mAChR	Neurological Disease
CDD0102 is a potent M₁ Muscarinic receptor agonist.

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.

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.

HY-148961

HTL-9936	mAChR	Neurological Disease
HTL-9936 is a selective M1 muscarinic acetylcholine receptor (M1-mAChR) agonist. HTL-9936 is promising for research of neurodegenerative disorders (e.g., Alzheimer’s) .

HY-120915

L 689660 maleate	mAChR	Neurological Disease
L 689660 maleate, a cholinomimetic agent, is a selective M1 and M3 muscarinic receptors agonist. L 689660 maleate is a potent M1 muscarinic receptor full agonist in the rat superior cervical ganglion (pEC₅₀ of 7.3). L 689660 maleate is a potent M3 receptors agonist in the guinea-pig ileum myenteric plexus-longitudinal muscle or in trachea (pEC₅₀ of 7.5 and 7.7, respectively) .

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) .

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 .

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 .

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 K_i of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .

HY-19752

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

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 .

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 K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the **muscarinic M4 receptor (EC₅₀**=11 nM) .

製品番号	製品名	Category	Target	構造式

HY-N4157

Isopteropodine	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	mAChR 5-HT Receptor Bacterial
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 .

HY-N4157R

Isopteropodine (Standard)	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	Reference Standards mAChR 5-HT Receptor Bacterial
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 .

製品番号	製品名	構造式

HY-105182S1

Xanomeline-d3
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 .

HY-B0527AS

Amitriptyline-d6 hydrochloride

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 (K_i = 3.45 nM) and NET (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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.

HY-14539S3

Clozapine-d3

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 K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM) .

HY-105182S

Xanomeline-d11
Xanomeline-d₁₁ (LY-246708-d₁₁) is the deuterium labeled Xanomeline (HY-105182). 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 .

製品番号	製品名		Classification

HY-120329

Lu 26-046		Alkynes
Lu 26-046 is the agonist for **muscarinic M1 receptor** and M2 receptor and a weak antagonist for M3 receptor, with K_i of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .

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