mAChR1 Modulator

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).

Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states.

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.

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.

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).

VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC₅₀: 492 nM). VU0467319 is selective (EC₅₀ > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research.

VU0119498 is a pan G_q mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC₅₀s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity.

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).

VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC₅₀ value of 155 nM. VU6004256 has the potential for the research of schizophrenia.

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.

VU6052254, a derivative of VU0467319 (HY-173396), is a selective, potent, orally active and brain-penetrant muscarinic M1 acetylcholine receptor (mAChR1) positive allosteric modulator with an EC₅₀ of 59 nM. VU6052254 has no activity on the M2-5 receptor (EC₅₀ > 30 μM). VU6052254 can improve memory recognition ability and reverse the cognitive impairment induced by Scopolamine (HY-N0296) with minimum effective dose both of 1 mg/kg. VU6052254 can be used for the research of neurological disease, such as Alzheimer's disease.

M1 mAChR modulator-1 (Example 66) is a muscarinic M1 receptor (mAChR1) positive allosteric modulator. M1 mAChR modulator-1 effectively promotes gastrointestinal motility and defecation in mouse models with low central permeability. M1 mAChR modulator-1 can be used for constipation research.

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.

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.

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).

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.

M1 receptor modulator-1 is a low-efficacy positive allosteric modulator of the muscarinic M1 receptor (mAChR1), with an EC₅₀ of 71 nM for the human M1 receptor. M1 receptor modulator-1 enables use-dependent attenuation of neurotransmitter signals and exhibits excellent in vivo properties without pseudo-agonist activity. M1 receptor modulator-1 can be used in research related to Alzheimer's disease and schizophrenia.