mAChR4 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.

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).

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).

VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia.

VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC₅₀ values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic.

VU6002703 (Compound 17) is a BBB-penetrable M4 mAChR positive allosteric modulator (PAM) with an EC₅₀ of 0.6  μM for hM4. VU6002703 can be used for neuropsychiatric and rare genetic CNS disorders 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.

Muscarinic M4 modulator-1 is a Muscarinic M4 receptor positive allosteric modulator. Muscarinic M4 modulator-1 activates the muscarinic M4 receptor with allosteric potency EC₅₀ s of 14 and 3 Nm in CHO-K1 cells and HEK293 cells. Muscarinic M4 modulator-1 has an antipsychotic-like activity, promising for psychiatric and/or neurological disorders research.

M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment.

VU6009048 is a CNS-penetrant human M4 muscarinic acetylcholine receptor (mAChR4) positive allosteric modulator. VU6009048 can be used for the research of parkinson’s disease, huntington’s disease, schizophrenia.

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).