Chemistry:Emraclidine
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| Formula | C20H21F3N4O |
| Molar mass | 390.410 g·mol−1 |
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Emraclidine (developmental code name CVL-231) is an investigational antipsychotic for the treatment of both schizophrenia and Alzheimer’s disease psychosis developed by Cerevel Therapeutics.[1] As of February 2023, it is in phase II of clinical trial.[2] Emraclidine is a positive allosteric modulator that selectively targets the muscarinic acetylcholine receptor M4 subtype. The M4 receptor subtype is expressed in the striatum of the brain, which plays a key role in regulating acetylcholine and dopamine levels. An imbalance of these neurotransmitters has been linked to psychotic symptoms in schizophrenia. Unlike other muscarinic receptors, M4 receptor subtypes are selectively expressed in the striatum and activation of these receptors has been shown to indirectly regulate dopamine levels without blocking D2/D3 receptors, which may lead to unwanted motor side effects seen in current antipsychotics.[3]
References
- ↑ "Emraclidine" (in en-US). https://www.cerevel.com/compounds/emraclidine/.
- ↑ Clinical trial number NCT05227690 for "A Trial of 10 and 30 mg Doses of CVL-231 (Emraclidine) in Participants With Schizophrenia" at ClinicalTrials.gov
- ↑ "Emraclidine, a novel positive allosteric modulator of cholinergic M4 receptors, for the treatment of schizophrenia: a two-part, randomised, double-blind, placebo-controlled, phase 1b trial". Lancet 400 (10369): 2210–2220. December 2022. doi:10.1016/S0140-6736(22)01990-0. PMID 36528376.
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