Emraclidine

Emraclidine
Clinical data
Other names	CVL-231; PF-06852231
Identifiers
	IUPAC name 1-(2,4-dimethyl-5,7-dihydropyrrolo[3,4-b]pyridin-6-yl)-2-[1-[2-(trifluoromethyl)pyridin-4-yl]azetidin-3-yl]ethanone;
CAS Number	2170722-84-4;
PubChem CID	140830653;
ChemSpider	114856397;
UNII	J241Y80EEO;
KEGG	D12468;
Chemical and physical data
Formula	C20H21F3N4O
Molar mass	390.410 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C;
	InChI InChI=1S/C20H21F3N4O/c1-12-5-13(2)25-17-11-27(10-16(12)17)19(28)6-14-8-26(9-14)15-3-4-24-18(7-15)20(21,22)23/h3-5,7,14H,6,8-11H2,1-2H3; Key:DTCZNKWBDTXEBS-UHFFFAOYSA-N;

Emraclidine (developmental code names CVL-231, PF-06852231) is an investigational antipsychotic for the treatment of both schizophrenia and Alzheimer's disease psychosis developed by Cerevel Therapeutics.^[1]^[2] As of August 2024, it is in phase 2 clinical trials.^[1]^[3]

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.^[4]

References

^ ^a ^b "Emraclidine - Cerevel Therapeutics". AdisInsight. 28 August 2024. Retrieved 20 October 2024.
^ "Emraclidine". Cerevel Therapeutics. 4 January 2020. Retrieved 2023-02-15.
^ Clinical trial number NCT05227690 for "A Trial of 10 and 30 mg Doses of CVL-231 (Emraclidine) in Participants With Schizophrenia" at ClinicalTrials.gov
^ Krystal JH, Kane JM, Correll CU, Walling DP, Leoni M, Duvvuri S, et al. (December 2022). "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. doi:10.1016/S0140-6736(22)01990-0. PMID 36528376. S2CID 254705359.

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[AdisInsight-1] "Emraclidine - Cerevel Therapeutics". AdisInsight. 28 August 2024. Retrieved 20 October 2024.

[2] "Emraclidine". Cerevel Therapeutics. 4 January 2020. Retrieved 2023-02-15.

[3] Clinical trial number NCT05227690 for "A Trial of 10 and 30 mg Doses of CVL-231 (Emraclidine) in Participants With Schizophrenia" at ClinicalTrials.gov

[4] Krystal JH, Kane JM, Correll CU, Walling DP, Leoni M, Duvvuri S, et al. (December 2022). "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. doi:10.1016/S0140-6736(22)01990-0. PMID 36528376. S2CID 254705359.

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See also

References