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Emraclidine

From Wikipedia, the free encyclopedia
Chemical compound
This article needs to beupdated. Please help update this article to reflect recent events or newly available information.(February 2025)
Pharmaceutical compound
Emraclidine
Clinical data
Other namesCVL-231; PF-06852231
Identifiers
  • 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
PubChemCID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC20H21F3N4O
Molar mass390.410 g·mol−1
3D model (JSmol)
  • CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C
  • 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 namesCVL-231,PF-06852231) is an investigationalantipsychotic for the treatment of bothschizophrenia andAlzheimer's disease psychosis developed byCerevel Therapeutics.[1][2] As of August 2024, it is inphase 2clinical trials.[1][3]

Emraclidine is apositive allosteric modulator that selectively targets themuscarinic acetylcholine receptor M4 subtype. The M4 receptor subtype is expressed in thestriatum of the brain, which plays a key role in regulatingacetylcholine anddopamine levels. An imbalance of these neurotransmitters has been linked to psychotic symptoms in schizophrenia. Unlike othermuscarinic receptors, M4 receptor subtypes are selectively expressed in the striatum and activation of these receptors has been shown to indirectly regulate dopamine levels without blockingD2/D3 receptors, which may lead to unwanted motor side effects seen in current antipsychotics.[4]

Further reading

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See also

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References

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  1. ^ab"Emraclidine - Cerevel Therapeutics".AdisInsight. 28 August 2024. Retrieved20 October 2024.
  2. ^"Emraclidine".Cerevel Therapeutics. 4 January 2020. Retrieved2023-02-15.
  3. ^Clinical trial numberNCT05227690 for "A Trial of 10 and 30 mg Doses of CVL-231 (Emraclidine) in Participants With Schizophrenia" atClinicalTrials.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.
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(andprodrugs)


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