5-HT2A SNPs Alter the Pharmacological Signaling of Potentially Therapeutic Psychedelics.
ACS Chem Neurosci
; 13(16): 2386-2398, 2022 08 17.
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| ID: mdl-35894503
ABSTRACT
Serotonin (5-hydroxytryptamine; 5-HT) 2A receptor (5-HT2AR) signaling is essential for the actions of classical psychedelic drugs. In this study, we examined whether sequence variations in the 5-HT2AR gene affect the signaling of four commonly used psychedelic drugs. We examined the in vitro pharmacology of seven non-synonymous single-nucleotide polymorphisms (SNPs), which give rise to Ser12Asn, Thr25Asn, Asp48Asn, Ile197Val4.47, Ala230Thr, Ala447Val, and His452Tyr variant 5-HT2A serotonin receptors. We found that these non-synonymous SNPs exert statistically significant, although modest, effects on the efficacy and potency of four therapeutically relevant psychedelics. Significantly, the in vitro pharmacological effects of the SNP drug actions at 5-HT2AR are drug specific.
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MEDLINE
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Alucinógenos
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En
Revista:
ACS Chem Neurosci
Año:
2022
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Article
País de afiliación:
Estados Unidos