| Autor: |
Schmitz GP; Department of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599-7365, United States., Jain MK; Department of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599-7365, United States., Slocum ST; Department of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599-7365, United States., Roth BL; Department of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599-7365, United States. |
| Jazyk: |
angličtina |
| Zdroj: |
ACS chemical neuroscience [ACS Chem Neurosci] 2022 Aug 17; Vol. 13 (16), pp. 2386-2398. Date of Electronic Publication: 2022 Jul 27. |
| DOI: |
10.1021/acschemneuro.1c00815 |
| Abstrakt: |
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, Ile197Val 4.47 , 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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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