The effect of chirality on serotonin receptor affinity. |
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Authors: | R A Glennon |
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Institution: | Department of Pharmaceutical Chemistry School of Pharmacy Medical College of Virginia Virginia Commonwealth University Richmond, Virginia 23298, USA |
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Abstract: | α-Methylation of phenethylamines or tryptamine appears to have very little effect on serotonin (5-HT) receptor affinity when racemates are examined. Examination of resolved materials, using an isolated rat stomach fundus preparation, reveals that the R-isomers of DOM and MDA and the S-isomer of α-methlytryptamine possess a higher 5-HT receptor affinity than do their enantiomers. While S(+)-DOB possesses a lower affinity than its racemate, R(-)-DOB produces an appreciable agonistic response which interferes with the measurement of pA2 values. |
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