Nichols D E, Monte A, Huang X, Marona-Lewicka D
Department of Medical Chemistry and Pharmacognosy, Purdue University, West Lafayette, IN 47907, USA.
Behav Brain Res. 1996;73(1-2):117-9. doi: 10.1016/0166-4328(96)00080-0.
Studies of the affinities for serotonin 5-HT2A and 5-HT1A receptor subtypes of lysergic acid amides prepared from chiral 2-aminoalkanes showed a stereoselective preference at both receptor types for the amides with alkyl groups containing the R configuration. The 5-HT2A receptor was less tolerant of long alkyl groups than was the 5-HT1A subtype. In vivo assays in rats trained to discriminate LSD from saline also showed that amides with alkyl groups having the R configuration were most potent.
对手性2-氨基烷烃制备的麦角酸酰胺的血清素5-HT2A和5-HT1A受体亚型亲和力的研究表明，在这两种受体类型上，对于含有R构型烷基的酰胺均存在立体选择性偏好。与5-HT1A亚型相比，5-HT2A受体对长烷基的耐受性更低。在经过训练可区分LSD和生理盐水的大鼠体内试验中也表明，具有R构型烷基的酰胺活性最强。
