EFFECT OF CHIRALITY ON SEROTONIN RECEPTOR AFFINITY

被引:15
作者
GLENNON, RA
机构
[1] Department of Pharmaceutical Chemistry School, Pharmacy Medical College, Virginia Virginia Commonwealth University Richmond
关键词
D O I
10.1016/0024-3205(79)90032-8
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
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. © 1979.
引用
收藏
页码:1487 / 1492
页数:6
相关论文
共 15 条
  • [1] STRUCTURE-ACTIVITY-RELATIONSHIPS IN PSYCHOTOMIMETIC PHENYLALKYLAMINES
    ALDOUS, FAB
    BARRASS, BC
    BREWSTER, K
    BUXTON, DA
    GREEN, DM
    PINDER, RM
    RICH, P
    SKEELS, M
    TUTT, KJ
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1974, 17 (10) : 1100 - 1111
  • [2] Anderson G. M., 1978, QUASAR QUANTITATIVE, P8
  • [3] SOME QUANTITATIVE USES OF DRUG ANTAGONISTS
    ARUNLAKSHANA, O
    SCHILD, HO
    [J]. BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1959, 14 (01): : 48 - 58
  • [4] COMPARATIVE EFFECTS OF STEREOISOMERS OF HALLUCINOGENIC AMPHETAMINES
    BENINGTON, F
    MORIN, RD
    BEATON, J
    SMYTHIES, JR
    BRADLEY, RJ
    [J]. NATURE-NEW BIOLOGY, 1973, 242 (119): : 185 - 186
  • [5] Brimblecombe RW., 1975, HALLUCINOGENIC AGENT
  • [6] COMPARATIVE EFFECTS OF STEREOISOMERS OF PSYCHOTOMIMETIC PHENYLISOPROPYLAMINES
    DYER, DC
    NICHOLS, DE
    RUSTERHOLZ, DB
    BARFKNECHT, CF
    [J]. LIFE SCIENCES, 1973, 13 (07) : 885 - 896
  • [7] SEROTONIN RECEPTOR-BINDING AFFINITIES OF SEVERAL HALLUCINOGENIC PHENYLALKYLAMINE AND N,N-DIMETHYLTRYPTAMINE ANALOGS
    GLENNON, RA
    LIEBOWITZ, SM
    MACK, EC
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1978, 21 (08) : 822 - 825
  • [8] GLENNON RA, 1975, PHARMACOLOGIST, V17, P259
  • [9] HARRIS RA, 1977, PHARMACOL BIOCHEM BE, V7, P307
  • [10] KIER KB, 1978, QUASAR22 RES MON, P159