PURINERGIC INHIBITION OF DIAZEPAM BINDING TO RAT-BRAIN (INVITRO)

被引：210

作者：

MARANGOS, PJ ^{[1
]}

PAUL, SM ^{[1
]}

PARMA, AM ^{[1
]}

GOODWIN, FK ^{[1
]}

SYAPIN, P ^{[1
]}

SKOLNICK, P ^{[1
]}

机构：

[1] NIAAA,BETHESDA,MD 20014

来源：

LIFE SCIENCES | 1979年 / 24卷 / 09期

关键词：

D O I：

10.1016/0024-3205(79)90369-2

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：

Our recent report that the endogenous purines inosine and hypoxanthine competitively inhibit [3H] diazepam binding to rat brain synaptosomal membranes (1,2) has now been confirmed (3). We now report that a wide spectrum of purines are able to inhibit specific [3H] diazepam binding while pyrimidines are inactive. Preliminary structure activity relationships indicate that the 2′-deoxypurines are more potent in diazepam binding inhibition as are the l-methyl compounds, whereas the 7-methyl purines are inactive. Data are also presented which show that the xanthine stimulants caffeine, theophylline, and theobromine as well as the central nervous system convulsant pentylenetetrazol all competitively inhibit [3H] diazepam binding. © 1979.

引用

页码：851 / 857

页数：7

共 16 条

[1]

ASANO T, P NAT ACAD SCI

[2] DIAZEPAM RECEPTOR CHARACTERIZATION - SPECIFIC BINDING OF A BENZODIAZEPINE TO MACROMOLECULES IN VARIOUS AREAS OF RAT-BRAIN [J].