Inhibition of [3H]diazepam binding in primary cultures of astrocytes by atrial natriuretic peptide and by a cyclic GMP analog.
Atrial natriuretic peptide (ANP) was found potently (IC50 = 88 nM) to inhibit [3H]diazepam binding to astrocytes in primary cultures but not to a corresponding preparation of neurons. Based upon this finding and literature data demonstrating a pronounced correlation between the distribution of 'peripheral-type' benzodiazepine receptors and ANP receptors, it is suggested that ANP may be an allosteric regulator of the astrocytic benzodiazepine binding site. Since ANP is known to increase the level of cGMP it was also investigated whether 8-bromoguanosine 3':5' cyclic monophosphate, a permeable cGMP analog, displaced diazepam binding. This was the case, suggesting that cGMP might be involved in the ANP effect on the astrocytic benzodiazepine receptor.
Bender
A S
AS
Department of Pharmacology, University of Saskatchewan, Saskatoon, Canada.
Hertz
L
L
D000818:Animals; D001253:Astrocytes / Q000187:drug effects / Q000378:metabolism*; D009320:Atrial Natriuretic Factor / Q000494:pharmacology*; D002478:Cells, Cultured; D006152:Cyclic GMP / Q000031:analogs & derivatives* / Q000494:pharmacology; D003975:Diazepam / Q000378:metabolism*; D051379:Mice
C016276:8-bromocyclic GMP; D009320:Atrial Natriuretic Factor; D006152:Cyclic GMP; D003975:Diazepam