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Effects of guanine nucleotides on cns neuropeptide receptors

✍ Scribed by Moody, Terry W. ;Taylor, Duncan P. ;Pert, Candace B.

Publisher
Wiley (John Wiley & Sons)
Year
1981
Tongue
English
Weight
370 KB
Volume
15
Category
Article
ISSN
0275-3723

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✦ Synopsis

Abstract

The effect of nucleotides on central nervous system neuropeptide receptor binding was investigated. The guanine nucleotides, guanosine‐5′‐triphosphate and guanylyl‐5′‐imidodiphosphate, significantly inhibited the binding of radiolabeled vasoactive intestinal polypeptide but not that of [Tyr^4^]bombesin to rat brain membranes. Vasoactive intestinal polypeptide binding was inhibited by guanine nucleotides in a dose‐dependent manner. Using a 20 μM dose, 60% of the specific vasoactive intestinal polypeptide binding was inhibited by guanylyl‐5′‐imidodiphosphate, which was more potent than guanosine‐5′‐triphosphate, whereas other nucleotides were not effective. This reduction in binding was a consequence of lower affinity of the receptor for vasoactive intestinal polypeptide, which in turn resulted from an increased rate of dissociation.

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