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Identification and affinity of very high affinity binding sites for the phenylalkylamine series of Ca/sup +/ channel blockers in the Drosophila nervous system

Journal Article · · Biochemistry; (United States)
OSTI ID:5513018
; ; ; ; ; ; ;
The interaction of putative Ca/sup 2 +/ channels of Drosophila head membranes with molecules of the phenylalkylamine series was studied from binding experiments using (-)-(/sup 3/H)D888 and (+/-)-(/sup 3/H)verapamil. These ligands recognize a single class of very high affinity binding sites. The most potent molecule in the phenylalkylamine series was (-)-verapamil with a K/sub d/ value as exceptional low as 4.7 pM. Molecules in the benzothiazepine and diphenylbutylpiperidine series of Ca/sup 2 +/ channel blockers as well as bepridil inhibited (-)-(/sup 3/H)D888 binding in a competitive way with K/sub d/ values between 12 and 190 nM, suggesting a close correlation, as in the mammalian system, between these receptor sites and those recognizing phenylalkylamines. A tritiated (arylazido)phenylalkylamine with high affinity for the Drosophila head membranes, phenylalkylamine receptor was used in photoaffinity experiments. A protein of M/sub r/ 135,000 +/- 5000 was specifically labeled after ultraviolet irradiation.
Research Organization:
CNRS, Nice, France
OSTI ID:
5513018
Journal Information:
Biochemistry; (United States), Journal Name: Biochemistry; (United States) Vol. 26:20; ISSN BICHA
Country of Publication:
United States
Language:
English

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Related Subjects

550201 -- Biochemistry-- Tracer Techniques
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ALKALINE EARTH METAL COMPOUNDS
AMINES
ANILINE
ANIMALS
AROMATICS
ARTHROPODS
BIOCHEMICAL REACTION KINETICS
CALCIUM COMPOUNDS
CELL CONSTITUENTS
CELL MEMBRANES
DIPTERA
DROSOPHILA
FLIES
FRUIT FLIES
INSECTS
INVERTEBRATES
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIGANDS
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
PROTEINS
RADIORECEPTOR ASSAY
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS