CHARACTERIZATION OF ALPHA(2) ADRENOCEPTORS AND OTHER ADRENOCEPTORS INMEMBRANES ISOLATED FROM DOG MESENTERIC NERVE AXONS

Citation
Ee. Daniel et al., CHARACTERIZATION OF ALPHA(2) ADRENOCEPTORS AND OTHER ADRENOCEPTORS INMEMBRANES ISOLATED FROM DOG MESENTERIC NERVE AXONS, The Journal of pharmacology and experimental therapeutics, 275(2), 1995, pp. 978-986
Citations number
52
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00223565
Volume
275
Issue
2
Year of publication
1995
Pages
978 - 986
Database
ISI
SICI code
0022-3565(1995)275:2<978:COAAAO>2.0.ZU;2-Z
Abstract
The axonal membranes from dog mesenteric nerves were isolated and char acterized. They had a high density of [H-3]saxitoxin, [H-3]rauwolscine and [I-125]iodocyanopindolol binding sites, but low densities of [I-1 25]omega-conotoxin (GVIA) and [H-3]prazosin binding sites. The microso mal membranes had one of the higher densities of [H-3]rauwolscine bind ing sites in centrifugation fractions. These sites were characterized by saturation, kinetic and competition studies. in competition with ox ymetazoline, WE 4101, prazosin, ARC-239, SK&F 104078 and SK&F 104856, these rauwolscine binding sites were alpha(2A)-like. Chloroethylclonid ine pretreatment did not affect the ability of SK&F 104078 or SK&F 104 856 to compete with rauwolscine binding sites on axonal membranes. B-m ax values were unchanged by chloroethylclonidine under conditions that also failed to reduce B-max values of rauwolscine binding to membrane s from human platelets. These receptors appear to be alpha(2A) adrenoc eptors and may represent sites of prejunctional control of neurotransm itter release in the dog. This membrane preparation may be useful in b iochemical studies of prejunctional neural receptors.