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Titolo:
Characteristics of norepinephrine and clonidine displacement of [H-3]yohimbine binding to platelet alpha(2)-adrenoreceptors in healthy volunteers
Autore:
Gurguis, GNM; Vo, SP; Blakeley, J; Orsulak, PJ; Rush, AJ;
Indirizzi:
Dept Vet Affairs Med Ctr, Dallas, TX 75216 USA Dept Vet Affairs Med Ctr Dallas TX USA 75216 ed Ctr, Dallas, TX 75216 USA Univ Texas, SW Med Sch, Dept Psychiat, Dallas, TX 75235 USA Univ Texas Dallas TX USA 75235 d Sch, Dept Psychiat, Dallas, TX 75235 USA
Titolo Testata:
PSYCHIATRY RESEARCH
fascicolo: 3, volume: 85, anno: 1999,
pagine: 305 - 314
SICI:
0165-1781(19990322)85:3<305:CONACD>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-ADRENERGIC-RECEPTOR; MAJOR DEPRESSIVE DISORDER; TERNARY COMPLEX MODEL; PARA-AMINOCLONIDINE BINDING; ADENYLATE-CYCLASE SYSTEM; H-3 YOHIMBINE BINDING; LOW-AFFINITY STATES; ALPHA-2-ADRENERGIC RECEPTORS; AGONIST BINDING; THERMODYNAMIC PROPERTIES;
Keywords:
platelets; adrenergic receptors; G protein; coupling; anxiety; depression;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Social & Behavioral Sciences
Life Sciences
Citazioni:
56
Recensione:
Indirizzi per estratti:
Indirizzo: Gurguis, GNM Dallas75216ed Ctr, Lab Clin Neurosci, 116A,4500 S Lancaster Rd, Dallas, TX Dallas VA Med Ctr 116A,4500 S Lancaster Rd Dallas TX USA 75216
Citazione:
G.N.M. Gurguis et al., "Characteristics of norepinephrine and clonidine displacement of [H-3]yohimbine binding to platelet alpha(2)-adrenoreceptors in healthy volunteers", PSYCHIAT R, 85(3), 1999, pp. 305-314

Abstract

Clonidine's estimates of platelet alpha(2)-adrenoreceptor (alpha(2)AR) density are substantially lower than yohimbine's. This discrepancy could have contributed to inconsistent results from studies on the role of alpha(2)AR in depression. Furthermore, few studies have investigated the relative distribution of alpha(2)AR between the high- and low-affinity states or their G(i) protein coupling. [H-3](y)ohimbine saturable binding to platelet alpha(2)AR, its displacement by norepinephrine and clonidine, and the effects of Gpp(NH)p on agonist displacement curves were investigated in 11 healthy volunteers. Clonidine estimates of alpha(2)AR density were close to norepinephrine estimates, and both were strongly correlated. Clonidine's K-L/K-H ratio was lower than norepinephrine's, consistent with its partial agonist nature. Norepinephrine and clonidine displacement curves revealed two affinity states. Gpp(NH)p induced a significant rightward shift to a single low-affinity state. When used in combination with a specific antagonist, clonidine's estimates of alpha(2)AR density were similar to those of norepinephrine's, and both were higher than previously reported, when clonidine was used alone. Re-evaluation of previous studies on alpha(2)AR in depression using clonidine is needed. The combined use of antagonist-saturation and agonist-displacement experiments to examine possible dysregulation in alpha(2)AR coupling to G(i) protein in psychiatric disorders is recommended. (C) 1999 Elsevier Science Ireland Ltd. All rights reserved.

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Documento generato il 04/04/20 alle ore 23:09:54