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Titolo:
Pharmacological similarities between native brain and heterologously expressed alpha 4 beta 2 nicotinic receptors
Autore:
Shafaee, N; Houng, M; Truong, A; Viseshakul, N; Figl, A; Sandhu, S; Forsayeth, JR; Dwoskin, LP; Crooks, PA; Cohen, BN;
Indirizzi:
Univ Calif Riverside, Div Biomed Sci, Riverside, CA 92521 USA Univ Calif Riverside Riverside CA USA 92521 Sci, Riverside, CA 92521 USA Univ Calif Riverside, Dept Environm Toxicol, Riverside, CA 92521 USA Univ Calif Riverside Riverside CA USA 92521 icol, Riverside, CA 92521 USA Elan Pharmaceut, Menlo Park, CA 94025 USA Elan Pharmaceut Menlo Park CA USA 94025 rmaceut, Menlo Park, CA 94025 USA Univ Kentucky, Coll Pharm, Lexington, KY 40536 USA Univ Kentucky Lexington KY USA 40536 Coll Pharm, Lexington, KY 40536 USA
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 6, volume: 128, anno: 1999,
pagine: 1291 - 1299
SICI:
0007-1188(199911)128:6<1291:PSBNBA>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACETYLCHOLINE-RECEPTORS; XENOPUS OOCYTES; ADENOVIRUS VECTORS; VACCINIA VIRUS; RAT-BRAIN; SUBUNIT; CELLS; BINDING; DIVERSITY; SYSTEM;
Keywords:
neuronal nicotinic acetylcholine receptors; alpha 4; beta 2; Xenopus oocytes; dihydro-beta-erythroidine; epibatidine binding; immunoprecipitation; mAb 299 antibody;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
34
Recensione:
Indirizzi per estratti:
Indirizzo: Cohen, BN Univ Calif Riverside, Div Biomed Sci, Riverside, CA 92521 USA Univ Calif Riverside Riverside CA USA 92521 rside, CA 92521 USA
Citazione:
N. Shafaee et al., "Pharmacological similarities between native brain and heterologously expressed alpha 4 beta 2 nicotinic receptors", BR J PHARM, 128(6), 1999, pp. 1291-1299

Abstract

1 We studied the pharmacological properties of native rat brain and heterologously expressed rat alpha 4 beta 2 nicotinic receptors immunoprecipitated onto a fixed substrate with the anti-alpha 4 antibody mAb 299.2 Immunodepletion with the anti-beta 2 antibody mAb 270 showed that 89% ofthe mAb-299 precipitated rat brain receptors contained beta 2.3 The association and dissociation rate constants for 30 pM +/-[H-3]-epibatidine binding to alpha 4 beta 2 receptors expressed in oocytes were 0.02 +/- 0.01 and 0.03 +/- 0.01 min(-1) (+/-standard error, degrees of freedom = 7 - 8) at 20 - 23 degrees C.4 The Hill coefficients for +/-[H-3]-epibatidine binding to the native brain, alpha 4 beta 2 receptors expressed in oocytes, and alpha 4 beta 2 receptors expressed in CV-I cells (using recombinant adenovirus) were 0.69-0.70 suggesting a heterogeneous receptor population. Fits of the +/-[H-3]-epibatidine concentration-binding data to a two-site model gave K-D s of 8-30 and550-1,200 pM. The high-affinity sites comprised 73 - 74% of the native brain and oocyte alpha 4 beta 2 receptor population, 85% of the CV-I alpha 4 beta 2 receptor population.5 The expression of rat alpha 4 beta 2 receptors in CV-I cells using vaccinia viral infection-transfection resulted in a more homogeneous receptor population (Hill coefficient of 1.0 +/- 0.2). Fits of the +/- [H-3]- epibatidine binding data to a single-site model gave a K-D of 40 +/- 3 pM.6 DH beta E (IC50 = 260 - 470 nM) and the novel nicotine analogue NDNI (IC50 = 7 - 10 mu M) inhibited 30 pM+/-[H-3]-epibatidine binding to the nativebrain and heterologously expressed alpha 4 beta 2 receptors equally well.7 The results show that alpha 4 beta 2-containing nicotinic receptors in the rat brain and heterologously expressed rat alpha 4 beta 2 receptors havesimilar affinities for +/-[H-3]-epibatidine, DH beta E, and NDNI.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 20:09:48