Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Characterization of I-125-IABN, a novel azabicyclononane benzamide selective for D2-like dopamine receptors
Autore:
Luedtke, RR; Freeman, RA; Boundy, VA; Martin, MV; Huang, YS; Mach, RH;
Indirizzi:
Univ N Texas, Hlth Sci Ctr, Dept Pharmacol, Ft Worth, TX 76116 USA Univ N Texas Ft Worth TX USA 76116 Dept Pharmacol, Ft Worth, TX 76116 USA Wake Forest Univ, Sch Med, Dept Radiol, Winston Salem, NC 27109 USA Wake Forest Univ Winston Salem NC USA 27109 , Winston Salem, NC 27109 USA Wake Forest Univ, Sch Med, Dept Physiol & Pharmacol, Winston Salem, NC 27109 USA Wake Forest Univ Winston Salem NC USA 27109 , Winston Salem, NC 27109 USA Ergo Sci Corp, Charlestown, MA USA Ergo Sci Corp Charlestown MA USAErgo Sci Corp, Charlestown, MA USA
Titolo Testata:
SYNAPSE
fascicolo: 4, volume: 38, anno: 2000,
pagine: 438 - 449
SICI:
0887-4476(200012)38:4<438:COIANA>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
D2 RECEPTORS; RAT-BRAIN; INVITRO BINDING; D-2; COCAINE; D1; RADIOLIGAND; ACTIVATION; SPIPERONE; ANALOGS;
Keywords:
dopamine receptors; D2 receptors; radioligand binding; benzamides;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
63
Recensione:
Indirizzi per estratti:
Indirizzo: Luedtke, RR Univ N Texas, Hlth Sci Ctr, Dept Pharmacol, 3500 Camp Bowie, Ft Worth, TX 76116 USA Univ N Texas 3500 Camp Bowie Ft Worth TX USA 76116 X 76116 USA
Citazione:
R.R. Luedtke et al., "Characterization of I-125-IABN, a novel azabicyclononane benzamide selective for D2-like dopamine receptors", SYNAPSE, 38(4), 2000, pp. 438-449

Abstract

The properties of an I-125-labeled structural analog of 2,3-dimethoxy-N-[9-(4-fluorobenzyl)-9-azabicyclo [3.3.1]nonan-3 beta -yl] benzamide (MABN), I-125-IABN, are described. I-125-IABN was developed as a high-affinity radioligand selective for the D2-like (D2, D3, and D4) dopamine receptor subtypes. I-125-IABN binds with picomolar affinity and nonselectively to rat D2 and D3 dopamine receptors expressed in Sig and HEK 293 cells. I-125-IABN binds with 7- to 25-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Rd) calculated from kinetic experiments were in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of I-125-IABN With rat caudate membrane preparations were monophasic and exhibited low nonspecific binding. The pharmacologic profile of the binding of I-125-IABN to rat caudate was consistent with a D2-like receptor, suggesting that the ligand binds primarily to D2 dopamine receptors. In addition, IABN was found to bind with low affinity to D1 dopamine receptors, as well as to the ol and sigma2 receptor subtypes. Quantitative autoradiographic studies using rat brain slices indicate that I-125-IABN selectively labels the striatum and the olfactory tubercle area, which is consistent with the labeling of D2-like receptors. IABN blocks dopamine-dependent inhibition of adenylyl cyclase activity at D2 or D4.4 receptors expressed in HEK cells. Therefore, I-125-IABN appears to be a high-affinity, selective antagonist at D2-like dopamine receptors. Finally, a unique property of the azabicyclononane benzamide I-125-IABN compared to previously studied substituted benzamides is that the binding of this radioligand is not effected by variations in Na+ concentration. (C) 2000 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/01/20 alle ore 06:52:15