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Titolo:
LACK OF DISCRIMINATION BY AGONISTS FOR D-2 AND D-3 DOPAMINE-RECEPTORS
Autore:
BURRIS KD; PACHECO MA; FILTZ TM; KUNG MP; KUNG HF; MOLINOFF PB;
Indirizzi:
BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,CNS DRUG DISCOVERY,5 RES PKWY WALLINGFORD CT 06492 UNIV PENN,SCH MED,DEPT PHARMACOL PHILADELPHIA PA 19104 UNIV PENN,SCH MED,DEPT RADIOL PHILADELPHIA PA 19104
Titolo Testata:
Neuropsychopharmacology
fascicolo: 4, volume: 12, anno: 1995,
pagine: 335 - 345
SICI:
0893-133X(1995)12:4<335:LODBAF>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-ADRENERGIC RECEPTORS; ANTERIOR-PITUITARY GLAND; MAMMALIAN-CELL LINE; HIGH-AFFINITY; RAT-BRAIN; D3-DOPAMINE RECEPTOR; GUANINE-NUCLEOTIDE; H-3 QUINPIROLE; INTACT-CELLS; BINDING;
Keywords:
DOPAMINE D-2 RECEPTOR; DOPAMINE D-3 RECEPTOR; DOPAMINE; AGONIST; (+/-)-7-HYDROXY-N,N-DIPROPYL-AMINOTETRALIN (7-OH-DPAT);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Physical, Chemical & Earth Sciences
Physical, Chemical & Earth Sciences
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
57
Recensione:
Indirizzi per estratti:
Citazione:
K.D. Burris et al., "LACK OF DISCRIMINATION BY AGONISTS FOR D-2 AND D-3 DOPAMINE-RECEPTORS", Neuropsychopharmacology, 12(4), 1995, pp. 335-345

Abstract

The affinities of D-3 dopamine receptors for antagonists are similar to those of D-2 receptors D-3 receptors have been reported, however, to have affinities nearly 100-fold higher than those of D-2 receptors for some agonists, including (+/-)-7-hydroxy-n, n-dipropyl-aminotetralin (7-OH-DPAT) and quinpirole. This has led to the use of these agonists to try to identify functional responses mediated by D-3 receptors invivo. However, D-2 receptors exist in multiple states having high andlow affinities for agonists. The G protein-coupled state of D-2 receptors is believed to be the functional stare of these receptors. When receptors were labeled with the D-2 receptor antagonist (S)-3-iodo-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5,6- dimethoxysalicylamide ([I-125]-NCQ-298) under conditions that promote uncoupling of receptors from G proteins, the affinities of D-3 receptors Were approximately 130-fold higher than those of D-2 receptors for 7-OH-DPAT and quinpirole. When receptors were labeled with the D-2 receptor agonist 2-[N-propyl-N-(3'-iodo-2'-propenyl)-amino]tetralin ([I-125]-7-OH-PIPAT) under conditions that favor interactions of receptors with G proteins, the affinities ofD-3 receptors were less than sevenfold higher than the affinities of D-2 receptors for the same drugs. Similarly, small differences in the affinities of D-2 and D-3 receptors for other agonists were seen when receptors were labeled with [I-125]-7-OH- PIPAT. These data demonstrate that putative D-3 receptor-selective agonists also interact with a high-affinity, G protein-coupled state of D-2 receptors. The similarities in affinities of the agonist-preferring state of D-2 and D-3 receptors means that currently available agonists cannot be used to discriminate between behavioral effects mediated by D-2 and D-3 receptors.

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Documento generato il 04/04/20 alle ore 08:37:00