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Titolo:
DIFFERENTIAL ANTAGONISM OF AMYLINS METABOLIC AND VASCULAR ACTIONS WITH AMYLIN RECEPTOR ANTAGONISTS
Autore:
BEAUMONT K; MOORE CX; PITTNER RA; PRICKETT KS; GAETA LSL; RINK TJ; YOUNG AA;
Indirizzi:
AMYLIN PHARMACEUT INC,9373 TOWNE CTR DR SAN DIEGO CA 92121
Titolo Testata:
Canadian journal of physiology and pharmacology
fascicolo: 7, volume: 73, anno: 1995,
pagine: 1025 - 1029
SICI:
0008-4212(1995)73:7<1025:DAOAMA>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
SKELETAL-MUSCLE; PANCREATIC AMYLIN; BINDING-SITES; CALCITONIN; PEPTIDE; RAT; INSULIN; INVITRO; GLUCOSE; BRAIN;
Keywords:
AMYLIN; CALCITONIN GENE RELATED PEPTIDE; DIABETES; SKELETAL MUSCLE; PEPTIDE RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
17
Recensione:
Indirizzi per estratti:
Citazione:
K. Beaumont et al., "DIFFERENTIAL ANTAGONISM OF AMYLINS METABOLIC AND VASCULAR ACTIONS WITH AMYLIN RECEPTOR ANTAGONISTS", Canadian journal of physiology and pharmacology, 73(7), 1995, pp. 1025-1029

Abstract

High affinity amylin binding sites are present in the rat nucleus accumbens. These sites bind [I-125]amylin with an affinity of 27 pM and have high affinity for salmon calcitonin (sCT) and moderately high affinity for calcitonin gene related peptide (CORP). N-terminally truncated peptides were tested for their ability to compete for [I-125]amylin binding to these sites and to antagonize the metabolic and vascular actions of amylin. CGRP(8-37), sCT(8-32), and ac-[Asn(30),Tyr(32)]sCT(8-32) (AC187) inhibited [I-125]amylin binding to rat nucleus accumbens. Order of potency at inhibiting amylin binding (AC187 > sCT(8-32) > CGRP(8-37)) differed from the order of potency at inhibiting [I-125]CGRP binding to SK-N-MC neuroblastoma cells (CGRP(8-37) > AC187 > sCT(8-32)). AC187 was the most potent antagonist of amylin's effects on isolated rat soleus muscle glycogen metabolism, and it was more effective than either sCT(8-32) or CGRP(8-37) at reducing amylin-stimulated hyperlactemia in rats. In contrast, CGRP(8-37) was the most potent peptide atantagonizing amylin-induced hypotension in rats. Amylin's hypotensiveactions appear to be mediated by a weak action at CORP receptors, while its metabolic actions are mediated by receptors with a distinct antagonist profile. AC187 is a potent antagonist of amylin binding sites in nucleus accumbens and of amylin's metabolic actions.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 16:33:43