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Titolo:
CHARACTERIZATION OF THE MELANOCORTIN-4 RECEPTOR BY RADIOLIGAND BINDING
Autore:
SCHIOTH HB; MUCENIECE R; WIKBERG JES;
Indirizzi:
UPPSALA UNIV,DEPT PHARMACEUT PHARMACOL,CTR BIOMED,BOX 591 S-75124 UPPSALA SWEDEN LATVIAN ACAD SCI,INST ORGAN SYNTH,PHARMACOL LAB LV-226006 RIGA LATVIA
Titolo Testata:
Pharmacology & toxicology
fascicolo: 3, volume: 79, anno: 1996,
pagine: 161 - 165
SICI:
0901-9928(1996)79:3<161:COTMRB>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
MELANOCYTE-STIMULATING HORMONE; MOLECULAR-CLONING; GAMMA-MSH; RAT-BRAIN; EXPRESSION; MELANOTROPIN; PEPTIDES; GENE; LOCALIZATION; FAMILY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
H.B. Schioth et al., "CHARACTERIZATION OF THE MELANOCORTIN-4 RECEPTOR BY RADIOLIGAND BINDING", Pharmacology & toxicology, 79(3), 1996, pp. 161-165

Abstract

The DNA encoding the human melanocortin 4 receptor was expressed in COS (CV-1 origin, SV 40) cells and its radioligand binding properties was tested by using the [I-125][Nle(4), D-Phe(7)]alpha-melanocyte stimulating hormone (MSH). The radioligand was found to bind to a single saturable site with a K-d of 3.84+/-0.57 nmol/l in the MC4 receptor expressing cells. The order of potency of a number of substance competing for the [I-125][Nle(4), D-Phe(7)]alpha-MSH binding was the following; [Nle(4), ha-MSH>beta-MSH>desacetyl-alpha-MSH>alpha-MSH>ACTH (1-39)>ACTH (4-10)>gamma 1-MSH>gamma 2-MSH. This order of potency is unique for the melanocortin 4 receptor when compared to our pre viously publisheddata for the other melanocortin receptor subtypes. Most notably the melanocortin 4 receptor shows highest affinity for beta-MSH, among the endogenous MSH-peptides. Furthermore the melanocortin 4 receptor showsvery low affinity for the gamma-MSH peptides. This distinguishes the melanocortin 4 receptor from the melanocortin 3 receptor, which is theother major central nervous system melanocortin-receptor, as melanocortin 3 receptor shows high affinity for gamma-MSH. Our finding might indicate a specific role for beta-MSH for the melanocortin 4 receptor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 14/07/20 alle ore 10:19:12