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Titolo:
Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119
Autore:
Schioth, HB; Muceniece, R; Mutulis, F; Bouifrouri, AA; Mutule, I; Wikberg, JES;
Indirizzi:
Uppsala Univ, Dept Pharmaceut Pharmacol, Uppsala, Sweden Uppsala Univ Uppsala Sweden Dept Pharmaceut Pharmacol, Uppsala, Sweden Inst Organ Synth, Pharmacol Lab, LV-1006 Riga, Latvia Inst Organ Synth Riga Latvia LV-1006 Pharmacol Lab, LV-1006 Riga, Latvia Inst Organ Synth, Dept Med Chem, LV-1006 Riga, Latvia Inst Organ Synth Riga Latvia LV-1006 Dept Med Chem, LV-1006 Riga, Latvia
Titolo Testata:
NEUROPEPTIDES
fascicolo: 3, volume: 33, anno: 1999,
pagine: 191 - 196
SICI:
0143-4179(199906)33:3<191:FPCOTS>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
MELANOCYTE-STIMULATING HORMONE; MOLECULAR-CLONING; RADIOLIGAND BINDING; MSH ANALOGS; ALPHA-MSH; SUBTYPES; EXPRESSION; OBESITY; MICE; RATS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Schioth, HB Ctr Biomed, Dept Pharmaceut Pharmacol, Box 591, S-75124 Uppsala, Sweden Ctr Biomed Box 591 Uppsala Sweden S-75124 124 Uppsala, Sweden
Citazione:
H.B. Schioth et al., "Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119", NEUROPEPTID, 33(3), 1999, pp. 191-196

Abstract

SHU9119 and HS014 are cyclic MSH analogues which are widely used to elucidate the physiology behind the various effects of the MSH peptides and theirreceptors. We carefully compared the potency of SHU9119 and HS014 in cellsexpressing the MC receptor clones. We found that both the peptides are partial agonists for the MC1 and MC5 receptors while they are potent antagonists for the MC3 and MC4 receptors. In agreement with earlier binding data, we found that SHU9119 has equal potency for the MC3 and MC4 receptor whereasHS014 has at least 10-fold higher potency for the MC4 receptor than the MC3 receptor in cAMP assay. Moreover, we synthesized analogues of HS014 wherethe C-terminal was truncated. We found that this C-terminal fragment of HS014, in particular the Lys(14) has a major influence on the affinity for the MC4 receptor without any particular influence on the affinity for the other MC receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 14/08/20 alle ore 17:00:33