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Titolo:
Structure-activity relationship of endomorphins and their analogs
Autore:
Huo, XF; Wu, N; Ren, WH; Wang, R; Chan, ASC;
Indirizzi:
Hong Kong Polytech Univ, Dept Appl Biol & Chem Technol, Hong Kong, Hong Kong, Peoples R China Hong Kong Polytech Univ Hong Kong Hong Kong Peoples R China ples R China Lanzhou Univ, Sch Life Sci, Dept Biochem & Mol Biol, Lanzhou 730000, Peoples R China Lanzhou Univ Lanzhou Peoples R China 730000 zhou 730000, Peoples R China
Titolo Testata:
CHINESE SCIENCE BULLETIN
fascicolo: 13, volume: 46, anno: 2001,
pagine: 1096 - 1100
SICI:
1001-6538(200107)46:13<1096:SROEAT>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
CONFORMATION; BIOACTIVITY; AGONIST;
Keywords:
endomorphins; structure-activity relationship; action of opioid receptor binding; analgesia; vasodilatation; mechanism of inactivation;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Citazioni:
14
Recensione:
Indirizzi per estratti:
Indirizzo: Wang, R Hong Kong Polytech Univ, Dept Appl Biol & Chem Technol, Hong Kong,Hong Kong, Peoples R China Hong Kong Polytech Univ Hong Kong Hong Kong Peoples R China hina
Citazione:
X.F. Huo et al., "Structure-activity relationship of endomorphins and their analogs", CHIN SCI B, 46(13), 2001, pp. 1096-1100

Abstract

To study the structure-activity relationship of endomorphins (EMs), the action of opioid receptor binding (AORB), analgesic activity and vasodilator effects of EMs and their eight analogs were investigated, which were prepared by rationally replacing the 2/3-amino acid (Aa) of EMs. The results showed: (i) The 2-Aa was comparatively more related to the selectivity of EMs while the 3-Aa to their affinity; (ii) the analgesia and vasodilatation of EMs and their analogs were not completely dictated by their AORB (in vitro),the action of [D-Pro(2)]EM-2 was unusual; (iii) EMs lost their analgesia in the central nervous system and their vasodilatation in the circulatory system with different mechanisms; the former was due to the degradation of some peptidase, and the latter possibly due to the feedback inhibition.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 11:40:53