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Tytuł oryginału:
Mechanism of the contractile effects of galantide and Galanin (1-14) [ŕ-aminobutyric acid8]scyliorhinin-I in rat isolated fundus strips.
Autorzy:
Korolkiewicz
Roman P.,
Konstański
Zdzisław,
Rekowski
Piotr,
Szyk
Agnieszka,
Ruczyński
Jarosław,
Dąbkowski
Jarosław,
Ujda
Marek,
Korolkiewicz
Konstanty Zbigniew,
Petrusewicz
Jacek
Źródło:
Med. Sci. Monitor 2002: 8 (1) s.BR19-BR23, il., tab., bibliogr. 25 poz.
Sygnatura GBL:
313,278
Hasła klasyfikacyjne GBL:
farmacja
Typ dokumentu:
praca doświadczalna
tytuł obcojęzyczny
Wskaźnik treści:
zwierzęta
szczury
Streszczenie angielskie:
Background: The study was undertaken to establish the pharmacological basis of the stimulatory activity of galantide (M15) and galanin(1-14)-ŕ-aminobutyric acid8-[Abu8])scyliorhinin-I [Scy-I] in gastric smooth muscle. Material/Methods: Isotnic contractions of the isolated, longitudinal rat gastric fundus strips were recorded. Results: Galanin, galanin(1-15)-NH2, M15 and galanin(1-14)-[Abu8]Scy-I elicited concentration-dependent contractions. Their EC50s equaled 12.95, 174, 70.06 and 187 nM respectively. Hill's coefficients for galanin and galanin(1-15)-NH2 were not different from unity, indicating an interaction of one peptide molecule with one receptor accoridng to the principles of classical receptor theory. Hill's coefficients were 0.73 and 1.56 for M15 and galanin (1-14)-[Abu8]Scy-I, respectively, a value significantly different from unity. Cold-storage denervation, tetrodotoxin-TTX (1 ćM), spantide 100 ćM) and NK1-3 receptor antagonists SR140333, 48968, 142801 (up to 10 ćM) notably diminished Mf15, galanin (1-14)-[Abu8]Scy-I, SP(5-11) and [Abu8]-Scy-I evoked contractions without affecting activities of galanin and galanin(1-15)-NH2. Additionally, cross-desensitization experiments attenuated activity of M15 and galanin(1-14)-[Abu8]Scy-I without any noticeable action on galanin or galanin(1-15)-NH2. Conclusions: The action of chimeric peptides on the smooth muscle of the rat gastrointestinal tract depended not only on the myogenic interaction of those peptides with galanin binding sites, but also on the activation of tachykinin receptors or the release of endogenous mediators from the presynaptic terminals.
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