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编 号:F146374
分子式:C104H151N25O26S
分子量:2199.53
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生物活性:
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM).

体内研究:
Intracerebroventricular injection of galanin (5 micrograms/rat) inhibited sexual behavior in experienced male rats--without producing any other locomotor or behavioral deficit-, injection of the galanin antagonist, galantide, by the same route (1 or 2 micrograms/rat) stimulated sexual behavior (improving arousal, motivation and performance indexes) and antagonized the effect of galanin. Galantide ameliorates mild acute pancreatitis (AP). Galantide significantly reduces AP-induced hyperenzymemia by 41–49%. Galantide has been found to improve social memory in 'socialrecognition' test when i.c.v. administered at doses varying from 6-6000 nM.

体外研究:
Galantide do not activate the K+ conductance but produces a concentration-dependent antagonism (IC50=4 nM) of the galanin-induced increase in K+ conductance. Galantide acts like galanin and inhibits the voltage-dependent Ba2+ current (IBa). The inhibition of IBa also is concentration dependent (IC50=16 nM) and the maximum inhibition produced by galantide is approximately 40%.
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