Galanin (1-13)-Substance P (5-11) amide;GALANTIDE| Galantide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Galantide 是一种特殊的甘丙肽受体 (galanin receptor) 拮抗剂，是一种由甘丙肽和 P 物质片段组成的肽段，在大鼠下丘脑可识别两类甘丙肽结合位点 (KD 分别小于 0.1 nM 和 ~6 nM)。Galantide 剂量依赖性 (IC50=1.0 nM) 拮抗甘丙肽介导的葡萄糖诱导的小鼠胰岛胰岛素分泌抑制。Galantide 似乎与单一的 SP 受体群结合 (KD~40 nM)。

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).

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.

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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138579-66-5

2199.53

C104H151N25O26S

>98% (HPLC)

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(-20℃)

With Ice Pack

≥ 2 years