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 (K D <0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC 50 =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 (K D ~40 nM).
性状
Solid
体外研究(In Vitro)
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%. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
[1]. Langel U, et al. Design of chimeric peptide ligands to galanin receptors and substance P receptors. Int J Pept Protein Res. 1992;39(6):516-522.[2]. Lindskog S, et al. The novel high-affinity antagonist, galantide, blocks the galanin-mediated inhibition of glucose-induced insulin secretion. Eur J Pharmacol. 1992;210(2):183-188.