|AR-M 1896 Catalog No.GC11955|
Sample solution is provided at 25 µL, 10mM.
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|Solubility||Soluble to 1 mg/ml in 20% formic acid||Storage||Desiccate at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
Binding IC50: 1.76 nM for rGalR2; 879 nM for hGalR1
Galanin is a 29-aa neuropeptide with a complex role in pain processing. Galanin receptor subtypes are present in dorsal root ganglia and spinal cord with a differential distribution. Three galanin receptors, GalR1, GalR2 and GalR3, have been identified and cloned. AR-M1896 is a specific galanin R2 (GalR2) agonist.
In vitro: Additional removal of the glycine residue in position 1 resulted in AR-M1896 with almost unchanged GalR2 affinity and functional activity, and 500-fold selectivity for GalR2-Rs over GalR1-Rs. This compound represents a truly GalR2-selective galanin analog and, thus, could be used as a pharmacological tool to differentiate between these two receptors .
In vivo: In normal rats mechanical and cold allodynia of the hindpaw are induced by intrathecal infusion of low-dose galanin. The same effect is seen with equimolar doses of AR-M1896 or AR-M961 (an agonist both at GalR1 and GalR2 receptors). In allodynic Bennett model rats, the mechanical threshold dose-dependently increased after intrathecal injection of a high AR-M961dose, whereas no effect was observed in the control or AR-M1896 group. No effect of either compounds was observed in nonallodynic Bennett model rats .
Clinical trial: Up to now, AR-M1896 is still in the preclinical development stage.
 Liu HX, Brumovsky P, Schmidt R, Brown W, Payza K, Hodzic L, Pou C, Godbout C, Hökfelt T.
Receptor subtype-specific pronociceptive and analgesic actions of galanin in the spinal cord: selective actions via GalR1 and GalR2 receptors. Proc Natl Acad Sci U S A. 2001 Aug 14;98(17):9960-4.