M871

M871 (Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide) is an orally active and selective galanin receptor type 2 (GalR2) antagonist. M871 exhibits K_i values of 13.1 nM, 420 nM and >10 μM for GalR2, GalR1 and GalR3 respectively. M871 relieves the mice allergic rhinitis by reducing IgE production, as well as the number of B cells in tissues. M871 can inhibit the nerve invasion of salivary adenoid cystic carcinoma (SACC) and alleviate myocardial ischemia-reperfusion injury. M871 can be used for research on GalR2-related diseases (such as epilepsy, pain)^{[1][2][3][4][5][6][7]}. IC50 & Target:GalR2^[1]. In Vitro:M871 (10^-8 M, 60 min) exhibits antagonist actions at galanin receptor type 2, blocking increased release of inositol phosphate produced by galanin in CHO cells^[1].
M871 decreases SACC-83 cell invasion and migration to the dorsal root ganglia (DRG), as well as the growth and extension of neurites^[5].
In Vivo:M871 (0.1 mg/kg, intranasal administration, once daily for 6 days) improves allergic rhinitis (AR) nasal symptoms, especially sneezing, in mice^[3].
M871 (3-12 mg/kg, i.v., single dose) protects the rat heart from ischemia/reperfusion (I/R) damage by a GalR2-dependent pathway^[4].
M871 (p.o., once every third day for 4 weeks) significantly reduces tumor growth induced by SACC cells and the incidence of perineural invasion (PNI) in BALB/c mice^[5].
M871 (4.575 mg/mL, bilateral intra-NAc injection, single dose) attenuates the Galanin (HY-P74132)-induced analgesic effect of inflammatory pain rats by activating CaMKII and PKC in nucleus accumbens (NAc) of inflammatory pain rats^[6].
M871 (100 nM/kg, intracerebroventricular injection, once daily for 21 days) exacerbates hyperglycemia and aggravates the inflammatory response in type 2 diabetic rats^[7].