Mastoparan 7 is a G protein activator and derivative of the mast cell degranulating peptide mastoparan.[1] It decreases the affinity of acetylcholine (ACh) to porcine brain muscarinic ACh receptors (mAChRs) when used at a concentration of 30 µM and induces GDP/GTP exchange by Gi in a concentration-dependent manner. Mastoparan 7 (1 µM) also induces activation of Gαo in, and increases dendritic spine density of, primary rat hippocampal neurons.[2] It induces contractions in isolated perfused rat tail arteries (EC50 = 44.1 nM).[3] Immunization with a vaccine against cocaine in combination with mastoparan 7 as an adjuvant increases hapten-specific serum IgG levels and decreases cocaine-induced locomotion in mice.[4]
References:
[1].Higashijima, T., Burnier, J., and Ross, E.M.Regulation of Gi and Go by mastoparan, related amphiphilic peptides, and hydrophobic amines. Mechanism and structural determinants of activityJ. Biol. Chem.265(24)14176-14186(1990).
[2].Ramírez, V.T., Ramos-Fernández, E., and Inestrosa, N.C.The Gαo activator mastoparan-7 promotes dendritic spine formation in hippocampal neuronsNeural Plast.4258171(2016).
[3].Grześk, G., Malinowski, B., Grześk, E., et al.Direct regulation of vascular smooth muscle contraction by mastoparan-7Biomed. Rep.2(1)34-38(2014).
[4].St. John, A.L., Choi, H.W., Walker, Q.D., et al.Novel mucosal adjuvant, mastoparan-7, improves cocaine vaccine efficacyNPJ Vaccines5(1)12(2020).