BIBP3226

BIBP3226 is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y1 (Ki = 1.1 nM). It is selective for Y1 over Y2, Y4, and Y5 receptors (Kis = >1,000 nM for all). It also binds to neuropeptide FF receptor 1 (NPFF1) and NPFF2 (Kis = 108 and 79 nM, respectively) and reverses NPFF-induced inhibition of forskolin-induced cAMP accumulation in CHO cells expressing human NPFF2 in a concentration-dependent manner. BIBP3226 inhibits NPY-induced increases in perfusion pressure in isolated rat kidney but not the NPY-induced twitch response in isolated rat vas deferens (IC50s = 26 and >10,000 nM, respectively). BIBP3226 inhibits NPY-induced increases in blood pressure in pithed rats (ED50 = 0.11 mg/kg). It also inhibits NPFF-induced hypothermia in mice when administered intracerebroventricularly (i.c.v.) at a dose of 5 nmol.Formal Name: N-[(1R)-4-[(aminoiminomethyl)amino]-1-[[[(4-hydroxyphenyl)methyl]amino]carbonyl]butyl]-alpha-phenyl-benzeneacetamide. CAS Number: 159013-54-4. Molecular Formula: C27H31N5O3. Formula Weight: 473.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble, Ethanol: soluble. SMILES: OC(C=C1)=CC=C1CNC([C@@H](CCCNC(N)=N)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=O. InChi Code: InChI=1S/C27H31N5O3/c28-27(29)30-17-7-12-23(25(34)31-18-19-13-15-22(33)16-14-19)32-26(35)24(20-8-3-1-4-9-20)21-10-5-2-6-11-21/h1-6,8-11,13-16,23-24,33H,7,12,17-18H2,(H,31,34)(H,32,35)(H4,28,29,30)/t23-/m1/s1. InChi Key: KUWBXRGRMQZCSS-HSZRJFAPSA-N.