BIBP3226 (trifluoroacetate salt)

BIBP3226 is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y₁ (K_i = 1.1 nM).¹ It is selective for Y₁ over Y₂, Y₄, and Y₅ receptors (K_is = >1,000 nM for all). It also binds to neuropeptide FF receptor 1 (NPFF1) and NPFF2 (K_is = 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.¹ 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).² BIBP3226 inhibits NPY-induced increases in blood pressure in pithed rats (ED₅₀ = 0.11 mg/kg).² It also inhibits NPFF-induced hypothermia in mice when administered intracerebroventricularly (i.c.v.) at a dose of 5 nmol.³

WARNING This product is not for human or veterinary use.

1. Mollereau, C., Gouardères, C., Dumont, Y., et al. Agonist and antagonist activities on human NPFF2 receptors of the NPY ligands GR231118 and BIBP3226. Br. J. Pharmacol. 133(1), 1-4 (2001).

2. Rudolf, K., Eberlein, W., Engel, W., et al. The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226. Eur. J. Pharmacol. 271(2-3), R11-R13 (1994).

3. Fang, Q., Guo, J., He, F., et al. In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist. Peptides 27(9), 2207-2213 (2006).