BIBP 3226 trifluoroacetate

BIBP 3226 trifluoroacetate is a non-peptide neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist with Ki values of 1.1, 79, 108 for rNPY Y1, hNPFF2, rNPFF, respectively.

Neuropeptide Y Y1 receptors (NPY Y1) involve in the regulation of exploratory behaviour and anxiety. Neuropeptide FF (NPFF) is a part of a neurotransmitter system functioning as a modulator of endogenous opioid functions [1].

BIBP 3226 was able to compete for the specific NPFF binding expressed in CHO cells as well as in rat dorsal spinal cord. In hNPFF2 receptors transfected cells, BIBP 3226 (10mM) is able to antagonize the inhibition of forskolin-stimulated cyclic AMP production induced by NPFF (10nM) in a concentration-dependent manner [2].

In male Wistar rats, BIBP3226 at the dose of 5 mg caused an anxiogenic-like effect while the lower dose was ineffective. While, the overall locomotory activity didn’t change in all treatment groups [1]. In mice model, BIBP3226 (5nmol) injected into the third ventricle completely antagonized the hypothermic effects of NPFF (30nmol) and NPVF (30nmol). In the mouse tail-flick assay, BIBP3226 (5nmol) prevented the anti-morphine actions of NPFF (10nmol). Also, in urethane-anaesthetized rats, BIBP3226 (500nmol/kg) significantly reduced the mean arterial blood pressure induced by NPFF (200nmol/kg) and NPVF (200nmol/kg) [3].

References:
[1].  Kask A1, R?go L, Harro J. Anxiogenic-like effect of the neuropeptide Y Y1 receptor antagonist BIBP3226: antagonism with diazepam. Eur J Pharmacol, 1996, 317(2-3): R3-4.
[2].  Mollereau C1, Gouardères C, Dumont Y, et al. Agonist and antagonist activities on human NPFF2 receptors of the NPY ligands GR231118 and BIBP3226. Br J Pharmacol, 2001, 133(1): 1-4.
[3].  Fang Q1, Guo J, He F, et al. In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist. Peptides, 2006, 27(9): 2207-2213.