BIBO 3304 trifluoroacetate

BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively)[1].

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> Neuropeptide Y Receptor

BIBO3304 TFA (30 μg; bilateral paraventricular nucleus injection) attenuates the hyperphagia following fasting[1]. BIBO3304 TFA (15-60 μg) dose-dependently inhibits the feeding reponse mediated by 1 μg NPY[1]. BIBO3304 TFA (0.5 μM; p.o.) significantly increases serum insulin levels[2]. Animal Model: Adult male Chbb:Thom rats weighing between 300 and 340 g[1] Dosage: 30 μg Administration: bilateral paraventricular nucleus injection Result: Attenuated the hyperphagia following fasting, especially during the first 2 h of refeeding. Animal Model: 7-week-old C57BL/6JAusb mice[2] Dosage: 0.5 μM Administration: p.o. Result: Significantly increased serum insulin levels.

[1]. Wieland HA, et al. Subtype selectivity of the novel nonpeptide neuropeptide Y Y1 receptor antagonist BIBO 3304 and its effect on feeding in rodents. Br J Pharmacol. 1998 Oct;125(3):549-55.

[2]. Loh K, et al. Inhibition of Y1 receptor signaling improves islet transplant outcome. Nat Commun. 2017 Sep 8;8(1):490.