BIBP-3226 explained

BIBP-3226 is a drug used in scientific research which acts as a potent and selective antagonist for both the Neuropeptide Y receptor Y₁^[1] and also the neuropeptide FF receptor.^[2] It was the first non-peptide antagonist developed for the Y₁ receptor and has been widely used to help determine its functions in the body. Activation of Y₁ is thought to be involved in functions such as regulation of appetite^[3] and anxiety,^[4] and BIBP-3226 has anxiogenic^[5] and anorectic effects, as well as blocking the Y₁-mediated corticotropin releasing hormone release.^[6] It has also been used as a lead compound to develop a number of newer more potent Y₁ antagonists.^{[7] [8]}

Notes and References

1. Rudolf K, Eberlein W, Engel W, Wieland HA, Willim KD, Entzeroth M, Wienen W, Beck-Sickinger AG, Doods HN . The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226 . European Journal of Pharmacology . 271 . 2–3 . R11–3 . December 1994 . 7705422 . 10.1016/0014-2999(94)90822-2.
2. Fang Q, Guo J, He F, Peng YL, Chang M, Wang R . In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist . Peptides . 27 . 9 . 2207–13 . September 2006 . 16762456 . 10.1016/j.peptides.2006.04.002 . 34414256 .
3. Kask A, Rägo L, Harro J . Evidence for involvement of neuropeptide Y receptors in the regulation of food intake: studies with Y1-selective antagonist BIBP3226 . . 124 . 7 . 1507–15 . August 1998 . 9723965 . 1565528 . 10.1038/sj.bjp.0701969 .
4. Kask A, Harro J, von Hörsten S, Redrobe JP, Dumont Y, Quirion R . The neurocircuitry and receptor subtypes mediating anxiolytic-like effects of neuropeptide Y . Neuroscience and Biobehavioral Reviews . 26 . 3 . 259–83 . May 2002 . 12034130 . 10.1016/S0149-7634(01)00066-5. 34688422 .
5. Kask A, Rägo L, Harro J . Anxiogenic-like effect of the NPY Y1 receptor antagonist BIBP3226 administered into the dorsal periaqueductal gray matter in rats . Regulatory Peptides . 75-76 . 255–62 . September 1998 . 9802417 . 10.1016/S0167-0115(98)00076-7. 19193956 .
6. Dimitrov EL, DeJoseph MR, Brownfield MS, Urban JH . Involvement of neuropeptide Y Y1 receptors in the regulation of neuroendocrine corticotropin-releasing hormone neuronal activity . Endocrinology . 148 . 8 . 3666–73 . August 2007 . 17463058 . 10.1210/en.2006-1730 . free .
7. Aiglstorfer I, Hendrich I, Moser C, Bernhardt G, Dove S, Buschauer A . Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226 . Bioorganic & Medicinal Chemistry Letters . 10 . 14 . 1597–600 . July 2000 . 10915060 . 10.1016/S0960-894X(00)00292-4.
8. Weiss S, Keller M, Bernhardt G, Buschauer A, König B . Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists . Bioorganic & Medicinal Chemistry . 16 . 22 . 9858–66 . November 2008 . 18851917 . 10.1016/j.bmc.2008.09.033 .