BIBP3226 |
Katalog-Nr.GC48494 |
BIBP3226 ist ein potenter und selektiver Neuropeptid Y Y1 (NPY Y1) und Neuropeptid FF (NPFF) Rezeptorantagonist mit Kis von 1,1, 79 und 108 nM fÜr rNPY Y1, hNPFF2 bzw. rNPFF.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 159013-54-4
Sample solution is provided at 25 µL, 10mM.
BIBP3226 is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y1 (Ki = 1.1 nM).1 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.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
1.Mollereau, C., GouardÈres, C., Dumont, Y., et al.Agonist and antagonist activities on human NPFF2 receptors of the NPY ligands GR231118 and BIBP3226Br. 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: BIBP3226Eur. 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 antagonistPeptides27(9)2207-2213(2006)
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