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BIBP 3226 trifluoroacetate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BIBP 3226 trifluoroacetate图片
CAS NO:1068148-47-9
包装与价格：
包装价格(元)
1mg电议
10mg电议

产品介绍
BIBP 3226 trifluoroacetate 是一种有效的选择性神经肽 Y Y1 (NPY Y1) 和神经肽 FF (NPFF) 受体拮抗剂，对 rNPY Y1、hNPFF2 和 rNPFF 的 Kis 分别为 1.1、79 和 108 nM。
Cas No.1068148-47-9
化学名(R)-2-(2,2-diphenylacetamido)-5-guanidino-N-(4-hydroxybenzyl)pentanamide bis(2,2,2-trifluoroacetate)
Canonical SMILESFC(F)(C(O)=O)F.OC1=CC=C(C=C1)CNC([C@@H](CCCNC(N)=N)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=O.FC(F)(C(O)=O)F
分子式C27H31N5O3.2CF3CO2H
分子量701.61
溶解度<7.02mg/ml in Water;<70.16mg/ml in DMSO
储存条件Store at -20°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.