PACAP (6-38), human, ovine, rat TFA 是一种有效的 PACAP 受体拮抗剂。PACAP (6-38) 作用于 PACAP I 型受体，PACAP II 型受体 VIP1 和 PACAP II 型受体 VIP2，IC50 分别为 30 nM，600 nM 和 40 nM。
货号:ajcx14058
CAS:N/A
分子式:C184H301N56FO47S
分子量：4138.76
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PACAP (6-38), human, ovine, rat TFA is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively. IC50: 30 nM (PACAP type I receptor), 600 nM (PACAP type II receptor VIP1), 40 nM (PACAP type II receptor VIP2)[1]

An increase of dopamine (DA) content by HPLC analysis and/or cell proliferation identified by MTT assay by Dexamethasone (DEX) is also observed which can be inhibited by PACAP (6-38) at concentration sufficient to block PACAP type 1 (PAC1) receptor. Pretreatment with PAC1 receptor antagonist PACAP (6-38) at 0.1 or 1 μM for 2 h significantly blocks this increase of DA content by 1 μM DEX. The MTT assay shows that DEX increases cell proliferation. Moreover, this action is also inhibited by the pre-incubation of PACAP (6-38). PACAP (6-38) at 1μM shows no effect on DA content and cell proliferation for 24 h. However, PACAP (6-38) at 0.3 μM has been mentioned to reduce the spontaneous tyrosine hydroxylase (TH) accumulation in differentiated retinal cultured cells for 5 days[2].

Intravesical administration of the PAC1 receptor antagonist, PACAP (6-38), significantly increases intercontraction interval (2.0-fold) and void volume (2.5-fold) in NGF-OE mice. Intravesical instillation of PACAP (6-38) also decreases baseline bladder pressure in NGF-OE mice. Intravesical administration of PACAP (6-38) (300 nM) significantly (p≤0.01) reduces pelvic sensitivity in NGF-OE mice but is without effect in WT mice[3].

[1]. Gourlet P, et al. Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors. Eur J Pharmacol. 1995 Dec 4;287(1):7-11. [2]. Yang TT, et al. Changes of dopamine content and cell proliferation by dexamethsone via pituitary adenylate cyclase-activating polypeptide in PC12 cell. Neurosci Lett. 2007 Oct 9;426(1):45-8. [3]. Girard BM, et al. Intravesical PAC1 Receptor Antagonist, PACAP(6-38), Reduces Urinary Bladder Frequency and Pelvic Sensitivity in NGF-OE Mice. J Mol Neurosci. 2016 Jun;59(2):290-9.