PACAP (6-38), HUMAN, OVINE, RAT
- CAS号:143748-18-9
- 英文名:PACAP 6-38
- 中文名:PACAP (6-38), HUMAN, OVINE, RAT
- CBNumber:CB9698459
- 分子式:C182H300N56O45S
- 分子量:4024.7426
- MOL File:143748-18-9.mol
- 储存条件 :-15°C
- 形态 :Solid
- 水溶解性 :Soluble to 2 mg/ml in water
PACAP (6-38), HUMAN, OVINE, RAT性质、用途与生产工艺
- 生物活性 PACAP (6-38), human, ovine, rat 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。
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靶点
IC50: 30 nM (PACAP type I receptor), 600 nM (PACAP type II receptor VIP 1 ), 40 nM (PACAP type II receptor VIP 2 )
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体外研究
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.
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体内研究
Intravesical administration of the PAC1 receptor antagonist, PACAP (6-38) (300 nM), significantly (p≤0.01) 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.
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