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ICI-63197

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Chemical Structure| 27277-00-5 同义名 : -
CAS号 : 27277-00-5
货号 : A122751
分子式 : C9H13N5O
纯度 : 95%
分子量 : 207.232
MDL号 : MFCD06407961
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Cyclic nucleotide phosphodiesterase (PDE), that is a multigenic enzyme superfamily ubiquitously distributed in mammalians, mainly contributes to intracellular signaling regulation. Its various isozymes specifically control in a spatio-temporal manner intracellular levels of cAMP and cGMP downstream receptor activation and nearby functional proteins[1].The compound ICI 63197, a selective inhibitor of the peripheral plasma membrane phosphodiesterase(PDE).[2]. ICI 63,197 and levodopa produced isoprenaline-like effects on contractions but times to peak effect and recovery were longer. Cyclic AMP levels estimated during the depressant action were elevated[3].ICI 63 197 (10 umol/l, 10 rnin incubation) increased cyclic AMP level by 29-39% in 3 preparations but decreased the level by 6% in one other preparation. Mean levels increased significantly (P<0.05, n =4). There was no consistent change in cyclic GMP level which decreased up to 47% or increased up to 15%. A higher dose of ICI 63 197 (50 umol/l,10 rnin incubation) increased cyclic AMP levels by 17-281%. The mean increase was statistically significant (P<0.01, n=4). As with the lower dose of ICI 63 197, there was no consistent change in cyclic GMP level which decreased up to 29% or increased up to 46%[4].While pretreatment with a single dose of rolipram, ICI 63,197 or IBMX administered either 1 or 24 h prior to clonidine (0.1 mg/kg) enhanced clonidine-induced hypothermia and hypoactivity, chronic dosing (twice daily for 14 days) with desipramine (10 mg/kg) or rolipram (5 mg/kg) antagonized these behavioural effects. In contrast, chronic dosing with IBMX or ICI 63,197 failed to antagonize clonidine-induced hypothermia and hypoactivity[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.83mL

0.97mL

0.48mL

24.13mL

4.83mL

2.41mL

48.26mL

9.65mL

4.83mL
参考文献

[1]Thérèse Keravis,et al. Cyclic nucleotide phosphodiesterases (PDE) and peptide motifs. Curr Pharm Des. 2010;16(9):1114-25.

[2]Davies, D. R. The structure and function of the aspartic proteinases. Annu. Rev. Biophys. Biophys. Chem. 19, 189–215.

[3] Z Merican, M W Nott. Effects of isoprenaline, levodopa and a phosphodiesterase inhibitor (ICI 63,197) on cyclic AMP levels and contractions of soleus muscles in anesthetized cats. Clin Exp Pharmacol Physiol. 1981 Jan;8(1):57-66.

[4]Z Merican, M W Nott. Effects of alpha- and beta-adrenoceptor agonists and a phosphodiesterase inhibitor (ICI 63 197) on cyclic AMP and GMP levels in bovine splenic nerve. Clin Exp Pharmacol Physiol. Jan-Feb 1983;10(1):35-44.

[5]M R Mustafa,et al. Effect of long-term rolipram administration on the sensitivity of alpha 2-adrenoceptors in rat brain. Eur J Pharmacol. 1988 Mar 29;148(2):171-7.