|2-氨基-6-甲基-4-丙基-[1,2,4]三唑并[1,5-a]嘧啶-5(4H)-酮|CsnPharm

CAS No.: 27277-00-5

2-Amino-6-methyl-4-propyl-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-one Catalog No. CSN22853

ICI 63197 is a potent phosphodiesterase (PDE) 4 inhibitor with antidepressant effects.

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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].
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实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.8255 mL
- 24.1275 mL
- 48.2550 mL
- 5 mM
- 0.9651 mL
- 4.8255 mL
- 9.6510 mL
- 10 mM
- 0.4826 mL
- 2.4128 mL
- 4.8255 mL

技术信息

CAS号	27277-00-5	储存条件	粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C9H13N5O	运输	蓝冰
分子量	207.23	别名

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2-Amino-6-methyl-4-propyl-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-one Catalog No. CSN22853

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