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PL-017  

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号： P11719 产品名称： PL-017 CAS: 83397-56-2   储存条件 粉末 -20℃ 四年     分子式： C29H37N5O5 溶于液体 -80℃ 6个月 分子量： 535.63 -20℃ 1个月 化学名：  (2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[(2R)-2-carbamoylpyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]-N-methylpyrrolidine-2-carboxamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3567mL 11.7836mL 23.5671mL 5mM 0.4713mL 2.3567mL 4.7134mL 10mM 0.2357mL 1.1784mL 2.3567mL   生物活性 产品描述 一种有效的，选择性 μ 阿片受体 (μ opioid receptor) 激动剂，对 125I-FK 33,824 与 μ 位点结合的 IC50 为 5.5nM。PL-017 在大鼠中产生持久的可逆性镇痛作用。 靶点 mAChR   体外研究 The antisecretory properties of pirenzepine on gastric acid and pepsin secretion may be attributed to the antagonistic activity of the drug on muscarinic M1 receptors of gastric intramural plexuses,whereas the effect on parietal muscarinic M2 receptors seems of less importance.Additional inhibitory mechanisms on gastric secretion may be represented by pirenzepine-induced increase in somatostatin release from gastrointestinal system.Significant cytoprotective properties of pirenzepinehave been observed on a variety of experimentally induced peptic ulcerations.Pirenzepine (5-500μg/mL) inhibits agonist-(acetylcholine-,carbachol- or nicotine-) induced contractions of the toad isolated rectus abdominis muscle,and depresses electrically provoked twitches of the rat phrenic nerve-hemidiaphragm muscle preparation. 体内研究 Pirenzepine is potent in impairing learning of an avoidance;much higher doses are required to antagonize other central muscarinic effects.Pirenzepine is found to impair passive avoidance learning when given i.c.v.20 min pre-training.The median latencies in pirenzepine-treated animals are 79.5,11,27 and 25.5 seconds with doses of 0.03,0.1,0.3 and 1μg per mouse respectively.Acid and pepsin secretion stimulated by either bethanechol or the vagus are inhibited in a doseresponsive manner by pirenzepine.Pirenzepine (5-25mg/kg i.v.) depresses indirect electrical stimulation-evoked twitches of the cat tibialis anterior and soleus muscle preparations.   推荐实验方法(仅供参考) 动物实验:   Dogs:In three of the Dogs,gastric secretion also is stimulated by bethanechol infused i.v.at the rate of 80μg (0.4μM)/kg.hr for 3hr.Atropine (1.4,2.8,5.6 and 11.2nM/kg) or pirenzepine (6,12 and 24nM/kg) are injected at 15-mm intervals,beginning 1hr after initiation of bethanechol infusion.Heart rate is measured every 7.5 mm during infusion of the drugs and for 75 mins thereafter.
保存条件：-20℃

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