中文名 | Otenzepad |
英文名 | 6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 11-((2-((diethylamino)methyl)-1-piperidinyl)acetyl)-5,11-dihydro- |
英文别名 | Otenzepad 6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 11-((2-((diethylamino)methyl)-1-piperidinyl)acetyl)-5,11-dihydro- |
CAS | 102394-31-0 |
化学式 | C24H31N5O2 |
分子量 | 421.54 |
溶解度 | DMSO : 10 mg/mL母液保存:分装冻存,避免反复冻融;-20℃,1个月;-80℃,6个月(稀释后溶液温度低保存可能会析出,尽量现用现配) |
存储条件 | -20℃ |
产品用途 | Otenzepad, also known as AF-DX 116, is a selective M2 antagonist. Oral AF-DX 116 resulted in greater elevation of DBP than SBP in unstressed rats. In stressed rats, greater and more prolonged elevation of SBP than in unstressed rats was noted, particularly at higher doses. he effects of AF-DX 116 on blood pressure and heart rate thus may arise from peripheral action and AF-DX 116 may be useful for treating hypotension related to autonomic imbalance of the vagotonia type. |
靶点 | M2 muscarinic acetylcholine receptor in rabbit peripheral lung M2 muscarinic acetylcholine receptor in rat heart |
参考资料 展开查看 | 1: Sahin L, Cevik OS, Koyuncu DD, Buyukafsar K. Role of rho-kinase (ROCK) in tonic but not phasic contraction in the frog stomach smooth muscle. Life Sci. 2018 Apr 1;198:46-55. doi: 10.1016/j.lfs.2018.02.023. Epub 2018 Feb 15. PubMed PMID: 29455004. 2: Leaderbrand K, Chen HJ, Corcoran KA, Guedea AL, Jovasevic V, Wess J, Radulovic J. Muscarinic acetylcholine receptors act in synergy to facilitate learning and memory. Learn Mem. 2016 Oct 17;23(11):631-638. doi: 10.1101/lm.043133.116. Print 2016 Nov. PubMed PMID: 27918283; PubMed Central PMCID: PMC5066603. 3: Zhu Y, Chen SR, Pan HL. Muscarinic receptor subtypes differentially control synaptic input and excitability of cerebellum-projecting medial vestibular nucleus neurons. J Neurochem. 2016 Apr;137(2):226-39. doi: 10.1111/jnc.13554. Epub 2016 Feb 15. PubMed PMID: 26823384; PubMed Central PMCID: PMC4828279. 4: Anderson RW, Strowbridge BW. Regulation of persistent activity in hippocampal mossy cells by inhibitory synaptic potentials. Learn Mem. 2014 Apr 15;21(5):263-71. doi: 10.1101/lm.033829.113. PubMed PMID: 24737918; PubMed Central PMCID: PMC3994498. 5: Barathi VA, Kwan JL, Tan QS, Weon SR, Seet LF, Goh LK, Vithana EN, Beuerman RW. Muscarinic cholinergic receptor (M2) plays a crucial role in the development of myopia in mice. Dis Model Mech. 2013 Sep;6(5):1146-58. doi: 10.1242/dmm.010967. Epub 2013 May 2. PubMed PMID: 23649821; PubMed Central PMCID: PMC3759334. 6: Arrighi N, Bodei S, Zani D, Michel MC, Simeone C, Cosciani Cunico S, Spa |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.372 ml | 11.861 ml | 23.723 ml |
5 mM | 0.474 ml | 2.372 ml | 4.745 ml |
10 mM | 0.237 ml | 1.186 ml | 2.372 ml |
5 mM | 0.047 ml | 0.237 ml | 0.474 ml |
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