CAS: 131543-23-2; (+)-Win 55212-2 Mesylate

该化合物是一家制药厂,主要以其作用为名,治疗勃起性机能障碍和肺动高血压;是一种硅酸盐,是一种五型磷酸酯(PDE5)选择性抑制剂;这种抑制导致循环guanosine 单磷酸酯(cGMP)水平的提高,导致血管传播和血液流改善; 盐可提高硅酸盐的溶性和生物利用率,使其更有效地用于治疗; 硅酸盐的特点是白色至非白晶状粉状,在水和有机溶剂中是溶液; 化合物经常通过口服,以相对快速的动作闻名而闻名; 其致癌性包括吸收,分配,主要在肝脏中的代谢和通过尿液排泄. 与任何药物一样,在开药或使用硅酸甲酸盐时,必须考虑潜在的副作用,反作用和与其他药物的相互作用.

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    专利信息


    专利号:US-2007287734-A1
    优先权日:2006-06-09
    标 题 :Preparation and utility of substituted pyrazole compounds with cannabinoid receptor activity
    发明人:GANT THOMAS G; SARSHAR SEPEHR
    权利人:AUSPEX PHARMACEUTICALS INC
    摘要:The present disclosure is directed to modulators of CB-1 type receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of the severity and duration of obesity, metabolic syndrome, dyslipidemia, glucose imbalance, the inability to maintain weight loss, insulin resistance, a cardiovascular disorder, memory loss, drug dependence, a depressive disorder, a panic disorder, an obsessive-compulsive disorder, anxiety, post-traumatic stress syndrome, and any other condition in which it is beneficial to inhibit, inversely agonize or modulate a cannabinoid receptor are described.

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    主要参考文献


    1: Rodríguez-Arias M, Roger-Sánchez C, Vilanova I, Revert N, Manzanedo C, Miñarro J, Aguilar MA. Effects of Cannabinoid Exposure during Adolescence on the Conditioned Rewarding Effects of WIN 55212-2 and Cocaine in Mice: Influence of the Novelty-Seeking Trait. Neural Plast. 2016;2016:6481862. doi: 10.1155/2016/6481862. Epub 2015 Dec 31.
    2: Shabani M, Mahnam A, Sheibani V, Janahmadi M. Alterations in the intrinsic burst activity of Purkinje neurons in offspring maternally exposed to the CB1 cannabinoid agonist WIN 55212-2. J Membr Biol. 2014 Jan;247(1):63-72. doi: 10.1007/s00232-013-9612-1. Epub 2013 Nov 12. doi: 10.1016/j.exer.2013.02.009. Epub 2013 Feb 20.
    5: Alonso-Alconada D, Alvarez A, Alvarez FJ, Martínez-Orgado JA, Hilario E. The cannabinoid WIN 55212-2 mitigates apoptosis and mitochondrial dysfunction after hypoxia ischemia. Neurochem Res. 2012 Jan;37(1):161-70. doi: 10.1007/s11064-011-0594-z. Epub 2011 Sep 11. doi: 10.1016/j.neulet.2010.10.067. Epub 2010 Nov 3.

    合成参考文献


    参考文献:10.1007/s002109900078
    摘要:Akinshola BE, Taylor RE, Ogunseitan AB, Onaivi ES. Anandamide inhibition of recombinant AMPA receptor subunits in Xenopus oocytes is increased by forskolin and 8-bromo-cyclic AMP. Naunyn Schmiedebergs Arch Pharmacol. 1999 Sep;360(3):242–8. doi: 10.1007/s002109900078.
    参考文献:10.1007/s00213-008-1190-z
    摘要:Soderstrom K, Tian Q. CB(1) cannabinoid receptor activation dose dependently modulates neuronal activity within caudal but not rostral song control regions of adult zebra finch telencephalon. Psychopharmacology (Berl). 2008 Aug;199(2):265–73.
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