(R)-(+)-WIN 55,212-2 甲磺酸盐
中文名称 | (R)-(+)-WIN 55,212-2 甲磺酸盐 |
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中文同义词 | 甲磺酸西地那非(酒溶西地那非);WIN552122 甲磺酸酯;(+)-【2,3-二氢-5-甲基-3-(4-吗啡啉甲基)吡咯[1,2,3-D]-1,4-苯并噁唑琳-6-】-1-萘基甲酮;(+)WIN 55212-2甲磺酸盐;(R)-(+)-WIN 55,212-2 甲磺酸盐;WIN 55212-2 甲磺酸盐;甲磺酸西地那非(Z);水溶性西地那非 |
英文名称 | WIN 55,212-2 MESYLATE |
英文同义词 | R(+)-WIN 55,212-2 ,MESYLATE HIGH AFFINIT Y CANNABI;(R)-(+)-(2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1.2.3-de]-1,4-benzoxazin-6-yl)-1-naphthalenylmethanonemesy;212-2Mesylate;WIN55;(R)-(+)-[2,3-Dihydro-5-methyl-3[(4-morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate salt;(R)-(+)-WIN 55,212-2 mesylate salt;WIN 552122 mesylate, (R)-(+)-[2,3-Dihydro-5-methyl-3[(4-morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate salt;(R)-(5-Methyl-3-(MorpholinoMethyl)-2,3-dihydro-[1,4]oxazino[2,3,4-hi]indol-6-yl)(naphthalen-1-yl)Methanone |
CAS号 | 131543-23-2 |
分子式 | C28H30N2O6S |
分子量 | 522.62 |
EINECS号 | 1592732-453-0 |
相关类别 | 定制化学品;保健原料;其他生化试剂;原料药;医药原料;原料及中间体;保健减肥原料;男性保健;Cannabinoid receptor;Cannabinoid;男性保健原料;原料;保健品 |
Mol文件 | 131543-23-2.mol |
结构式 |
(R)-(+)-WIN 55,212-2 甲磺酸盐 性质
储存条件 | Store at +4°C |
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溶解度 | 0.1 M HCl:0.25 mg/mL |
形态 | 固体 |
颜色 | 白色至类白色 |
稳定性 | DMSO中的溶液可在-20°下稳定储存3个月。 |
InChIKey | FSGCSTPOPBJYSX-OZYVVJTJNA-N |
SMILES | S(O)(=O)(=O)C.C(N1CCOCC1)[C@@H]1COC2=CC=CC3C(C(C4=CC=CC5=CC=CC=C45)=O)=C(C)N1C=32 |&1:12,r| |
Target | Value |
CB2
(Cell-free assay) | 3.3 nM(Ki) |
CB1
(Cell-free assay) | 62.3 nM(Ki) |
WIN 55,212-2 is more potent in CHO-CB2 cells than in CHO-CB1 cells by a factor of 6O. WIN 55,212-2 has no effect on arachidonic acid release in CHO-CB2 or control CHO cells. WIN 55,212-2 fails to stimulate any increase in intracellular Ca 2+ up to 10 μM. In primary cultures of rat cerebral cortex neurons, WIN 55,212-2 (0.01--100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve. The facilitatory effect of WIN 55,212-2 (1 nM) is fully counteracted by SR141716A (10 nM), by the replacement of the normal Krebs Ringer-bicarbonate buffer with a low Ca 2+ medium (0.2 mM) and by the IP(3) receptor antagonist xestospongin C (1 μM). WIN 55,212-2 evokes CGRP release from TG neurons in vitro (EC 50 =26 μM) in a concentration- and calcium-dependent manner. WIN 55,212-2-2 neither inhibits capsaicin-evokes CGRP release nor does it inhibit forskolin-, isoproteranol- or prostaglandin E2-stimulated cAMP accumulation. WIN 55,212-2 significantly inhibits (EC 50 =1.7 μM) 50 mm K + -evoked CGRP release by approximately 70%. WIN 55,212-2 inhibition of 50 mm K + -evoked CGRP release is not reversed by antagonists of cannabinoid type 1 (CB1) receptor, but is mimicks in magnitude and potency (EC 50 =2.7 μM) by its cannabinoid-inactive enantiomer WIN 55,212-2-3.
In the prefrontal cortex WIN 55,212-2 (0.1 and 1 mg/kg i.p.) increases dialysate glutamate levels from of the awake rat, while the lower (0.01 mg/kg) and the higher (2 mg/kg) doses are ineffective. Furthermore, the WIN 55,212-2 (0.1 mg/kg)- induced increase of dialysate glutamate levels is counteracted by pretreatment with the selective CB(1) receptor antagonist SR141716A (0.1 mg/kg, i.p.) and by the local perfusion with a low-calcium Ringer solution (Ca 2+ 0.2 mM). WIN 55,212-2 (0.5, 1, 3, 5, 10 and 15 mg/kg, i.p.) does not alter the seizure threshold at low doses, while higher doses of the drug significantly increases the threshold in a dose-dependent manner. The anticonvulsant effect of WIN 55,212-2, which is observed with doses as high as 5 mg/kg, can be observed with doses as low as 0.5 mg/kg in groups pre-treated with 20 mg/kg of pioglitazone.
安全信息
WGK Germany | 3 |
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提供商 | 语言 |
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/16 | W0019 | WIN 55212-2甲磺酸盐 WIN 55212-2 Mesylate | 131543-23-2 | 50MG | 1290元 |
2023/03/20 | HY-13291 | (R)-(+)-WIN 55,212-2 甲磺酸盐 WIN 55,212-2 Mesylate | 131543-23-2 | 5mg | 810元 |