中文名 | WIN 55,212-2甲磺酸盐 |
英文名 | WIN 55,212-2 MESYLATE |
别名 | 水溶性西地那非 甲磺酸西地那非 甲磺酸西地那非(Z) WIN552122 甲磺酸酯 甲磺酸西地那非(酒溶西地那非) WIN 55,212-2甲磺酸盐 WIN 55212-2 甲磺酸盐 (+)WIN 55212-2甲磺酸盐 (R)-(+)-WIN 55,212-2 甲磺酸盐 (+)-【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 |
英文别名 | WIN55 CS-754 WIN552122 WIN-552122 212-2Mesylate Sildenafil Mesylate WIN 55,212-2 MESYLATE R(+)-WIN 55,212-2 MESYLATE 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 R(+)-[2,3-DIHYDRO-5-METHYL-3-[(MORPHOLINYL)METHYL]PYRROLO[1,2,3-DE]-1,4-BENZOXAZINYL]-(1-NAPHTHALENYL)METHANONE MESYLATE (R)-(+)-[2,3-DIHYDRO-5-METHYL-3-(4-MORPHOLINYLMETHYL)PYRROLO[1,2,3-DE]-1,4-BENZOXAZIN-6-YL]-1-NAPHTHALENYLMETHANONE MESYLATE [(3R)-5-methyl-3-(morpholin-4-ylmethyl)-2,3-dihydro[1,4]oxazino[2,3,4-hi]indol-6-yl](naphthalen-1-yl)methanone methanesulfonate (R)-(+)-[2,3-Dihydro-5-methyl-3[(4-morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate salt |
CAS | 131543-23-2 |
EINECS | 1592732-453-0 |
化学式 | C28H30N2O6S |
分子量 | 522.61 |
InChI | InChI=1/C27H26N2O3.CH4O3S/c1-18-25(27(30)22-9-4-7-19-6-2-3-8-21(19)22)23-10-5-11-24-26(23)29(18)20(17-32-24)16-28-12-14-31-15-13-28;1-5(2,3)4/h2-11,20H,12-17H2,1H3;1H3,(H,2,3,4)/t20-;/m1./s1 |
沸点 | 627.7°C at 760 mmHg |
闪点 | 333.4°C |
蒸汽压 | 1.14E-15mmHg at 25°C |
溶解度 | 0.1 M HCl: 0.25mg/ml |
存储条件 | Store at +4°C |
稳定性 | 从提供的购买之日起稳定2年。在DMSO中的溶液可以在-20 ° 储存长达3个月。 |
外观 | 固体 |
颜色 | white to off-white |
物化性质 | 溶解度:0.1 M HCl: 0.25 mg/mL WGK Germany:3 |
体外研究 | 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. |
体内研究 | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.913 ml | 9.567 ml | 19.135 ml |
5 mM | 0.383 ml | 1.913 ml | 3.827 ml |
10 mM | 0.191 ml | 0.957 ml | 1.913 ml |
5 mM | 0.038 ml | 0.191 ml | 0.383 ml |
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