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Zolmitriptan
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Zolmitriptan图片
CAS NO:139264-17-8
规格:≥98%
包装与价格:
包装价格(元)
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)287.36
FormulaC16H21N3O2
CAS No.139264-17-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 58 mg/mL (201.8 mM)
Water: <1 mg/mL
Ethanol: 58 mg/mL (201.8 mM)
Other info

Chemical Name: (4S)-4-[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]-1,3-oxazolidin-2-one

InChi Key: ULSDMUVEXKOYBU-ZDUSSCGKSA-N

InChi Code: InChI=1S/C16H21N3O2/c1-19(2)6-5-12-9-17-15-4-3-11(8-14(12)15)7-13-10-21-16(20)18-13/h3-4,8-9,13,17H,5-7,10H2,1-2H3,(H,18,20)/t13-/m0/s1

SMILES Code: O=C1OC[C@H](CC2=CC3=C(NC=C3CCN(C)C)C=C2)N1

Synonyms311C 90; Flezol; zolmitriptan; 311C90; 311 C90; trade names Zomig, Zomigon, AscoTop, Zomigoro
实验参考方法
In Vitro

In vitro activity: Zolmitriptan produces concentration-dependent contractions of primate basilar artery and human epicardial coronary artery rings. Zolmitriptan displays high affinity at human recombinant 5-HT1D (formerly 5-HT1D alpha) and 5-HT1B (formerly 5-HT1D beta) receptors in transfected CHO-K1 cell membranes. Zolmitriptan increases I(K) in a concentration-dependent manner (maximum increase 16.3%) with a pD(2) value of 7.03 in C6 glioma cells expressing recombinant human 5-HT(1B) receptor. Zolmitriptan-induced increases in I(K) are prevented by the calcium chelator, EGTA (5 mM) when included in the patch pipette in C6 cells expressing cloned human 5-HT(1B) receptors.

In VivoZolmitriptan (3-30 mg/kg, i.v.) administrated ten minutes before unilateral electrical stimulation of the trigeminal ganglion causes a dose-dependent inhibition of [125I]-albumin extravasation within the ipsilateral dura mater in anaesthetized guinea-pigs. Zolmitriptan (10-1000 mg/kg, i.v.) selectively reduces arteriovenous-anastomotic (AVA) conductance producing a maximum decrease of 92.5%. Zolmitriptan also produces a modest reduction in extra-cerebral conductance (23.9% maximum reduction at 30 mg/kg, i.v.), but is without effect on cerebral conductance. Zolmitriptan (1-30 mg/kg, i.v.) produces dose-dependent decreases in ear microvascular conductance (15% to 60%) which mirror decreases in carotid arterial conductance in anaesthetised cats. Zolmitriptan exerts behaviorally specific anti-aggressive effects in mice. Zolmitriptan also decreases alcohol-heightened aggression with equal efficacy in mice.
Animal modelPigs
Formulation & Dosage3-30 mg/kg, i.v.
References

Br J Pharmacol. 1997 May;121(2):157-64; Eur J Pharmacol. 1998 Nov 20;361(2-3):191-7.