| CAS NO: | 139264-17-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 287.36 |
|---|---|
| Formula | C16H21N3O2 |
| 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 |
| Synonyms | 311C 90; Flezol; zolmitriptan; 311C90; 311 C90; trade names Zomig, Zomigon, AscoTop, Zomigoro |
| 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 Vivo | Zolmitriptan (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 model | Pigs |
| Formulation & Dosage | 3-30 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. |
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