产品
编 号:F148438
分子式:C16H21N3O2
分子量:287.36
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10mM*1mL in DMSO
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询价
50mg
310
In-stock
100mg
320
In-stock
500mg
960
In-stock
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生物活性:
Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with Kis of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine.

体内研究:
Zolmitriptan (311C90; 3-30 μg/kg, i.v.) causes a dose-dependent inhibition of [125I]-albumin extravasation within the ipsilateral dura mater. Zolmitriptan also produces dose-dependent falls in cranial vascular conductance (32.3% at 30 μg/kg).Zolmitriptan is an anti-migraine agent with action at 5-HT1B/D receptors. Zolmitriptan is an effective and behaviorally specific anti-aggressive agent in situations that engender moderate and alcohol-heightened levels of aggression. Zolmitriptan (1-30 mg/kg, i.p.) exerts behaviorally specific anti-aggressive effects in mice."Animal Model:Anaesthetized guinea-pigs
Dosage:0, 3, 10, 30 μg/kg
Administration:I.v.
Result:In vehicle-treated animals, unilateral electrical stimulation of the trigeminal ganglion increased extravasation of [125I]-albumin into the dura on the side ipsilateral to stimulation producing a stimulated/unstimulated ratio of 1.57. Zolmitriptan decreased this ratio in a dose-dependent fashion.Zolmitriptan produced concomitant, dose-related falls in ear conductance.
Animal Model:Adult male CFW mice weighing approximately 25 g
Dosage:1, 3, 5.6, 10, 30, 56 mg/kg
Administration:Administered i.p. in a volume of 1 mL/100 g body weight
Result:Significantly decreased the frequency of attack bites.

体外研究:
Zolmitriptan (311C90) exhibits higher affinity to 5-HT than sumatriptan (pKA=6.63±0.04 and 6.16±0.03, respectively). 311C90 displays high affinity at human recombinant 5-HT1D and 5-HT1B receptors in transfected CHO-K1 cell membranes (pIC50 values=9.16±0.12 and 8.32±0.09, respectively) .
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