Zolmitriptan (BW-311C90; 311C90) 是一种5-HT1B/1D受体部分激动剂，对 5-HT1B、5-HT1D、5-HT1F 受体的Ki分别为 5.01 nM、0.63 nM 和 63.09 nM。Zolmitriptan可用于偏头痛的研究。
| 生物活性 | Zolmitriptan (BW-311C90; 311C90) is a5-HT1B/1D receptorpartial agonist withKis 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[1][2]. |
| IC50& Target[1] | Human Endogenous Metabolite | 5-HT1BReceptor 5.01 nM (Ki) | 5-HT1DReceptor 0.63 nM (Ki) | 5-HT1FReceptor 63.09 nM (Ki) |
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体外研究
(In Vitro) | 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 (pIC50values=9.16±0.12 and 8.32±0.09, respectively)[1].
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体内研究
(In Vivo) | "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)[1].
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[3]."
| Animal Model: | Anaesthetized guinea-pigs[1] | | 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[3] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(348.00 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.4800 mL | 17.3998 mL | 34.7996 mL | | 5 mM | 0.6960 mL | 3.4800 mL | 6.9599 mL | | 10 mM | 0.3480 mL | 1.7400 mL | 3.4800 mL |
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以下溶剂前显示的百
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此方案可获得 ≥ 2.5 mg/mL (8.70 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.70 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: 2.5 mg/mL (8.70 mM); Suspended solution; Need ultrasonic
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