Zolmitriptan

製品コードS1649 バッチS164903

印刷

化学情報

Chemical Structure Synonyms BW-311C90 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H21N3O2
分子量 287.36 CAS No. 139264-17-8
Solubility (25°C)* 体外 DMSO 57 mg/mL (198.35 mM)
Ethanol 57 mg/mL (198.35 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.85mg/ml (9.92mM) Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.41mg/ml (1.43mM) Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Zolmitriptan(BW-311C90) is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.
in vitro

Zolmitriptan produces concentration-dependent contractions of primate basilar artery and human epicardial coronary artery rings. This compound 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. [1] It 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. This compound-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. [2]
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. [1] This compound (10-1000 mg/kg, i.v.) selectively reduces arteriovenous-anastomotic (AVA) conductance producing a maximum decrease of 92.5%. It 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. This chemical (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. [3] It exerts behaviorally specific anti-aggressive effects in mice. This compound also decreases alcohol-heightened aggression with equal efficacy in mice. [4]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/9154322/
  • https://pubmed.ncbi.nlm.nih.gov/10844127/
  • https://pubmed.ncbi.nlm.nih.gov/9865508/
  • https://pubmed.ncbi.nlm.nih.gov/11594437/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Entry of therapeutics into the brain: Influence of exposed polarity calculated in silico and measured in vitro by supercritical fluid chromatography. [ Int J Pharm, 2019, 560:294-305] PubMed: 30771469

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。