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(±)-McN 5652

カタログ番号GC16735

5-HT再取り込み阻害剤

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(±)-McN 5652 化学構造

Cas No.: 96795-89-0

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Sample solution is provided at 25 µL, 10mM.

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Background

(±)-McN 5652は、ラット脳シナプトソームにおけるセロトニン(5-HT、5-ヒドロキシトリプタミン)の取り込みを非常に強力に阻害する物質であり、in vitroではKi値が約0.6 nM、ex vivoではED50値が約2 mg/kg p.o.です[1]。

5-HTは、哺乳動物の神経系において多数の感覚、行動プロセス、運動を調節する単胺性神経伝達物質です[2]。少なくとも3つの主要な5-HT受容体グループがあります:5-HT1、5-HT2、そして5-HT3です。それぞれのグループは構造的にも操作上も異なります。各受容体グループには独自の転写システムがあります。 5-HT4は最近特定された受容体であり、実質的に第4の5-HT受容体クラスを表します[3]。

受容体結合実験により、McN-5652はセロトニン5-HT2受容体に弱い親和性(表面上のKi約200 nM)を持ち、セロトニン5-HT1受容体に非常に低い親和性を示すことが示されました[1]。

生体内では、ラットにおいてセロトニン症候群を増強するために低用量のMcN-5652が必要でした。このセロトニン症候群に対して、p.o.投与後2時間でED50値は1.5 mg/kgでした。マウスにおいてL-5-ヒドロキシトリプトファン(L-5HTP)によって誘発される頭部けいれんを増強するためには、p.o.投与後2時間でED50値はわずか0.4 mg/kgです。これは、McN-5652が高いポテンシャルを持つセロトニン再取り込み阻害剤であることを意味します[1]。

References:
[1].  Shank RP, Vaught JL, Pelley KA, et al. McN-5652: a highly potent inhibitor of serotonin uptake. J Pharmacol Exp Ther, 1988, 247(3):1032-8.
[2].  Tecott LH, Sun LM, Akana SF, et al. Eating disorder and epilepsy in mice lacking 5-HT2c serotonin receptors. Nature, 1995, 374(6522):542-6.
[3].  Hoyer D, Clarke DE, Fozard JR, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev, 1994, 46(2):157-203.

Chemical Properties

Cas No. 96795-89-0 SDF
Chemical Name (6R,10bS)-6-(4-(methylthio)phenyl)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline
Canonical SMILES CSC1=CC=C(C=C1)[C@H]2CN3[C@H](C4=CC=CC=C24)CCC3
Formula C19H21NS M.Wt 295.44
溶解度 <14.77mg/ml in 1eq. HCl; <22.16mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.3848 mL 16.9239 mL 33.8478 mL
5 mM 0.677 mL 3.3848 mL 6.7696 mL
10 mM 0.3385 mL 1.6924 mL 3.3848 mL
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