(±)-McN 5652 |
カタログ番号GC16735 |
5-HT再取り込み阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 96795-89-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(±)-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.
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. |
Prepare stock solution | |||
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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