(+)-Igmesine hydrochloride |
カタログ番号GC18146 |
σ1受容体リガンド
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 130152-35-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50:19.1ナノモル
JO 1784は選択的なσ1受容体リガンドです。
CNS σ受容体リガンドは、知られているように中枢神経伝達物質系(ノルアドレナリン、グルタミン酸、ドーパミンニューロンを含む)を調節します。
体外実験:対照群と比較して、フルオキセチン(18%)、デシプラミン(DMI、32%)およびJO 1784(20%)処理群ではβ-アドレナリン受容体の密度が有意に低下したが、σ1、5-HT1AおよびGABAB受容体は低下しなかった。チロシンヒドロキシラーゼ(TH)活性はすべての処理群で有意に減少した(30〜32%)。さらに、フルオキセチンとDMIを除くJO 1784処理群では、セロトニン(5-HT)およびノルアドレナリン(NE)神経細胞摂取量がそれぞれ85%および40%減少した。急性治療後、JO 1784は単アミン酸化酵素(MAO)AまたはBに対して不活性である[1]。
In vivo:行動学的に有効な用量での研究では、JO 1784はNE再取り込みに対して弱い影響を示しましたが、5-HTおよびDA合成の変化や選択的薬剤刺激による単胺神経再取り込み減少の拮抗作用はありませんでした。NMDA誘発性cGMP増強作用はJO 1784によって阻害されたため、JO 1784がNMDA受容体/NOS/cGMP経路に干渉する可能性があることを示唆しています。JO 1784の薬理作用は部分的にモノアミン系から調節されているようですが、抗うつ作用の他の可能なメカニズムを見つける必要があります[1]。
臨床試験:現時点では、まだ臨床研究は行われていません。
Reference:
[1]. Akunne HC, Zoski KT, Whetzel SZ, Cordon JJ, Brandon RM, Roman F, Pugsley TA. Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant. Neuropharmacology. 2001 Jul;41(1):138-49.
Cas No. | 130152-35-1 | SDF | |
Chemical Name | (R,E)-N-(cyclopropylmethyl)-N-methyl-3,6-diphenylhex-5-en-3-amine hydrochloride | ||
Canonical SMILES | CN([C@](C/C=C/C1=CC=CC=C1)(C2=CC=CC=C2)CC)CC3CC3.Cl | ||
Formula | C23H29N.HCl | M.Wt | 355.94 |
溶解度 | <17.8mg/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 | 2.8095 mL | 14.0473 mL | 28.0946 mL |
5 mM | 0.5619 mL | 2.8095 mL | 5.6189 mL |
10 mM | 0.2809 mL | 1.4047 mL | 2.8095 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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