RS 127445 |
カタログ番号GC11729
One-Click Copy Product Info
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RS 127445は経口活性で、高い選択性を持つ5-HT2B受容体拮抗剤であり、pKiは9.5であり、5-HT2Bに対する選択性は、5-HT2Aや5-HT2Cなど他の関連受容体よりも1000倍以上高かった。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 199864-87-4
Sample solution is provided at 25 µL, 10mM.
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RS 127445は経口活性で、高い選択性を持つ5-HT2B受容体拮抗剤であり、pKiは9.5であり、5-HT2Bに対する選択性は、5-HT2Aや5-HT2Cなど他の関連受容体よりも1000倍以上高かった[1, 2]。5-HT2B受容体は、中枢と末梢神経系で重要な役割を果たし、心血管効果や神経細胞の感作など様々な生理機能の制御に関与している[3]。RS 127445は側坐核でドーパミン神経伝達を阻害できる[4]。
体内で、RS 127445 (1-30mg/kg)をマウスに腹腔内注射した結果、腸の蠕動運動を著しく阻害し、排便量を用量依存的に減らした[5]。RS 127445 (10mg/kg)は経口投与の場合、実験性内臓過敏症ラットで、拘束ストレスによる内臓過敏症を著しく阻害し、阻害率は74%で、排便をも減らした[6]。
References:
[1] Bonhaus D W, Flippin L A, Greenhouse R J, et al. RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist[J]. British journal of pharmacology, 1999, 127(5): 1075-1082.
[2] Maroteaux L. Gene structure, expression, and 5-HT2B receptor signaling[M]//5-HT2B Receptors: From Molecular Biology to Clinical Applications. Cham: Springer International Publishing, 2021: 1-32.
[3] Monassier L. 5-HT2B Receptor, the Heart and Blood Vessels[M]//5-HT2B Receptors: From Molecular Biology to Clinical Applications. Cham: Springer International Publishing, 2021: 153-163.
[4] Cathala A, Devroye C, Robert É, et al. Serotonin2B receptor blockade in the rat dorsal raphe nucleus suppresses cocaine-induced hyperlocomotion through an opposite control of mesocortical and mesoaccumbens dopamine pathways[J]. Neuropharmacology, 2020, 180: 108309.
[5] Bassil A K, Taylor C M, Bolton V J N, et al. Inhibition of colonic motility and defecation by RS‐127445 suggests an involvement of the 5‐HT2B receptor in rodent large bowel physiology[J]. British journal of pharmacology, 2009, 158(1): 252-258.
[6] Ohashi‐Doi K, Himaki D, Nagao K, et al. A selective, high affinity 5‐HT2B receptor antagonist inhibits visceral hypersensitivity in rats[J]. Neurogastroenterology & Motility, 2010, 22(2): e69-e76.
| 動物実験 [1]: | |
動物モデル | 成体した雄C57BL/6Jマウス |
準備方法 | 3mL/kgの最終投与体積で、試験化合物（RS 127445 1、3、10または30mg/kg）または溶媒（10%のエタノール、40%のポリエチレングリコール、50%の蒸留H2O）を動物に腹腔内投与した。投与後、動物をケージに戻した。処理の3時間後、排出された糞便を採取し、量った；ペレットを紙製のトレイライナーに集め、尿または水からの汚染を最小限に抑えた。個体のラットから排泄された糞便ペレットの数と大きさに大きな差がある為、結果を、排泄されたペレットの平均湿重量SEMとして表した。 |
投与形態 | 1、3、10または30mg/kg；腹腔内注射 |
アプリケーション | RS 127445 (1-30 mg/kg)は用量依存的に排便量を減らし、用量が10と30mg/kgの場合は特に著しかった。 |
References: | |
| Cas No. | 199864-87-4 | SDF | |
| Chemical Name | 4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine | ||
| Canonical SMILES | FC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=CC=CC=C31 | ||
| Formula | C17H16FN3 | M.Wt | 281.33 |
| 溶解度 | ≥ 15.89mg/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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5545 mL | 17.7727 mL | 35.5454 mL |
| 5 mM | 710.9 μL | 3.5545 mL | 7.1091 mL |
| 10 mM | 355.5 μL | 1.7773 mL | 3.5545 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)