SSR 149415 |
カタログ番号GC50376
One-Click Copy Product Info
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SSR 149415は選択的で、非ペプチドのVasopressin V1b Receptorの拮抗剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 439687-69-1
Sample solution is provided at 25 µL, 10mM.
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SSR 149415は選択的で、非ペプチドのVasopressin V1b Receptorの拮抗剤である[1-2]。SSR 149415は、主に鬱病や不安などのストレス関連障害の治療に関連する研究に使われている[3-4]。
体外で、SSR 149415（0.66–1.2nM）でIn-R1-G9細胞を15分間事前処理し、続いてアルギニン・バゾプレッシン（Arginine Vasopressin、AVP；100nM）で4-15分間刺激した結果、AVP誘発の細胞内カルシウムの上昇とグルカゴンの分泌を著しく阻害し、AVP媒介の細胞増殖をも拮抗した[5]。
体内で、SSR 149415（10mg/kg）をNMRIマウスに腹腔内注射して事前処理し、続いてAVP（20μg/kg）を投与した結果、AVPの抗痙攣作用を著しく逆転させた[7]。急性心筋梗塞（AMI）のラットモデルで、SSR 149415（40ng；0.1μL）を室傍核（PVN）を微小注射した結果、AMI誘発の血行動態機能障害と心臓損傷を著しく改善した[8]。
References:
[1] Serradeil-Le Gal C, Raufaste D, Derick S, et al. Biological characterization of rodent and human vasopressin V1b receptors using SSR-149415, a nonpeptide V1b receptor ligand. Am J Physiol Regul Integr Comp Physiol. 2007 Aug;293(2):R938-49.
[2] Decaux G, Soupart A, Vassart G. Non-peptide arginine-vasopressin antagonists: the vaptans. Lancet. 2008 May 10;371(9624):1624-32.
[3] Dannenhoffer CA, Kim EU, Saalfield J, et al. Oxytocin and vasopressin modulation of social anxiety following adolescent intermittent ethanol exposure. Psychopharmacology (Berl). 2018 Oct;235(10):3065-3077.
[4] Braida D, Donzelli A, Martucci R, et al. Neurohypophyseal hormones manipulation modulate social and anxiety-related behavior in zebrafish. Psychopharmacology (Berl). 2012 Mar;220(2):319-30.
[5] Folny V, Raufaste D, Lukovic L, et al. Pancreatic vasopressin V1b receptors: characterization in In-R1-G9 cells and localization in human pancreas. Am J Physiol Endocrinol Metab. 2003 Sep;285(3):E566-76.
[6] Javadian N, Rahimi N, Javadi-Paydar M, et al. The modulatory effect of nitric oxide in pro- and anti-convulsive effects of vasopressin in PTZ-induced seizures threshold in mice. Epilepsy Res. 2016 Oct;126:134-40.
[7] Cheng W, Sun Y, Wu Q, et al. Paraventricular Nucleus P2X7 Receptors Aggravate Acute Myocardial Infarction Injury via ROS-Induced Vasopressin-V1b Activation in Rats. Neurosci Bull. 2021 May;37(5):641-656.
| 細胞実験[1]: | |
細胞株 | In-R1-G9細胞（ラットインスリン産生細胞株） |
準備方法 | 適切な培養培地でIn-R1-G9細胞を培養した。細胞をSSR 149415（0.66–1.2nM）で15分間事前処理し、続いてAVP（100nM）で4-15分間刺激した。 |
反応条件 | 0.66–1.2nM；15分間の事前処理 |
アプリケーション | SSR 149415は、In-R1-G9細胞でAVP誘発の細胞内Ca²⁺の上昇とグルカゴンの分泌を著しく阻害した。SSR 149415はAVP媒介の細胞増殖をも拮抗した。結合アッセイで、SSR 149415は、高い親和性を持ち、In-R1-G9細胞膜との[³H]AVPの結合を競合的に阻害し（Ki=0.81±0.38nM）、V1aとV2受容体に対するV1b受容体の立体特異性と選択性を示した。 |
| 動物実験 [2]: | |
動物モデル | NMRIマウス |
準備方法 | マウスをSSR 149415（10mg/kg；腹腔内注射）で事前処理し、60分間後に、痙攣促進（0.1μg/kg、腹腔内投与）または抗痙攣の用量（20μg/kg、腹腔内投与）のArginine-Vasopressin（AVP）を投与した。AVPの30分後に、Pentylenetetrazol（PTZ）を静脈内潅流し、痙攣を誘発した。痙攣の閾値を測定し、血漿一酸化窒素（NO）の代謝物を、Griess反応を通じて定量化した。 |
投与形態 | 10mg/kg；腹腔内注射；AVPの60分前 |
アプリケーション | SSR 149415は、PTZ誘発の痙攣に対するAVPの痙攣促進と抗痙攣作用の両方を逆転させた。血漿NO代謝物で、SSR 149415はAVP誘発の上昇を正常化させた。 |
References: | |
| Cas No. | 439687-69-1 | SDF | |
| Canonical SMILES | COC1=CC(OC)=C(S(=O)(N2C([C@@](C3=CC(Cl)=CC=C23)(C4=C(C=CC=C4)OC)N5C[C@@H](C[C@H]5C(N(C)C)=O)O)=O)=O)C=C1 | ||
| Formula | C30H32ClN3O8S | M.Wt | 630.11 |
| 溶解度 | 63.01mg/ml in DMSO; 63.01mg/ml in ethanol | 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 | 1.587 mL | 7.9351 mL | 15.8702 mL |
| 5 mM | 317.4 μL | 1.587 mL | 3.174 mL |
| 10 mM | 158.7 μL | 793.5 μL | 1.587 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)