SSR 149415是一种选择性非肽类Vasopressin V1b Receptor拮抗剂。
Cas No.:439687-69-1
Sample solution is provided at 25 µL, 10mM.
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SSR 149415 is a selective, non-peptide antagonist of the Vasopressin V1b Receptor[1-2]. SSR 149415 is primarily used in research related to the treatment of stress-related disorders, such as depression and anxiety [3-4].
In vitro, pretreatment of In-R1-G9 cells with SSR 149415 (0.66–1.2nM) for 15 minutes, followed by stimulation with Arginine Vasopressin (AVP; 100nM) for 4–15 minutes, significantly inhibited AVP-induced intracellular calcium elevation and glucagon secretion, while also antagonized AVP-mediated cell proliferation[5].
In vivo, pretreatment of NMRI mice with SSR 149415 (10mg/kg) via intraperitoneal injection, followed by administration of AVP (20μg/kg), significantly reversed the anticonvulsant effect of AVP[7]. In a rat model of acute myocardial infarction (AMI), microinjection of SSR 149415 (40ng; 0.1μL) into the paraventricular nucleus (PVN) significantly ameliorated AMI-induced hemodynamic dysfunction and cardiac injury[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.
SSR 149415是一种选择性非肽类Vasopressin V1b Receptor拮抗剂[1-2]。SSR 149415主要被用于治疗应激相关障碍（如抑郁症和焦虑症）的相关研究中[3-4]。
在体外，SSR 149415（0.66–1.2nM）预处理In-R1-G9细胞15分钟，随后以精氨酸加压素（AVP；100nM）刺激4–15分钟，显著抑制AVP诱导的细胞内钙离子浓度升高和胰高血糖素分泌，同时拮抗AVP介导的细胞增殖作用[5]。
在体内，SSR 149415（10mg/kg）通过腹腔注射预处理NMRI小鼠，随后注射AVP（20μg/kg），SSR 149415显著逆转AVP的抗惊厥作用[6]。SSR 149415（40ng；0.1μL）通过下丘脑室旁核（PVN）微注射，用于处理急性心肌梗死（AMI）模型大鼠。SSR 149415显著改善了AMI诱导的血流动力学功能障碍和心脏损伤[7]。
| Cell experiment [1]: | |
Cell lines | In-R1-G9 cells (rat insulinoma cell line) |
Preparation Method | In-R1-G9 cells were maintained in appropriate culture medium. Cells were pretreated with SSR 149415 (0.66–1.2nM) for 15 minutes, followed by stimulation with AVP (100nM) for 4–15 minutes. |
Reaction Conditions | 0.66–1.2nM; pretreatment for15min. |
Applications | SSR 149415 significantly inhibited AVP-induced intracellular Ca²⁺ elevation and glucagon secretion in In-R1-G9 cells. SSR 149415 also antagonized AVP-mediated cell proliferation. In binding assays, SSR 149415 competitively inhibited [³H]AVP binding to In-R1-G9 cell membranes with high affinity (Ki=0.81±0.38nM), demonstrating stereospecificity and selectivity for V1b receptors over V1a and V2 receptors. |
| Animal experiment [2]: | |
Animal models | NMRI mice |
Preparation Method | Mice were pretreated with SSR 149415 (10mg/kg; i.p.) 60 minutes before administration of Arginine-Vasopressin (AVP) at pro-convulsant (0.1μg/kg; i.p.) or anti-convulsant (20μg/kg; i.p.) doses. Pentylenetetrazol (PTZ) was infused intravenously 30 minutes post-AVP to induce seizures. Seizure thresholds were measured, and plasma nitric oxide (NO) metabolites were quantified via the Griess reaction. |
Dosage form | 10mg/kg; i.p.; administered 60 minutes prior to AVP |
Applications | SSR 149415 reversed both pro-convulsant and anti-convulsant effects of AVP on PTZ-induced seizures. SSR 149415 normalized AVP-induced elevations in plasma NO metabolites. |
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 | ||
| 分子式 | C30H32ClN3O8S | 分子量 | 630.11 |
| 溶解度 | 63.01mg/ml in DMSO; 63.01mg/ml in ethanol | 储存条件 | Store at -20°C |
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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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