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Submit ReviewSR 141716A
说明： Selective CB1 inverse agonist
别名： Rimonabant hydrochloride
化学名： N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride
纯度： ≥99% (HPLC)
生物活性 for SR 141716A
SR 141716A is a potent and selective cannabinoid CB1 receptor antagonist (Ki = 1.98 nM). Also acts as an inverse agonist reversing adenylyl cyclase inhibition by WIN 55,212-2 (Cat.No. 1038) (IC50 = 48 nM). Displays no activity at CB2 receptors. Reduces food intake and body weight in orally dosed non-obese Wistar rats. Also μ-opioid receptor antagonist (Ki = 652 nm)
技术数据 for SR 141716A
| 分子量 | 500.25 |
| 公式 | C22H21Cl3N4O.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 158681-13-1 |
| PubChem ID | 104849 |
| InChI Key | REOYOKXLUFHOBV-UHFFFAOYSA-N |
| Smiles | O=C(NN4CCCCC4)C1=NN(C3=CC=C(Cl)C=C3Cl)C(C2=CC=C(Cl)C=C2)=C1C.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SR 141716A
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 50.02 | 100 |
制备储备液 for SR 141716A
以下数据基于产品分子量 500.25。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2 mL | 10 mL | 19.99 mL |
| 5 mM | 0.4 mL | 2 mL | 4 mL |
| 10 mM | 0.2 mL | 1 mL | 2 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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产品说明书 for SR 141716A
参考文献 for SR 141716A
参考文献是支持产品生物活性的出版物。
Janiak et al (2007) Blockade of cannabinoid CB1 receptors improves renal function, metabolic profile, and increased survival of obese Zucker rats. Kidney Int. 72 1345 PMID: 17882151
Rinaldi-Carmona et al (1994) SR 141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett. 350 240 PMID: 8070571
Rinaldi-Carmona et al (1995) Biochemical and pharmacological characterisation of SR 141716A, the first potent and selective brain cannabinoid receptor antagonist. Life Sci. 56 1941 PMID: 7776817
Colombo et al (1998) Appetite suppression and weight loss after the cannabinoid antagonist SR 141716. Life Sci. 63 113 PMID: 9718088
Seely et al (2012) AM-251 and rimon. act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies. Neuropharmacology 63 905 PMID: 22771770
If you know of a relevant reference for SR 141716A, please let us know.
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关键词: SR 141716A, SR 141716A supplier, SR141716A, rimonabant, cannabinoid, cb1, selective, potent, orally, available, inverse, agonists, antagonists, RIMO, Rimonabant, hydrochloride, CB1, Receptors, 0923, Tocris Bioscience
18 篇 SR 141716A 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SR 141716A 的部分引用包括：
Mahmoud et al (2015) (4-(Bis(4-fluorophenyl)methyl)piperazin-1-yl)(cyclohexyl)methanone hydrochloride (LDK1229): a new cannabinoid CB1 receptor inverse agonist from the class of benzhydryl piperazine analogs. Mol Pharmacol 87 197 PMID: 25411367
Tang and Alger (2015) Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome. J Neurosci 35 3938 PMID: 25740522
Sumislawski et al (2011) Reversible gating of endocannabinoid plasticity in the amygdala by chronic stress: a potential role for monoacylglycerol lipase inhibition in the prevention of stress-induced behavioral adaptation. Neuropsychopharmacology 36 2750 PMID: 21849983
Jimenez-Blasco et al (2020) Glucose metabolism links astroglial mitochondria to cannabinoid effects. Nature 583 603 PMID: 32641832
Marcu et al (2013) Novel insights into CB1 cannabinoid receptor signaling: a key interaction identified between the extracellular-3 loop and transmembrane helix 2. J Pharmacol Exp Ther 345 189 PMID: 23426954
Kapur et al (2008) Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction. J Pharmacol Exp Ther 325 341 PMID: 18174385
Pedersen et al (2021) A novel luminescence-based-β-arrestin recruitment assay for unmodified receptors J Biol Chem 296 100503 PMID: 33684444
Cecconi et al (2019) Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation. Int J Mol Sci 20 PMID: 31212770
Jiang et al (2017) Antidepressant-like effects of fenofi. in mice via the hippocampal brain-derived neurotrophic factor signalling pathway. Br J Pharmacol 174 177 PMID: 27861729
Khan et al (2018) Involvement of the CB2 cannabinoid receptor in cell growth inhibition and G0/G1 cell cycle arrest via the cannabinoid agonist WIN 55,212-2 in renal cell carcinoma. BMC Cancer 18 583 PMID: 29792186
Hayase (2016) Putative Epigenetic Involvement of the Endocannabinoid System in Anxiety- and Depression-Related Behaviors Caused by Nicotine as a Stressor. PLoS One 11 e0158950 PMID: 27404492
Bruijnzeel et al (2016) Behavioral Characterization of the Effects of Cannabis Smoke and Anandamide in Rats. PLoS One 11 e0153327 PMID: 27065006
Klingerman et al (2016) Acute Metabolic Effects of olanz. Depend on Dose and Injection Site. Dose Response 13 1559325815618910 PMID: 26740814
Kettunen et al (2005) Neuromodulation via conditional release of endocannabinoids in the spinal locomotor network. Neuron 45 95 PMID: 15629705
Graham et al (2006) Induction of Krox-24 by endogenous cannabinoid type 1 receptors in Neuro2A cells is mediated by the MEK-ERK MAPK pathway and is suppressed by the phosphatidylinositol 3-kinase pathway. Br J Pharmacol 281 29085 PMID: 16864584
Stanford et al (2001) Identification of two distinct vasodilator pathways activated by ATP in the mesenteric bed of the rat. Br J Pharmacol 133 825 PMID: 11454655
Martin et al (2000) Effects of cannabinoid receptor agonists on neuronally-evoked contractions of urinary bladder tissues isolated from rat, mouse, pig, dog, monkey and human. Front Mol Neurosci 129 1707 PMID: 10780977
MacLennan et al (1998) Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB1 and CB2 receptors. Br J Pharmacol 124 619 PMID: 9690851
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Rimonabant treatment in mice.
By
Sebastiaan Dalle on 05/24/2023
分析类型： In Vivo
种属： Mouse
10mg/kg body weight, dissolved in solution with 6.7% dmso, 1.7% tween80 and 91.6% saline; intraperitoneally injected.
Rimonabant stock was prepared in dmso and tween80, and consequently freshly diluted with saline.
Highly recommend..
By
Anonymous on 06/01/2020
分析类型： Ex Vivo
种属： Mouse
细胞系/组织： Bed nucleus of the stria terminalis
SR 141716A was solubilized in DMSO and bath applied at a 5 micromolar concentration. It effectively blocked CB1-receptor-dependent long term depression of evoked excitatory postsynaptic current in the bed nucleus of the stria terminalis.
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