Introduction:Basic information about CAS 185259-85-2|GR 46611, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | GR 46611 |
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| CAS Number | 185259-85-2 | Molecular Weight | 377.47900 |
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| Density | 1.168g/cm3 | Boiling Point | 645.9ºC at 760mmHg |
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| Molecular Formula | C23H27N3O2 | Melting Point | / |
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| MSDS | / | Flash Point | 344.4ºC |
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Names
| Name | (E)-3-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-[(4-methoxyphenyl)methyl]prop-2-enamide |
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| Synonym | More Synonyms |
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GR 46611 BiologicalActivity
| Description | GR-46611 is a 5-HT1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia[1][3]. |
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| Related Catalog | Research Areas >>CancerSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor |
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| Target | 5-HT1D Receptor |
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| In Vitro | GR-46611 (1 μM, 48 h) induces CEM cell proliferation[2]. Cell Proliferation Assay[2] Cell Line: CEM cells (human T lymphoblastic leukemia cell line) Concentration: 1 μM Incubation Time: 48 h Result: Induced a significant increase in cell proliferation by 37.0%. |
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| In Vivo | GR-46611 (1 mg/kg, i.p. ) significantly improves survival of Dravet syndrome (DS) mice[1]. GR-46611 (0.03-300 μg/kg, i.v.) increases threshold volume, bladder capacity, and residual volume in chronic spinal cord injury (SCI) cats[3]. GR46611 (3-30 mg/kg, s.c.) causes a dose-related decrease in rectal temperature in the adult guinea-pig[4]. Animal Model: Dravet syndrome (DS) mice[1] Dosage: 0.01, 0.1 and 1 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Improved survival relative to vehicle treated controls with 89% surviving rate. |
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| References | [1]. Paul G Hatini, et al. A 5-HT 1D -receptor agonist protects Dravet syndrome mice from seizure and early death. Eur J Neurosci. 2020 Nov;52(10):4370-4374. [2]. C Sibella-Argüelle, et al. The proliferation of human T lymphoblastic cells induced by 5-HT1B receptors activation is regulated by 5-HT-moduline. C R Acad Sci III. 2001 Apr;324(4):365-72. [3]. Baojun Gu, et al. Inhibition of bladder activity by 5-hydroxytryptamine1 serotonin receptor agonists in cats with chronic spinal cord injury. J Pharmacol Exp Ther. 2004 Sep;310(3):1266-72. [4]. M Skingle, et al. Stimulation of central 5-HT1D receptors causes hypothermia in the guinea-pig. J Psychopharmacol. 1994 Jan;8(1):14-21. |
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Chemical & Physical Properties
| Density | 1.168g/cm3 |
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| Boiling Point | 645.9ºC at 760mmHg |
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| Molecular Formula | C23H27N3O2 |
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| Molecular Weight | 377.47900 |
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| Flash Point | 344.4ºC |
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| Exact Mass | 377.21000 |
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| PSA | 57.36000 |
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| LogP | 4.00110 |
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| Vapour Pressure | 1.43E-16mmHg at 25°C |
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| Index of Refraction | 1.639 |
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| InChIKey | LBVZWEWTNUDWNS-YRNVUSSQSA-N |
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| SMILES | COc1ccc(CNC(=O)C=Cc2ccc3[nH]cc(CCN(C)C)c3c2)cc1 |
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| Storage condition | -20°C |
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Safety Information
| Hazard Codes | Xi: Irritant; |
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| Risk Phrases | R36/37/38 |
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| Safety Phrases | S26 |
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Synonyms
| GR 4661 |
| Mecamylamine hydrochloride |