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  • DC Chemicals Limited
  • China
  • Product Name: GR-46611
  • Price: ¥Inquiry/100mg ¥Inquiry/250mg ¥Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 10 Day
  • Contact: Tony Cao

185259-85-2

185259-85-2 structure
185259-85-2 structure
  • Name: GR 46611
  • Chemical Name: (E)-3-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-[(4-methoxyphenyl)methyl]prop-2-enamide
  • CAS Number: 185259-85-2
  • Molecular Formula: C23H27N3O2
  • Molecular Weight: 377.47900
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2019-01-02 17:19:11
  • Modify Date: 2024-04-05 15:21:25
  • GR-46611 is a 5-HT1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia[1][3].

Name (E)-3-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-[(4-methoxyphenyl)methyl]prop-2-enamide
Synonyms GR 4661
Mecamylamine hydrochloride
Description GR-46611 is a 5-HT1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia[1][3].
Related Catalog
Target

5-HT1D Receptor

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%.
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.
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.

Density 1.168g/cm3
Boiling Point 645.9ºC at 760mmHg
Molecular Formula C23H27N3O2
Molecular Weight 377.47900
Flash Point 344.4ºC
Exact Mass 377.21000
PSA 57.36000
LogP 4.00110
Vapour Pressure 1.43E-16mmHg at 25°C
Index of Refraction 1.639
Storage condition -20°C
Hazard Codes Xi: Irritant;
Risk Phrases R36/37/38
Safety Phrases S26