GR 46611

Names

[ CAS No. ]:
185259-85-2

[ Name ]:
GR 46611

[Synonym ]:
GR 4661
Mecamylamine hydrochloride

Biological Activity

[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]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[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.