GR 46611

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GR 46611 是一种选择性 5-HT1B 和 5-HT1D 受体激动剂，可用于癫痫治疗的研究。

GR 46611 is a selective 5-HT1B and 5-HT1D receptor agonist and can be used in studies about the treatment of epilepsy.(In Vivo):GR 46611 (0.6 and 6 nmol; paraventricular hypothalamic nucleus (PVN)) promptly and reliably elicited feeding at their higher doses, without affecting drinking or non-ingestive behaviors. GR 46611 (6 nmol) elicited intense feeding responses in the n. medialis hypothalami posterioris and in the adjacent n. lateralis hypothalami posterioris (PMH/PLH complex, in the caudoventral hypothalamus) and in the n. magnocellularis preopticus (PPM, in the caudal preoptic region). GR 46611 (1 mg/kg) significantly increased the threshold of hyperthermia-induced seizure and lowered seizure severity thereby improving the survival of DS mice.

GR-46611 (1 μM, 48 h) induces CEM cell proliferation. Cell Proliferation Assay 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%.

GR-46611 (1 mg/kg, i.p. ) significantly improves survival of Dravet syndrome (DS) mice.GR-46611 (0.03-300 μg/kg, i.v.) increases threshold volume, bladder capacity, and residual volume in chronic spinal cord injury (SCI) cats.GR46611 (3-30 mg/kg, s.c.) causes a dose-related decrease in rectal temperature in the adult guinea-pig. Animal Model:Dravet syndrome (DS) mice 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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Endocrinology/Hormones

5-HT Receptor

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185259-85-2

377.488

C23H27N3O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (264.91 mM)

COc1ccc(CNC(=O)\C=C/c2ccc3[nH]cc(CCN(C)C)c3c2)cc1

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(-20℃)

With Ice Pack

≥ 2 years