Name | 1-(1-methylindol-5-yl)-3-pyridin-3-ylurea |
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Synonyms |
Mip-urea
Tocris-1371 |
Description | SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo[1][2]. |
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Related Catalog | |
Target |
5-HT2B Receptor:7.5 (pKi) 5-HT2C Receptor:6.9 (pKi) 5-HT2A Receptor:5.2 (pKi) |
In Vitro | SB-200646 (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency[1]. |
In Vivo | SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) treatment significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons[1]. The i.v. administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and % events as bursts in spontaneously active VTA dopaminergic neurons and significantly increases the % events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons[1]. Animal Model: Male albino Sprague-Dawley rats (200-225 g at the beginning of treatment and 300-350 g at the time of the experiment)[1] Dosage: 20 mg/kg Administration: Intravenous injection; daily; for 21 days Result: Significantly decreased the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons. |
References |
Density | 1.26g/cm3 |
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Boiling Point | 390.9ºC at 760mmHg |
Molecular Formula | C15H14N4O |
Molecular Weight | 266.29800 |
Flash Point | 190.2ºC |
Exact Mass | 266.11700 |
PSA | 58.95000 |
LogP | 3.36330 |
Vapour Pressure | 2.57E-06mmHg at 25°C |
Index of Refraction | 1.663 |
Storage condition | 2-8°C |