Name | 1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole,hydrochloride |
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Description | LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression[1]. |
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Related Catalog | |
Target |
5-HT2B Receptor:9.8 (pKi) 5-HT2A Receptor:7.7 (pKi) 5-HT2C Receptor:7.6 (pKi) |
In Vitro | LY266097 is a highly selective 5-HT2B receptor antagonist with a pKi of 9.7 for the human cloned 5-HT2B receptor and a 100-fold greater selectivity over human 5-HT2C and 5-HT2A sites[2]. |
In Vivo | LY266097 (0.6 mg/kg for 2-day administration) rescues Escitalopram-induced decrease in dopamine (DA) [1]. The administration of LY266097 alone or its addition on the last 3 days of a 14-day Escitalopram regimen increases pyramidal neuron firing and burst activity[1]. Animal Model: Male Sprague-Dawley rats weighing 250-350 g[1] Dosage: 0.6 mg/kg Administration: Administered i.p. alone or concomitantly with Escitalopram (2 mg/kg) for 2 days Result: Short-term administration (0.6 mg/kg/day for 2 days; i.p.) alone had no effect on these parameters, its co-administration counteracted the inhibitory effect of escitalopram on the firing activity of DA neurons, resulting in a recovery to control level. |
References |
Molecular Formula | C21H24Cl2N2O2 |
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Molecular Weight | 407.33300 |
Exact Mass | 406.12100 |
PSA | 46.28000 |
LogP | 5.70720 |
Storage condition | -20°C |
Symbol |
GHS07 |
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Signal Word | Warning |
Hazard Statements | H319 |
Precautionary Statements | P305 + P351 + P338 |
Hazard Codes | Xi |
RIDADR | NONH for all modes of transport |