172895-39-5

172895-39-5 structure
172895-39-5 structure
  • Name: LY 266097 hydrochloride
  • Chemical Name: 1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole,hydrochloride
  • CAS Number: 172895-39-5
  • Molecular Formula: C21H24Cl2N2O2
  • Molecular Weight: 407.33300
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2017-03-04 02:44:54
  • Modify Date: 2024-01-09 10:33:43
  • 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].

Name 1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole,hydrochloride
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].
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

[1]. Rami Hamati, et al. Serotonin-2B receptor antagonism increases the activity of dopamine and glutamate neurons in the presence of selective serotonin reuptake inhibition. Neuropsychopharmacology. 2020 Nov;45(12):2098-2105.

[2]. Luc Maroteaux, et al. New therapeutic opportunities for 5-HT 2 receptor ligands. Pharmacol Ther. 2017 Feb;170:14-36.

Molecular Formula C21H24Cl2N2O2
Molecular Weight 407.33300
Exact Mass 406.12100
PSA 46.28000
LogP 5.70720
Storage condition -20°C
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H319
Precautionary Statements P305 + P351 + P338
Hazard Codes Xi
RIDADR NONH for all modes of transport
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