| Bioactivity | 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]. |
| Invitro | 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: |
| Name | LY266097 hydrochloride |
| CAS | 172895-39-5 |
| Formula | C21H24Cl2N2O2 |
| Molar Mass | 407.33 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [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. |