8-OH-DPAT

Description: 8-OH-DPAT (also known as 8-Hydroxy-DPAT) is a classic, potent and selective agonist of 5-HT1A with pIC50 of 8.19 for 5-HT1A. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site, and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B with pIC50 of 5.42 and pIC50 < 5 for 5-HT. Also It is able to reduce the accumulation of both autophagic-derived and photoreceptor outer segment-derived lipofuscin, increase antioxidant protection and reduce oxidative damage in cultured human RPE cells. Dysfunction of 5-HT1A receptors is involved in the narcoleptic-like sleep dysfunction in orexin KO mice, and such dysfunction may participate in orexin deficiency-induced sleep disorders. Further, the use of 5-HT1A receptor agonist such as 8-OH-DPAT could be useful for treating the sleep disorder under a deficiency of orexin.

References: PLoS One. 2012; 7(4):e34468; Psychopharmacology (Berl). 2016 Jun; 233(12):2343-53.

Related CAS#:76135-31-4 (HBr); 141215-27-2 (HCl)