Setiptiline-d3

Setiptiline-d3 (Org-8282-d3) is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Yamada K, Furukawa T. [Behavioral effects of a new antidepressant, setiptiline]. Nihon Yakurigaku Zasshi. 1991 Jan;97(1):31-9.

[3]. Kamimura M, Aoba A, Yamaguchi N et al. The effect of age on plasma level of setiptiline maleate in depressed patients. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Oct;18(6):1015-26.

[4]. Kuniyoshi M, Nakamura J, Miura C, Inanaga K. Effectiveness of concomitant setiptiline maleate (Tecipul) on negative symptoms of schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Mar;18(2):339-46.

[5]. Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K. [Pharmacological properties of MO-8282, a novel antidepressant]. Nihon Yakurigaku Zasshi. 1986 Oct;88(4):309-20.