(Z)-Thiothixene-d₈  (Synonyms: NSC 108165-d₈; Navan-d₈; Navane-d₈)

(Z)-Thiothixene-d₈ (NSC 108165-d₈; Navan-d₈; Navane-d₈) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

451.67

C₂₃H₂₁D₈N₃O₂S₂

5591-45-7

O=S(C1=CC2=C(SC3=CC=CC=C3/C2=C\CCN4C([2H])(C([2H])(N(C([2H])(C4([2H])[2H])[2H])C)[2H])[2H])C=C1)(N(C)C)=O

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• [1]. Silvestre, et al. Research on adverse drug events. I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes. Methods Find. Exp. Clin. Pharmacol. 27(5), 289-304 (2005).