Thioridazine-d3 (hydrochloride)

An internal standard for the quantification of thioridazine

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Background

Thioridazine-d₃ is intended for use as an internal standard for the quantification of thioridazine by GC- or LC-MS. Thioridazine is a typical antipsychotic.¹ It binds to dopamine D₂, histamine H₁, M₃ muscarinic, and α₁- and α₂-adrenergic receptors (K_is = 5-341.3 nM), as well as the serotonin (5-HT) receptor subtypes 5-HT_1A, 5-HT_2A, 5-HT_2C, 5-HT₆, and 5-HT₇ (K_is = 10-180.7 nM). Thioridazine (5 mg/kg) reduces amphetamine-induced repetitive head bobbing and oral behavior in rats.² It reduces conditioned fear stress-induced freezing behavior in rats when administered at doses ranging from 3 to 100 mg/kg.³ Thioridazine is also active against multidrug-resistant tuberculosis in vitro and in vivo.⁴

1.Kroeze, W.K., Hufeisen, S.J., Popadak, B.A., et al.H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugsNeuropsychopharmacology28(3)519-526(2003) 2.Tschanz, J.T., and Rebec, G.V.Atypical antipsychotic drugs block selective components of amphetamine-induced stereotypyPharmacol. Biochem. Behav.31(3)519-522(1988) 3.Ishida-Tokuda, K., Ohno, Y., Sakamoto, H., et al.Evaluation of perospirone (SM-9018), a novel serotonin-2 and dopamine-2 receptor antagonist, and other antipsychotics in the conditioned fear stress-induced freezing behavior model in ratsJpn. J. Pharmacol.72(2)119-126(1996) 4.Amaral, L.Thioridazine: An old neuroleptic effective against totally drug resistant tuberculosisActa Med. Port.25(2)118-121(2012)