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Paroxetine is a selective serotonin reuptake inhibitor (SSRI; Ki = 0.04 nM).1 It is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (Kis = 400 and 90 nM, respectively) as well as the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2A, the histamine H1 receptor, α1- and α2-adrenergic receptors (α2-ARs), and muscarinic acetylcholine receptors (mAChRs; Kis = 21,168, 6,320, 13,746, 995, 3,915, and 42 nM, respectively).1,2 Paroxetine (5 mg/kg) decreases immobility time in the forced swim test in mice.3 Formulations containing paroxetine have been used in the treatment of depression, obsessive-compulsive disorder (OCD), panic disorder, social and generalized anxiety disorders, and post-traumatic stress disorder (PTSD).
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1. Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors. J. Med. Chem. 48(19), 6023-6034 (2005).
2. Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites. J. Pharmacol. Exp. Ther. 283(3), 1305-1322 (1997).
3. Involvement of the sigma1 receptor in the antidepressant-