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Tramadol’s Inhibitory Effects on Sexual Behavior: Pharmacological Studies in Serotonin Transporter Knockout Rats
Journal article   Open access   Peer reviewed

Tramadol’s Inhibitory Effects on Sexual Behavior: Pharmacological Studies in Serotonin Transporter Knockout Rats

Diana C. Esquivel-Franco, Berend Olivier, Marcel D. Waldinger, Gabriel Gutiérrez-Ospina and Jocelien D. A. Olivier
Frontiers in pharmacology, v 9, pp 676-676
27 Jun 2018
DOI: https://doi.org/10.3389/fphar.2018.00676
PMID: 29997507
Featured in Collection :   UN Sustainable Development Goals @ Drexel
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https://doi.org/10.3389/fphar.2018.00676View
Published, Version of Record (VoR)CC BY V4.0,  Open

Abstract

5-HT1A receptor Pharmacology rat serotonin transporter sexual behavior SSRI tramadol μ-opioid receptor
Tramadol is an effective pharmacological intervention in human premature ejaculation (PE). To investigate whether the inhibitory action of tramadol is primarily caused by its selective serotonin reuptake inhibitory (SSRI) effects we tested the dose–response effects of tramadol on sexual behavior in serotonin transporter wild type (SERT +/+ ), heterozygous (SERT +/- ), and knockout (SERT -/- ) rats. To investigate whether other mechanisms contribute to the inhibitory effects, WAY100,635, a 5-HT 1A receptor antagonist and naloxone, a μ-opioid receptor antagonist, were tested on sexual behavior together with tramadol. Tramadol dose-dependently decreases sexual activity in all genotypes. In all studies, SERT +/- rats did not respond differently from SERT +/+ rats. WAY100,635 did not affect sexual activity in SERT +/+ , but dose-dependently reduced sexual activity in SERT -/- rats. WAY100,635 (0.3 mg/kg) combined with tramadol (20 mg/kg) significantly reduced sexual activity in SERT +/+ and even stronger in SERT -/- rats. Naloxone did not affect sexual behavior consistently in SERT +/+ rats, while in SERT -/- rats all doses reduced ejaculation frequency mildly. Combining naloxone (20 mg/kg) and tramadol (20 mg/kg) decreased ejaculation frequencies in both genotypes. Interestingly, combining tramadol (20 mg/kg), WAY100,635 (0.3 mg/kg) and naloxone (20 mg/kg) led to complete elimination of all sexual activity in both SERT +/+ and SERT -/- rats. These findings suggest that the inhibitory effects of tramadol on male sexual behavior in SERT +/+ rats is mainly, if not exclusively, due to SERT inhibition, with an important role for 5-HT 1A receptors, although influence of other systems (e.g., noradrenergic) cannot be excluded. As SSRIs exert their sexual inhibition after chronic administration, tramadol may be therapeutically attractive as “on demand” therapy for PE.

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#3 Good Health and Well-Being
#5 Gender Equality

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Web of Science research areas
Pharmacology & Pharmacy
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