Possible involvement of sigma-1 receptors in the anti-immobility action of bupropion, a dopamine reuptake inhibitor

Fundamental & Clinical Pharmacology
Ashish Dhir, Shrinivas K Kulkarni

Abstract

Sigma receptors particularly, sigma-1 subtype is known to modulate the release of catecholamines in the brain and may participate in the mechanism of action of various antidepressants. The present study investigated the possible involvement of sigma receptors in modulating the anti-immobility-like effect of bupropion (a dopamine reuptake inhibitor) using the forced swim test (FST) in mice. Bupropion produced dose-dependent (10-40 mg/kg, i.p.) reduction in immobility period and the ED(50) value was found to be 18.5 (7.34-46.6) mg/kg, i.p. (+)-Pentazocine (2.5 mg/kg, i.p.), a high-affinity sigma-1 receptor agonist, produced synergistic response when it was co-administered with a subeffective dose of bupropion (10 mg/kg, i.p.). On the contrary, pretreatment with progesterone (10 mg/kg, s.c.), a sigma-1 receptor antagonist neurosteroid, rimcazole (5 mg/kg, i.p.), another sigma-1 receptor antagonist, or BD 1047 (1 mg/kg, i.p.), a novel sigma-1 receptor antagonist, reversed the anti-immobility effects of bupropion (20 mg/kg, i.p.). The various modulators used in the study did not show any effect per se on locomotor activity except bupropion which at a higher dose (15-40 mg/kg, i.p.) significantly increased the locomotor activity. The...Continue Reading

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Citations

Jul 1, 2009·Expert Review of Clinical Pharmacology·Rae R Matsumoto
Jul 11, 2009·Expert Review of Neurotherapeutics·Shrinivas K Kulkarni, Ashish Dhir
May 12, 2009·Expert Opinion on Investigational Drugs·Shrinivas K Kulkarni, Ashish Dhir
May 6, 2010·Journal of Ethnopharmacology·Geun Hee SeolSun Seek Min
Dec 23, 2008·Behavioural Brain Research·Valentina SabinoEric P Zorrilla
Jul 26, 2012·Fundamental & Clinical Pharmacology·Jeferson Falcão do AmaralFrancisca Cléa Florenço de Sousa
Aug 24, 2012·Fundamental & Clinical Pharmacology·Francisca Cléa Florenço de SousaJosé Maria Barbosa Filho
Jun 10, 2015·Journal of Receptor and Signal Transduction Research·Colin G Rousseaux, Stephanie F Greene
Feb 1, 2011·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Ashish DhirS K Kulkarni
May 24, 2011·Journal of Affective Disorders·Konstantinos N FountoulakisHagop Akiskal
Sep 4, 2012·Pharmacology, Biochemistry, and Behavior·Katarzyna SocałaPiotr Wlaź
Feb 28, 2015·Indian Journal of Psychological Medicine·Kazhungil FirozTm Raghuram
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Aug 5, 2020·Expert Opinion on Therapeutic Targets·James Michael BrimsonTewin Tencomnao
May 3, 2019·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Tangui MauriceJean-Luc Pirat

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