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Involvement of sigma-1 receptor modulation in the antidepressant action of venlafaxine.
Neurosci Lett. 2007 Jun 15; 420(3):204-8.NL

Abstract

Multiple lines of investigation have explored the role of sigma receptors in mental depression. Sigma receptors particularly, sigma-1 subtype is known to modulate the release of various catecholamines in the brain and may play, in some way, a role in the mechanism of action of various antidepressants. The present study investigated the possible involvement of sigma receptors in modulating the antidepressant-like effect of venlafaxine (dual serotonin and norepinephrine reuptake inhibitor) in the mouse forced swim test (FST). Immobility period in the forced swim test was registered for a total period of 6 min. Venlafaxine produced dose-dependent (4-16 mg/kg, i.p.) reduction in immobility period. Pretreatment of mice with (+)-pentazocine (2.5 mg/kg, i.p.), a high-affinity sigma-1 receptor agonist, produced synergism with subeffective dose of venlafaxine (2 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 venlafaxine (8 mg/kg i.p.). The various modulators used in the study did not produce any changes in locomotor activity per se except venlafaxine which at higher dose (16 mg/kg, i.p.) significantly increased the locomotor activity in mice. The results for the first time demonstrated that the anti-immobility effects of venlafaxine in the FST possibly involve an interaction with sigma-1 receptors.

Authors+Show Affiliations

Pharmacology Division, University Institute of Pharmaceutical Sciences, Punjab University, Chandigarh 160014, India.No affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17532136

Citation

Dhir, Ashish, and S K. Kulkarni. "Involvement of Sigma-1 Receptor Modulation in the Antidepressant Action of Venlafaxine." Neuroscience Letters, vol. 420, no. 3, 2007, pp. 204-8.
Dhir A, Kulkarni SK. Involvement of sigma-1 receptor modulation in the antidepressant action of venlafaxine. Neurosci Lett. 2007;420(3):204-8.
Dhir, A., & Kulkarni, S. K. (2007). Involvement of sigma-1 receptor modulation in the antidepressant action of venlafaxine. Neuroscience Letters, 420(3), 204-8.
Dhir A, Kulkarni SK. Involvement of Sigma-1 Receptor Modulation in the Antidepressant Action of Venlafaxine. Neurosci Lett. 2007 Jun 15;420(3):204-8. PubMed PMID: 17532136.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Involvement of sigma-1 receptor modulation in the antidepressant action of venlafaxine. AU - Dhir,Ashish, AU - Kulkarni,S K, Y1 - 2007/04/29/ PY - 2007/02/27/received PY - 2007/03/26/revised PY - 2007/04/23/accepted PY - 2007/5/29/pubmed PY - 2007/9/27/medline PY - 2007/5/29/entrez SP - 204 EP - 8 JF - Neuroscience letters JO - Neurosci Lett VL - 420 IS - 3 N2 - Multiple lines of investigation have explored the role of sigma receptors in mental depression. Sigma receptors particularly, sigma-1 subtype is known to modulate the release of various catecholamines in the brain and may play, in some way, a role in the mechanism of action of various antidepressants. The present study investigated the possible involvement of sigma receptors in modulating the antidepressant-like effect of venlafaxine (dual serotonin and norepinephrine reuptake inhibitor) in the mouse forced swim test (FST). Immobility period in the forced swim test was registered for a total period of 6 min. Venlafaxine produced dose-dependent (4-16 mg/kg, i.p.) reduction in immobility period. Pretreatment of mice with (+)-pentazocine (2.5 mg/kg, i.p.), a high-affinity sigma-1 receptor agonist, produced synergism with subeffective dose of venlafaxine (2 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 venlafaxine (8 mg/kg i.p.). The various modulators used in the study did not produce any changes in locomotor activity per se except venlafaxine which at higher dose (16 mg/kg, i.p.) significantly increased the locomotor activity in mice. The results for the first time demonstrated that the anti-immobility effects of venlafaxine in the FST possibly involve an interaction with sigma-1 receptors. SN - 0304-3940 UR - https://www.unboundmedicine.com/medline/citation/17532136/Involvement_of_sigma_1_receptor_modulation_in_the_antidepressant_action_of_venlafaxine_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0304-3940(07)00504-6 DB - PRIME DP - Unbound Medicine ER -