Interaction between the tetracyclic antidepressant mianserin HCl and opioid receptors

Schreiber, Shaul; Backer, Maria M; Kaufman, Jarrod P.; Pick, Chaim G.

doi:10.1016/s0924-977x(97)00088-6

Cited by 23 publications

(16 citation statements)

References 21 publications

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“…These results suggest that activation of central, but not peripheral, µ-opioid receptors mediate tianeptine-induced antinociception. Several lines of evidence suggest the role of µ-opioid receptors in the antinociception induced by different antidepressant drugs [20, 22]. Since none of these studies have used peripherally restricted opioid antagonist NLXM at its μ-opioid receptor-selective dose, our study confirms and extends these studies indicating the involvement of µ-opioid receptors.…”

Section: Discussionsupporting

confidence: 80%

Opioid Receptors Contribute to Antinociceptive Effect of Tianeptine on Colorectal Distension-Induced Visceral Pain in Rats

et al. 2017

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Tianeptine is a clinically effective atypical antidepressant with distinct neurochemical properties. In this study, we aimed to investigate the contribution of opioid receptors in the antinociceptive effect of tianeptine on visceral pain in awake rats and to differentiate the subtype and the localization (central and/or peripheral) of these opioid receptors involved in this antinociception. Visceromotor response to noxious colorectal distension (CRD) was quantified with electromyographic recordings, obtained from previously implanted electrodes into the external oblique musculature of rats under anesthesia, before and after tianeptine administration. The opioid receptor antagonist naloxone hydrochloride (NLX) and peripherally restricted opioid receptor antagonist naloxone methiodide (NLXM) were administered intravenously 10 min before tianeptine (10 mg/kg, i.v.). The antinociceptive effect of tianeptine was abolished by NLX (1 and 2 mg/kg, i.v.), but was partially reduced by NLXM (1 and 2 mg/kg, i.v.). A µ-opioid receptor-selective dose (0.03 mg/kg, i.v.) of NLX, but not NLXM, significantly inhibited the antinociceptive effect of tianeptine. Our results suggest that antinociceptive effect of tianeptine on CRD-induced visceral nociception in rats involves the activation of both central and peripheral opioid receptors.

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Section: Discussionsupporting

confidence: 80%

Opioid Receptors Contribute to Antinociceptive Effect of Tianeptine on Colorectal Distension-Induced Visceral Pain in Rats

et al. 2017

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“…Mianserin'in antidepresan etkinliğinin yanı sıra analjezik etkinliğe de sahip olduğu rapor edilmiştir 15,16 . Ancak, literatürde bu ilacın normoglisemik ya da hiperglisemik koşullarda kan glukozu üzerine etkilerine ilişkin detaylı bir deneysel araştırmaya rastlanmamıştır.…”

Section: Introductionunclassified

Mianserin’in sıçanlarda streptozotosin ile indüklenen hiperglisemi ve metabolik değişiklikler üzerine etkisi

Can

Üçel

Özkay

et al. 2017

Cukurova Medical Journal (Çukurova Üniversitesi Tıp Fakültesi Dergisi)

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AbstractÖz Purpose: The aim of this study was to investigate possible effects of atypical antidepressant mianserin on glycemia levels and metabolic parameters of normoglycemic and diabetic rats. Material and Methods: Effects of mianserin administration on blood glucose levels in rats were assessed by measuring "fasting blood glucose", "glycosylated haemoglobin" levels and conducting the "oral glucose tolerance test". Changes in metabolic parameters such as food and water consumption and urine and faeces excretion were observed using metabolic cages. Results: Administration of mianserin for 7 and 14 days at doses of 30 and 45 mg/kg significantly reduced the hyperglycemia and elevated HbA1c levels; also improved hyperglycemia induced polydipsia, polyuria, polyphagia, and increased faeces amounts. Mianserin, at both of the administrated doses, reduced the weight loss observed in diabetic animals. With regard to the anti-hyperglycaemic effect, mianserin administered at a dose of 30 mg/kg was found to be as effective as the reference drug metformin (dose, 1 g/kg). Conclusion: This study showed that the antihyperglycemic effect of mianserin, an atypical antidepressant, was comparable to those of the reference drug metformin. However, the pharmacological mechanisms underlying this anti-hyperglycemic effect of mianserin remain to be elucidated.

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“…Indeed, the antidepressant effect of mianserin is considered to mainly derive from the blockade of pre‐synaptic, auto‐ and hetero‐α 2 ‐adrenoceptors, with the consequent increase of noradrenergic and 5‐hydroxytryptaminergic neurotransmission (Marshall, 1983; Pinder, 1985). However, like TCAs, mianserin has been reported to produce analgesia that was blocked by opioid antagonists, indicating that also this antidepressant acts through the opioid system (Reichenberg et al ., 1985; Schreiber et al ., 1998). Moreover, mianserin has been shown to either potentiate or antagonize the analgesic effect of the selective κ‐opioid receptor agonist U‐50 488 (Ho and Takemori, 1989).…”

Section: Introductionmentioning

confidence: 99%

The atypical antidepressant mianserin exhibits agonist activity at κ‐opioid receptors

Olianas

Dedoni

Onali

2012

British J Pharmacology

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BACKGROUND AND PURPOSEAntidepressants are known to interact with the opioid system through mechanisms not completely understood. We previously reported that tricyclic antidepressants act as agonists at distinct opioid receptors. Here, we investigated the effect of the atypical antidepressant mianserin at cloned and native opioid receptors. EXPERIMENTAL APPROACHEffects of mianserin were examined in CHO cells transfected with human opioid receptors, C6 glioma cells and rat brain membranes by the use of radioligand binding and functional assays including the stimulation of [ KEY RESULTSMianserin displayed 12-and 18-fold higher affinity for k-than m-and d-opioid receptors respectively. In [ 35 S]GTPgS assays, mianserin selectively activated k-opioid receptors. The agonist activity was antagonized by the selective k-opioid blocker nor-binaltorphimine (nor-BNI). The mianserin analogue mirtazapine also displayed k-opioid agonist activity. Mianserin and mirtazapine increased ERK1/2 phosphorylation in CHO cells expressing k-opioid receptors and C6 cells, and these effects were antagonized by nor-BNI. In rat striatum and nucleus accumbens, mianserin stimulated [35S]GTPgS binding in a nor-BNI-sensitive manner with maximal effects lower than those of the full k-opioid agonists (-)-U50,488 and dynorphin A. When combined, mianserin antagonized the effects of the full k-opioid receptor agonists in [ CONCLUSIONS AND IMPLICATIONSIn different cell systems, mianserin directly activates k-opioid receptors, displaying partial agonist activity at brain receptors. Thus, this property appears to be a common feature of different classes of antidepressants.

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Interaction between the tetracyclic antidepressant mianserin HCl and opioid receptors

Cited by 23 publications

References 21 publications

Opioid Receptors Contribute to Antinociceptive Effect of Tianeptine on Colorectal Distension-Induced Visceral Pain in Rats

Opioid Receptors Contribute to Antinociceptive Effect of Tianeptine on Colorectal Distension-Induced Visceral Pain in Rats

Mianserin’in sıçanlarda streptozotosin ile indüklenen hiperglisemi ve metabolik değişiklikler üzerine etkisi

The atypical antidepressant mianserin exhibits agonist activity at κ‐opioid receptors

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