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Serotonin receptors and site-selective agents

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Gelennon R. A.

Journal of Physiology and Pharmacology

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1991

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tom 42

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nr 1

Few site-selective serotonergic agents are currently available; in fact, most of these agents might more appropriately be termed semi-selective in that they typically bind to at least two different populations of serotonin receptors. We describe the application of structure-affinity relationship (SAFIR) studies to the development of high- affinity and/or site-selective serotonergic agents; examples are provided from work conducted in our laboratories. Also discussed is the concept of selectively non-selective agents and their potential preclinical and clinical utility. A case is made for development of selective and nonselective serotonergic agents.

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Involvement of some 5-HT receptors in methamphetamine-induced locomotor activity in mice

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Ginawi O. T., Al-Majed A. A., Al-Suwailem A. K., El-Hadiyah T. M. H.

Journal of Physiology and Pharmacology

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2004

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tom 55

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nr 2

Effects of some selective 5-HT antagonists on methamphetamine-induced locomotor activity were investigated in male mice in order to study whether this effect of methamphetamine is selectively or at least partially, induced through stimulation of a specific serotonin receptor subtype. Methamphetamine (1.5mg/kg, IP) produced a significant increase in locomotor activity. Methamphetamine-induced hyperactivity by the above mentioned dose was signficantly antagonized by NAN-190 ( 5-HT1A antagonist) at a dose of 4 mg/kg, IP, methiothepin (5-HT1B/1D antagonist) at a dose of 0.1mg/kg, IP or mianserin ( 5-HT2C antagonist) at a dose of 8mg/kg, IP. On the other hand, methysergide ( 5-HT 2A/2B antagonist) at a dose of 1mg/kg, IP or ondansetron ( 5-HT3 antagonist) at a dose of 0.5mg/kg, IP potentiated the methamphetamine-induced hyperactivity. None of the above mentioned doses of 5-HT antagonists altered the spontaneous activity of mice when administered alone. The results of the present study indicate a possible role for serotonergic mechanisms, in addition to the catecholaminergic systems, in the locomotor stimulant activity of methamphetamine in mice. This role is possibly mediated through direct stimulation of some 5-HT receptor subtypes. Stimulation by methamphetamine of 5-HT 1A, 5-HT 1B/1D and/or 5-HT2C receptor subtypes may result in hyperactivity, whereas stimulation by methamphetamine of 5-HT 2A/2B and/or 5-HT3 receptor subtypes may result in decreased activity.

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Endogenous systems involved in exercise-induced analgesia

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Da Silva Santos R., Galdino G.

Journal of Physiology and Pharmacology

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2018

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tom 69

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nr 1

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Fear behavior and regional brain monoamines distribution after R[plus]-8-OHDPAT and R[plus]-UH-301 injections into the dorsal raphe nucleus in rats

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Koprowska M., Krotewicz M., Romaniuk A., Strzelczuk M., Wieczorek M.

Acta Neurobiologiae Experimentalis

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2002

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tom 62

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nr 2

Ograniczanie wyników

3 Journal of Physiology and Pharmacology

1 Acta Neurobiologiae Experimentalis

1 Al-Majed A. A.

1 Al-Suwailem A. K.

1 Da Silva Santos R.

1 El-Hadiyah T. M. H.

1 Galdino G.

1 Gelennon R. A.

1 Ginawi O. T.

1 Koprowska M.

1 Krotewicz M.

1 Romaniuk A.

1 Strzelczuk M.

1 Wieczorek M.

1 2018

1 2004

1 2002

1 1991

Serotonin receptors and site-selective agents

Involvement of some 5-HT receptors in methamphetamine-induced locomotor activity in mice

Endogenous systems involved in exercise-induced analgesia

Fear behavior and regional brain monoamines distribution after R[plus]-8-OHDPAT and R[plus]-UH-301 injections into the dorsal raphe nucleus in rats