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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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Blockade of 5-HT1A receptors in the phrenic nucleus of the rat attenuated raphe induced activation of the phrenic nerve activity

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Pecotic R., Dogas Z., Valic Z., Valic M.
Journal of Physiology and Pharmacology
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2009
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tom 60
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nr 3
167-172
Stimulation of the raphe pallidus nucleus produces facilitatory effects on respiratory activity. Numerous serotonergic projections from the raphe pallidus have been shown to terminate in the phrenic nucleus. This study was undertaken to examine the role of 5-hydroxytryptamine 1A (5-HT1A) receptors in the phrenic nucleus on the excitatory response of the phrenic nerve activity elicited from the raphe pallidus. We hypothesized that blockade of 5-HT1A receptors in the phrenic nucleus will attenuate raphe-induced facilitation of the phrenic nerve. Chemical stimulation of the raphe pallidus by synaptic excitant D,L-homocysteic acid produced increase in the amplitude of the phrenic nerve activity. After microinjection of the specific 5-HT1A receptor antagonist WAY, N-(2-(4,2-methoxyphenyl)-1-piperazinyl)ethyl)-N-2-pyridinyl-cyclohexane-carboxamide maleate into the phrenic nucleus, the raphe-induced facilitation of the phrenic nerve was attenuated. These data suggest that excitation of the phrenic nerve activity elicited by activation of the neurons in the raphe pallidus is mediated by 5-HT1A receptors in the phrenic nucleus.
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Phrenic nerve activity is enhanced by 5-HT1A receptor agonist 8-OH-DPAT in spontaneously breathing anesthetized rats

100%
Valic M., Pecotic R., Dogas Z.
Journal of Physiology and Pharmacology
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2008
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tom 59
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nr 1
Activation of serotonin 1A (5-HT1A) receptors has been shown to have diverse effects on respiration. The purpose of this study was to determine changes in respiratory motor pattern of phrenic nerve activity and respiratory rhythm after systemic application of specific 5-HT1A receptor agonist 8-hydroxy-2-di-n-propylamino-tetralin (8-OH-DPAT). We hypothesized that systemic application of specific 5-HT1A receptor agonist 8-OH-DPAT in spontaneously breathing anaesthetized rats will enhance phrenic motor output and phrenic respiratory rate. The study was performed in spontaneously breathing urethane anesthetized rats. Intravenous application of 8-OH-DPAT produced dose dependent increase in the amplitude of integrated phrenic nerve activity and disturbances in respiratory rhythm. Stimulating effect of 8-OH-DPAT on phrenic nerve activity was abolished by intravenous application of the selective 5-HT1A receptor antagonist WAY, N-(2-(4,2-methoxyphenyl)-1-piperazinyl)ethyl)-N-2-pyridinyl-cyclohexane-carboxamide maleate (WAY-100635). These results show that stimulation of 5-HT1A receptors by intravenous application of 8-OH-DPAT enhances phrenic nerve activity in spontaneously breathing rats.
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A search for colocalization of serotonin 5-HT2A and 5-HT1A receptors in the rat medial prefrontal and entorhinal cortices-immunohistochemical studies

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Wedzony K., Chocyk A., Mackowiak M.
Journal of Physiology and Pharmacology
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2008
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tom 59
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nr 2
Recently developed antipsychotic drugs ameliorating the negative symptoms of schizophrenia act not only on dopamine D2 receptors but also on serotonin 2A (5-HT2A) and 1A (5-HT1A) receptors in specific regions of the cerebral cortex. Since it is not yet known whether serotonin 5-HT1A and 5-HT2A receptors coexist in the same population of neurons in the cortex, the present study investigated their colocalization in the rat medial prefrontal (MPC) and entorhinal (EC) cortices. Using antibodies that recognize epitopes specific to the serotonin 5-HT2A or 5-HT1A receptors, studies employing confocal microscopy have shown that in the MPC 5-HT2A receptors are preferentially, if not exclusively, present on the pyramidal neurons and that 5-HT1A-immunopositive material is present in the axonal hillocks and, to lower extend, in cytoplasm of presumably pyramidal cell bodies. With the regard of labeling of active receptors (i.e. present in shafts and axonal hillocks) we found that about 38% of neurons positive for the presence of serotonin 5-HT2A receptors, are also positive for serotonin 5-HT1A receptors in the MPC. In the EC, only 22% of serotonin 5-HT2A-positive neurons were positive for serotonin 5-HT1A receptor-immunoreactivity. In the respect of cytoplasmatic serotonin 5-HT1A receptor-immunoreactivity (possibly inactive receptors), 65% and 73% of serotonin 5-HT2A receptor-positive neurons were colocalized with serotonin 5-HT1A receptors in the MPC and EC, respectively. Data obtained on serotonin 5-HT2A and 5-HT1A receptor localization provide anatomical grounds for at least three distinct populations of pyramidal neurons, one governed only by 5-HT2A, one only by 5-HT1A and one by both types of serotonin receptors.
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The role of serotonergic 5-HT1A receptors in central cardiovascular regulation in hemorrhagic shock in rats

84%
Sowa P., Adamczyk-Sowa M., Zwirska-Korczala K., Namyslowski G., Misiolek M., Pierzchala K.
Journal of Physiology and Pharmacology
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2013
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tom 64
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nr 2
6
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Proopiomelanocortin but not vasopressin or renin-angiotensin system induces resuscitative effects of central 5-HT1A activation in haemorrhagic shock in rats

84%
Sowa P., Adamczyk-Sowa M., Zwirska-Korczala K., Pierzchala K., Adamczyk D., Paluch Z., Misiolek M.
Journal of Physiology and Pharmacology
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2014
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tom 65
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nr 5
7
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Expression of 5-HT1A and 5-HT7 receptors in Caco-2 cells and their role in the regulation of serotonin transporter activity

84%
Iceta R., Mesonero J. E., Aramayona J. J., Alcalde A. I.
Journal of Physiology and Pharmacology
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2009
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tom 60
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nr 1
157-164
Serotonin (5-HT) receptors are expressed in the gastrointestinal tract and play an important role in gastrointestinal activity regulation. 5-HT binding to receptors depends on 5-HT availability, which is, in part, modulated by the 5-HT transporter (SERT) expressed in enterocytes. This work concerns the expression of 5-HT1A and 5-HT7 receptors (5-HTR1A and 5-HTR7) in the human enterocyte-like Caco-2 cell line and their role in SERT activity modulation. The results demonstrate the mRNA and protein expression of 5-HTR1A and 5-HTR7 in these cells. In addition, both receptors are shown to modulate SERT activity; 5-HTR1A activation increased 5-HT uptake and 5-HTR7 activation inhibited it. In both cases, SERT modulation might involve a cAMP/PKA pathway. Effects on SERT disappeared after long-term activation of 5-HTR1A and 5-HTR7, indicating their desensitization. However, in both cases, the desensitization did not show itself to be mediated by a reduction of the amount of receptors in the membrane.
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Imipramine and citalopram reverse corticosterone-induced alterations in the effects of the activation of 5-HT1A and 5-HT2 receptors in rat frontal cortex

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Zahorodna A., Hess G.
Journal of Physiology and Pharmacology
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2006
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tom 57
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nr 3
Using extracellular recording we studied changes in the reactivity of rat frontal cortical slices to the 5-HT1A, 5-HT2 and 5-HT4 receptor agonists, (±)-2-dipropyloamino-8-hydroxy-1,2,3,4-tetrahydronaphtalene hydrobromide (8-OH-DPAT), (±)-2,5-dimethoxy-4-iodoamphetamine hydrochloride (DOI) and zacopride, respectively, induced by an earlier treatment of animals with corticosterone lasting 1 or 3 weeks. Spontaneous bursting activity was recorded in ex vivo slices incubated in a medium devoid of Mg2+ ions and containing picrotoxin (30 µM). Repetitive, but not single, corticosterone administration resulted in an attenuation of the effect of the activation of 5-HT1A receptors and in an enhancement of the effect related to 5-HT2 receptors. The effect of 5-HT4 receptor activation remained unchanged. In separate two sets of experiments rats were treated with corticosterone for 3 weeks and additionally with imipramine or citalopram, beginning on the eighth day of corticosterone administration. In the corticosterone plus imipramine as well as corticosterone plus citalopram groups the effects of 8-OH-DPAT and DOI were not different from control indicating that corticosterone-induced functional modifications in the reactivity of 5-HT1A and 5-HT2 receptors were reversed by antidepressant treatments.
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Glutamatergic neurons of rat medial prefrontal cortex innervating the ventral tegmental area are positive for serotonin 5-HT1A receptor protein

84%
Wedzony K., Chocyk A., Kolasiewicz W., Mackowiak M.
Journal of Physiology and Pharmacology
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2007
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tom 58
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nr 4
The present study was designed to investigate whether serotonin 5-HT1A receptor protein (5-HT1A receptor-immunoreactivity), is present on cortical pyramidal neurons of the rat medial prefrontal cortex (MPC) innervating the ventral tegmental area (VTA). Recent data stress the role of serotonin 5-HT1A receptors in the pathology of schizophrenia, and in the mechanism of action of novel antipsychotic drugs. It was found that approximately 52% of cells in layers II/III of the MPC whose axons initial segments were immunoreactive for serotonin 5HT1A receptor were also labeled with Fluoro-Gold (FG), a retrograde tracer injected into the VTA, indicating that certain portion of neurons forming glutamatergic innervations of the VTA may be controlled by serotonin 5-HT1A receptors. In deep cortical layers (V/VI) retrogradely labeled neurons never colocalized with serotonin 5-HT1A receptor-mmunoreactivity. These anatomical data indicate that serotonin 5-HT1A receptors might potentially control the excitability and propagation of information transmitted by the pyramidal cells to the VTA. Moreover, our results indicate that the drugs operating via serotonin 5-HT1A receptors in the MPC, might control from this level the release of glutamate in the VTA and restore function of glutamate neurotransmission, whose dysfunction is observed for example in schizophrenia.
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The influence of repeated administration of clozapine and haloperidol on the effects of the activation of 5-HT1A, 5-HT2 and 5-HT4 receptors in rat frontal cortex

84%
Zahorodna A., Bobula B., Grzegorzewska M., Tokarski K., Hess G.
Journal of Physiology and Pharmacology
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2004
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tom 55
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nr 2
The effects of a repeated treatment with antipsychotic drugs, clozapine and haloperidol, on the modulation of network activity ex vivo by 5-HT receptors were examined in rat frontal cortical slices using extracellular recording. Rats were treated for 21 days with clozapine (30 mg/kg p.o.), or haloperidol (1 mg/kg p.o.). Spontaneous bursting activity was induced in slices prepared 3 days after the last drug administration by perfusion with a medium devoid of Mg2+ ions and with added picrotoxin (30 mM). The application of 2-3 µM 8-OH-DPAT, acting through 5-HT1A receptors, resulted in a reversible decrease of bursting frequency. In the presence of 1 µM DOI, the 5-HT2 agonist, or 5 µM zacopride, the 5-HT4 agonist, bursting frequency increased. Chronic clozapine treatment resulted in an attenuation of the effect of the activation of 5-HT2 receptors, while the effects related to 5-HT1A and 5-HT4 receptor activation were unchanged. Treatment with haloperidol did not influence the reactivity to the activation of any of the three 5-HT receptor subtypes. These data are consistent with earlier findings demonstrating a selective downregulation of 5-HT2A receptors by clozapine and indicate that chronic clozapine selectively attenuates the 5-HT-mediated excitation in neuronal circuitry of the frontal cortex while leaving the 5-HT-mediated inhibition intact.
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