Chronic alnespirone-induced desensitization of somatodendritic 5-HT1A autoreceptors in the rat dorsal raphe nucleus
| Autor: | Elisabeth Mocaer, N Laaris, Laurence Lanfumey, Emmanuel Le Poul, Claude-Michèle Fattaccini, Michel Hamon, E. Doucet |
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| Rok vydání: | 1999 |
| Předmět: |
Male
Agonist medicine.medical_specialty Time Factors medicine.drug_class Stimulation Rats Sprague-Dawley chemistry.chemical_compound Dorsal raphe nucleus Internal medicine polycyclic compounds medicine Animals Alnespirone Receptor Serotonin 5-HT2A Spiro Compounds heterocyclic compounds Receptor 5-HT receptor Pharmacology Binding Sites Behavior Animal Dose-Response Relationship Drug musculoskeletal neural and ocular physiology Body Weight Rats Serotonin Receptor Agonists Endocrinology nervous system chemistry Receptors Serotonin Autoreceptor Autoradiography Raphe Nuclei Receptors Serotonin 5-HT3 Raphe nuclei Receptors Serotonin 5-HT1 |
| Zdroj: | European Journal of Pharmacology. 365:165-173 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/s0014-2999(98)00886-3 |
| Popis: | The effects of long-term (7, 14 or 21 days) administration of the 5-HT1A receptor agonist alnespirone [5 mg/(kg day), i.p.] on the binding characteristics of 5-HT1A, 5-HT2A and 5-HT3 receptors, and the functional status of 5-HT1A autoreceptors were assessed using biochemical and electrophysiological approaches in rats. Whatever the treatment duration, the specific binding of [3H]8 hydroxy-2-(di-n-propylamino)tetralin ([3H]8-OH-DPAT), [3H]trans,4-[(3Z)3-(2-dimethylaminoethyl) oxyimino-3(2-fluorophenyl) propen-1-yl] phenol hemifumarate ([3H]SR 46349B), and [3H]S-zacopride to 5-HT1A, 5-HT2A and 5-HT3 receptors, respectively, were unaltered in all the brain areas examined. In contrast, in vitro electrophysiological recordings performed 24 h after the last injection of alnespirone showed that the potency of the 5-HT1A receptor agonist, 8-OH-DPAT, to depress the firing of serotoninergic neurons in the dorsal raphe nucleus, was significantly reduced after a 21-day treatment with alnespirone. However, no changes were noted after a 7-day or 14-day treatment. These data indicate that desensitization of somatodendritic 5-HT1A autoreceptors is a selective but slowly developing adaptive phenomenon in response to their chronic stimulation in rats. |
| Databáze: | OpenAIRE |
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