Table 6.2. Serotonin receptor subtypes and disease states
Physiological or pathological condition
Serotonin receptor subtype implicated
Feeding behaviour Thermoregulation Sexual behaviour Cardiovascular system Sleep
Hallucinogenic activity Antipsychotic activity
Anxiolytic activity Depression
5-HT1A agonists enhance food consumption in experimental animals
5-HT1B/5-HT2C agonists decrease food consumption in experimental animals
5-HT1A agonists cause hypothermia in experimental animals
5-HT1B and 5-HT2 agonists cause hyperthermia in experimental animals
5-HT1A agonists both facilitate and inhibit sexual behaviour in male rats
5-HT1B agonists inhibit sexual behaviour in the male but facilitate this behaviour in the female rat 5-HT1, 5-HT2 and 5-HT3 receptors may be involved in the complex action of serotonin on blood pressure 5-HT2 agonists appear to be hypertensive agents whereas the antagonists are hypotensives 5-HT1A agonists delay the onset of REM sleep 5-HT2 antagonists suppress REM sleep Most "classical" hallucinogens such as LSD and mescaline are antagonists at 5-HT2 receptors Many atypical neuroleptics (e.g. amperozide and risperidone) are 5-HT2 receptor antagonists. In animals, 5-HT3 antagonists have profiles similar to chronically active neuroleptics
Several novel anxiolytics (e.g. buspirone, ipsapirone) are 5-HT1A partial agonists
5-HT2 and 5-HT3 antagonists have anxiolytic properties 5-HT1A receptors are functionally sensitized by chronic antidepressant treatments in rats 5-HT2 receptor numbers are increased and activity decreased, in depression; return to control values in response to treatment
Nevertheless, despite these cautions, there is a growing body of information which implicates different 5-HT receptor subtypes in a variety of physiological and pharmacological responses and these will be briefly reviewed (see Table 6.2).
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