Serotonin receptor subtypes and disease states
Physiological or pathological -- condition Serotonin receptor subtype implicated
Feeding behaviour: 5-HT1A agonists enhance food consumption in experimental animals
5-HT1B/5-HT2C agonists decrease food consumption in experimental animals
Thermoregulation: 5-HT1A agonists cause hypothermia in experimental animals
5-HT1B and 5-HT2 agonists cause hyperthermia in experimental animals
Sexual behaviour: 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 Cardiovascular system: 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
Sleep: 5-HT1A agonists delay the onset of REM sleep
5-HT2 antagonists suppress REM sleep
Hallucinogenic activity: Most ‘‘classical’’ hallucinogens such as LSD and mescaline are antagonists at 5-HT2 receptors
Antipsychotic activity: 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
Anxiolytic activity: Several novel anxiolytics (e.g. buspirone, ipsapirone) are
5-HT1A partial agonists
5-HT2 and 5-HT3 antagonists have anxiolytic properties
Depression: 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
Physiological or pathological -- condition Serotonin receptor subtype implicated
Feeding behaviour: 5-HT1A agonists enhance food consumption in experimental animals
5-HT1B/5-HT2C agonists decrease food consumption in experimental animals
Thermoregulation: 5-HT1A agonists cause hypothermia in experimental animals
5-HT1B and 5-HT2 agonists cause hyperthermia in experimental animals
Sexual behaviour: 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 Cardiovascular system: 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
Sleep: 5-HT1A agonists delay the onset of REM sleep
5-HT2 antagonists suppress REM sleep
Hallucinogenic activity: Most ‘‘classical’’ hallucinogens such as LSD and mescaline are antagonists at 5-HT2 receptors
Antipsychotic activity: 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
Anxiolytic activity: Several novel anxiolytics (e.g. buspirone, ipsapirone) are
5-HT1A partial agonists
5-HT2 and 5-HT3 antagonists have anxiolytic properties
Depression: 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
