Psychopharmacology of 5-HT(1A) receptors.
Serotonin(1A) (5-HT(1A)) receptors are located on both 5-HT cell bodies where they act as inhibitory autoreceptors and at postsynaptic sites where they mediate the effects of 5-HT released from nerve terminals. The sensitivity of 5-HT(1A) receptors in humans can be measured using the technique of pharmacological challenge. For example, acute administration of a selective 5-HT(1A) receptor agonist, such as ipsapirone, decreases body temperature and increases plasma cortisol through activation of pre- and postsynaptic 5-HT(1A) receptors, respectively. Use of this technique has demonstrated that unmedicated patients with major depression have decreased sensitivity of both pre- and postsynaptic 5-HT(1A) receptors. Treatment with selective serotonin reuptake inhibitors further down-regulates 5-HT(1A) receptor activity. Due to the hypotheses linking decreased sensitivity of 5-HT(1A) autoreceptors with the onset of antidepressant activity, there is current interest in the therapeutic efficacy of combined treatment with selective serotonin reuptake inhibitors and 5-HT(1A) receptor antagonists.
Cowen
P J
PJ
University Department of Psychiatry, Warneford Hospital, Oxford OX3 7JX, United Kingdom.
D000818:Animals; D003863:Depression / Q000378:metabolism; D006801:Humans; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000502:physiology; D044263:Receptors, Serotonin, 5-HT1; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology
D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D017367:Selective Serotonin Reuptake Inhibitors