5-Hydroxytryptamine receptors 5-HTia

Another type of anxiolytic is buspirone, which appears to work principally as a partial agonist at 5-HTia receptors (see 5-HYDROXYTRYPTAMINE receptor agonists). Examples under development include tandospirone, zalospirone and zolmitriptan. 

U 8344) is derived from mustine, and is an alkylating anti-CANCER AGENT used orally to treat lymphomas and leukaemias, urapidil [ban.inn.jan] is a novel piperazinyl pyrimidinedione derivative with mixed ( i-subtype) a-ADRENOCEPTOR ANTAGONIST, CNS and (5-HTia) 5-HYDROXYTRYPTAMINE RECEPTOR ANTAGONIST properties. It has been used as an antihypertensive. urea [usan] (carbamide) is a constituent of ail vertebrate tissues, concentrated in urine. It can be used topically as a... 

In a series of studies, Markou and her colleagues have sought to identify drugs that ameliorate the changes in brain reward function evoked by nicotine withdrawal (see Kenny and Markon 2001 for review). This review snmmarises the evidence that 5-hydroxytryptamine (5-HT) and, especially, 5-HTia receptors may play an important role in nicotine withdrawal, although the specific nature of the changes evoked... 

Assie M-B, Koek W. Effects of 5-HTia receptor antagonists on hippocampal 5-hydroxytryptamine levels (S)-WAY100135, but not WAY100635, has partial agonist properties. Eur J Pharmacol 1996 304 15-21. 

Serotonin (5-hydroxytryptamine, 5-HT) occurs in the intestinal wall, where it regulates motility and secretion in blood platelets, where it modulates platelet aggregation and vascular blood flow and in the CNS, where it acts as a neurotransmitter in areas of the midbrain. At least seven different receptors for serotonin have been characterized, which mediate a wide variety of different physiological effects. Depression and anxiety are thought to be the result of actions on 5-HTia receptors in the brain limbic system. Following release from neurons by a depolarizing action potential at central synapses, the activity of 5-HT is terminated by neuronal reuptake. This is performed by a synaptic membrane amine transporter protein, specific for 5-HT, which also co-transports sodium and chloride ions to repolarize the neuronal membrane. 

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