5-hydroxytryptamine type 3 receptor

Muller C, Pongratz S, Pidlich J, et al. (1998) Treatment of pruritus in chronic liver disease with the 5-hydroxytryptamine receptor type 3 antagonist ondansetron A randomized, placebo-controlled, double-blind cross-over trial. Eur Gastroenterol Hepatol 10 865-870. 

FIGURE 18.4 Pharmacologist s view of emetic stimuli. Myriad signaling pathways lead from the periphery to the emetic center. Stimulants of these pathways are noted in italics. These pathways involve specific neurotransmitters and their receptors (bold text). Receptors are shown for dopamine, D acetylcholine (muscarinic), M histamine, H and 5-hydroxytryptamine, 5-HT. Some of these receptor types also may mediate signaling in the emetic center. This knowledge offers a rationale for current antiemetic therapy. 

The first of at least 14 serotonin (5-hydroxytryptamine [5-HT]) receptor types currently known to exist in the mammalian central nervous system (CNS) was pharmacologically defined more than 25 yr ago (1,2). Yet, it is only within the last 15 yr, with the cloning and sequencing of these receptors, that it has become possible to visualize their distribution at cellular and subcellular... 

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. 

Fluorescent ligands for adenosine receptors 13BML26. 5-Hydroxytryptamine sub-type 6 receptor modulators 12ETP1123. Medicinal chemistry of A3 adenosine receptor modulators Pharmacological activities and therapeutic implications 12JMC5676. 

Monoester 4-(methoxycarbonyl)bicyclo[2.2.1]heptane-l-carboxylic acid 59 (Figure 4.17) is a building block of many potential therapeutic candidates for inhibitors of 11-p-hydroxysteroid dehydrogenase type 1 enzyme and their use in the treatment of non-insulin-dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and CNS disorders. It is also required for the synthesis of 5-hydroxytryptamine receptor agonists, useful for the treatment of anxiety disorders and schizophrenia [90,91]. 

Beginning in the 1960s, ben2odia2epiae anxiolytics and hypnotics rapidly became the standard prescription dmg treatment. In the 1980s, buspkone [36505-84-7] (3), which acts as a partial agonist at the serotonin [50-67-9] (5-hydroxytryptamine, 5-HT) type lA receptor, was approved as treatment for generali2ed anxiety. More recently, selective serotonin reuptake inhibitors (SSRIs) have been approved for therapy of panic disorder and obsessive—compulsive behavior. 

List of Abbreviations RNA, ribonucleic acid nAChR, nicotinic acetylcholine receptor GABAa, y-amino-butyric type A 5-HT3, 5-hydroxytryptamine type 3... 

Peters JA, Garland JE, Cooper MA, Livesey MR, Deeb TZ, Hales TG, Lambert JJ (2006) Novel structural determinants of single-channel conductance in nicotinic acetylcholine and 5-hydroxytryptamine type-3 receptors. Biochem Soc Trans 34(5) 882-886 Picciotto MR, Zoli M, Rimondini R, Lena C, Marubio LM, Pich EM, Fuxe K, Changeux JP (1998) Acetylcholine receptors containing the beta2 subunit are involved in the reinforcing properties of nicotine. Nature 391 173-177... 

Serotonin (5-hydroxytryptamine 5-HT) acts as transmitter and mediator on several locations in the body with quite different effects. There are multiple sub-types of the serotonin receptor. This offers the possibility of a selective therapeutic interference using subtype specific agonists or antagonists. 

Presynaptic receptor that is activated by a neurotransmitter from an adjacent neuron the type of neurotransmitter activating the heteroceptor differs from that released from the axon. 5-Hydroxyindoleacetic acid, the main metabolite of 5-hydroxytryptamine (serotonin) formed by monoamine oxidase. 

Mayer SE, Sanders-Bush E. 5-Hydroxytryptamine type 2A and 2C receptors linked to Na+/K+/Cl cotransport. Mol Pharmacol 1994 45 991-996. 

Becamel C, Figge A, Poliak S, et al. Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1. J Biol Chem 2001 276 12,974-12,982. 

Torres GE, Chaput Y, Andrade R. Cyclic AMP and protein kinase A mediate 5-hydroxytryptamine type 4 receptor regulation of calcium-activated potassium current in adult hippocampal neurons. Mol Pharmacol 1995 47 191-197. 

Baker LP, Nielsen MD, Impey S, et al. Stimulation of type 1 and type 8 Ca2+/ calmodulin-sensitive adenylyl cyclases by the Gs coupled 5-hydroxytryptamine subtype 5-HT7A receptor. J Biol Chem 1998 273 17,469-17,476. 

Gray JA, Sheffler DJ, Bhatnagar A, et al. Cell-type specific effects of endocytosis inhibitors on 5-hydroxytryptamine(2A) receptor desensitization and resensiti-zation reveal an arrestin-, GRK2-, and GRK5-independent mode of regulation in human embryonic kidney 293 cells. Mol Pharmacol 2001 60 1020-1030. 

Belelli D, Balcarek JM, Hope AG, Peters JA, Lambert JJ, Blackburn TP. Cloning and functional expression of a human 5-hydroxytryptamine type 3A(S) receptor subunit. Mol Pharmacol 1995 48 1054-1062. 

Parsons MJ, D Souza UM, Arranz MJ, Kerwin RW, Makoff AJ. The -1438A/G polymorphism in the 5-hydroxytryptamine type 2A receptor gene affects promoter activity. Biol Psychiatry 2004 56(6) 406-410. 

Schworer, H., Hartmann, H., Ramadori, G. Relief of cholestatic pruritus by a novel class of drugs 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist effectiveness of ondansetron. Pain 1995 61 31-37... 

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