5- Hydroxytryptamine agonists

Caccia S, Ballabio M, Samanin R, et al. (-)-m-Chlorophenyl-piperazine, a central 5-hydroxytryptamine agonist, is a metabolite of trazodone. J Pharm Pharmacol 1981 33 477-478. 

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. 

Some derivatives of adamantane with antagonist or agonist effects have also been synthesized. For instance, monocationic and dicationic adamantane derivatives block the a-amino-3-hydroxy-5-methylisoxazole -propionic acid (AMPA) receptors, A-methyl-o-aspartate (NMDA) receptors [134—136] and 5-hydroxytryptamine (5-HT3) receptors [137]. 

FDA, Combined Use of 5-Hydroxytryptamine Receptor Agonists (Triptans), Selective Serotonin Reuptake Inhibitors (SSRIs) or Selective Serotonin/Norepinephrine Reuptake Inhibitors (SNRIs) May Result in Life-Threatening Serotonin Syndrome , FDA Public Health Advisory (2006) http //www.fda.gov/Cder/Drug/advisory/ S SRI S S200607.htm... 

Cowen, P. J., Grahame-Smith, D. G., Green, A. R., and Heal, D. J. (1982) Beta-adrenoceptor agonists enhance 5-hydroxytryptamine-mediated behavioural responses. Br. J. Pharmacol.. 76 265-270. 

Hole, K., Jonsson, G., and Berge, O. (1977) 5,7-Dihydroxytryptamine lesions of ascending 5-hydroxytryptamine pathways Habituation, motor activity and agonistic behavior. Pharmacol. Biochem. Behav., 7 205-210. 

The pathology of Parkinson s disease is associated with a substantial reduction in neurotransmitters such as dopamine, 5-hydroxytryptamine, GABA, in the brain. Treatment is based on the use of replacement of dopamine or dopamine agonists which relieve the rigidity but do not affect a cure. Currently, there is no laboratory-based diagnostic test for PD and so diagnosis is based on clinical presentation alone. 

Pharmacology Naratriptan, rizatriptan, sumatriptan, frovatriptan, almotriptan, eletriptan, and zolmitriptan are selective agonists for a vascular 5-hydroxytryptamine-i(serotonin) receptor subtype. Use of 5-HT- agonists results in... 

A life-threatening condition, when selective serotonin reuptake inhibitors (SSRIs) and 5-hydroxytryptamine receptor agonists (triptans) are used together. However, many other drugs have been implicated (see below). Signs and symptoms of serotonin syndrome include the following ... 

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. 

To date, the only serotonergic agonist that was associated with the provocation of brief exacerbations of OCD symptoms in some studies is mCPP, which possesses only weak affinity for dopamine, acetylcholine, and a,-adrenergic and (i-adrenergic receptors [Hamik and Peroutka 1989). The agonistic activity of mCPP is greatest for the 5-hydroxytryptamine [5-HT serotonin] S-HTjc and S-HTj receptor subtypes and to a lesser extent to the 5-HT, and 5-HTjp subtypes [Barr et al. 1992]. 

Meller E, Goldstein M, Geyer MA Receptor reserve for 5-hydroxytryptamine lA-mediated inhibition of serotonin synthesis possible relationship to anxiolytic properties of 5-hydroxitryptamine lA agonists. Mol Pharmacol 37 231-237, 1990... 

Quercetin also inhibited rat aortic contractions induced by noradrenaline, 5-hydroxytryptamine, and caffeine in Ca2+ -free media [110]. PMA enhanced this transient contraction elicited by noradrenaline, an effect that was abolished by quercetin. Furthermore, quercetin or the PKC inhibitor staurosporine, had no effect on 45Ca2+ efflux under resting conditions or when stimulated by noradrenaline. So, the inhibitory effects of quercetin on phasic contractile response induced by receptor agonists in... 

Shapiro, D. A., Kristiansen, K., Weiner, D. M., Kroeze, W. K., and Roth, B. L. (2002). Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2a serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6./. Biol. Chem. 277, 11441-11449. 

Yokoo H, Goldstein M, Meller E (1988) Receptor reserve at striatal dopamine receptors modulating the release of [3H] dopamine. Eur J Pharmacol 155 323-7 Yokoyama H, Onodera K, Maeyama K, Sakurai E, Iinuma K, Leurs R, Timmerman H, Watanabe T (1994) Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur J Pharmacol 260 23-8 Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006) Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus. Proc Natl Acad Sci USA, in press Young CS, Mason R, Hill SJ (1988) Studies on the mechanism of histamine-induced release of noradrenaline and 5-hydroxytryptamine from slices of rat cerebral cortex. Biochem Pharmacol 37 2799-2805... 

GOthert M, Duhrsen U (1979) Effects of 5-hydroxytryptamine and related compounds on the sympathetic nerves of the rabbit heart. Naunyn Schmiedebergs Arch Pharmacol 308 9-18 Gotti C, Zoli M, Clementi F (2006) Brain nicotinic acetylcholine receptors native subtypes and their relevance. Trends Pharmacol Sci 27 482-91 Grady SR, Meinerz NM, Cao J, Reynolds AM, Picciotto MR, Changeux JP, McIntosh JM, Marks MJ, Collins AC (2001) Nicotinic agonists stimulate acetylcholine release from mouse interpeduncular nucleus a function mediated by a different nAChR than dopamine release from striatum. J Neurochem 76 258-68... 

Rauser L, Savage JE, Meltzer HY, Roth BL. Inverse agonist actions of typical and atypical antipsychotic drags at the human 5-hydroxytryptamine(2C) receptor. J Pharmacol Exp Ther 2001 299 83-89. 

Shapiro DA, Kristiansen K, Kroeze WK, Roth BL. Differential modes of agonist binding to 5-hydroxytryptamine(2A) serotonin receptors revealed by mutation and molecular modeling of conserved residues in transmembrane region 5. Mol Pharmacol 2000 58 877-886. 

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