5-Hydroxytryptamine receptor antagonist

Key Words 5-Hydroxytryptamine serotonin receptor antagonist knockout autoradiography thermoregulation hippocampus behavior electrophysiology depression oleamide. 

King FD. 5-Hydroxytryptamine-3-receptor antagonists King FD, Jones BJ, Sanger GJ, eds. CRC Boca Raton FLA 1994 1-44. 

Navari RM, Koeller JM. Comment electrocardiographic and cardiovascular effects of the 5-hydroxytryptamine-3 receptor antagonists. Authors reply. Arm Pharmaco r (2003) 37, 1918-19. 

The involvement of serotonin (5-hydroxytryptamine) in disease states has been recognized for several decades. Research on antagonists awaited the recent development of methodology involving serotonin receptors. A thiazolopyrimidone serves as the nucleus for a pair of serotonin antagonists. The key intermediate 118 is in fact simply the lactonized form of 2-hydroxyethyl acetoace-tate. Condensation of this P-keto ester can be visualized to involve initial attack on the reactive... 

Schreiber R, Brocco M, Audinot V, et al (l-(2,5-Dimethoxy-4 iodophenyl)-2-amino-propane)-induced head-twitches in the rat are mediated by 5-hydroxytryptamine (5-HT) 2A receptors modulation by novel 5-HT2A/2C antagonists, Dj antagonists and 5-HTagonists. J Pharmacol Exp Ther 273 101—112, 1995 Screaton GR, Singer M, Cairns HS, et al Hyperpyrexia and rhabdomyolysis after MDMA ( ecstasy ) abuse. Lancet 399 667—668, 1992... 

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]. 

Ko FN, Yu SM, Su MJ, Wu YC, Teng CM. Pharmacological activity of (-)-discreta-mine, a novel vascular alpha-adrenoceptor and 5-hydroxytryptamine receptor antagonist, isolated from Fissistigma glaucescens. BrJ Pharmacol. 1993 110 882-888. 

N-methyl-actinodaphnine possesses 5-hydroxytryptamine receptor blocking activity and a selective antagonist of cq-adrenoceptors, selective for the a1B. than for the a1A-adrenoceptor subtype (14). What are the activities of N-methyl-actinodaphnine and other aporphines of Illigera and Hernandia species against topoisomerase ... 

Blier P, Steinberg S, Chaput Y, de Montigny C. (1989). Electrophysiological assessment of putative antagonists of 5-hydroxytryptamine receptors a single-cell study in the rat dorsal raphe nucleus. Can J Physiol Pharmacol. 67(2) 98-105. 

A series of indole oxadiazoles, such as (249), have been shown to be potent antagonists of the 5-hydroxytryptamine receptors <91JMC140>. 

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. 

The EOs reduced the contraction induced by acetylcholine, histamine [226-228, 210, 225, 232, 233], carbachol (muscarinic receptor activator) [237] and 5-hydroxytryptamine [229]. The EOs were found to relax intestinal smooth muscle by reducing the influx of Ca [227, 234], K+ [210, 224-226, 229, 230] and Ba [229, 237]. However, other reports have shown that lavender and geranium EOs were unlikely to act as cationic channel blockers [232]. The activities of the EOs resembled those of dicyclomine and atropine (muscarinic receptor antagonists) and dihydropyridine (calcium antagonist) by producing smooth-muscle relaxation [225, 236]. 

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... 

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