Serotonin 5-HT2 receptor

Pompeiano, M., Palacios, J. M. Mengod, G. (1994). Distribution of the serotonin 5-HT2 receptor family mRNAs comparison between 5-HT2a and 5-HT2C receptors. Molec. Brain Res. 23, 163-78. 

Wong DF, Lever JR, Hartig PR, Dannals RF, Villemagne V, Hoffman BJ, Wilson AA, Ravert HT, Links JM, Scheffel U, et al. (1987). Localization of serotonin 5-HT2 receptors in living human brain by positron emission tomography using Nl-([llC]-methyl)-2-Br-LSD. Synapse. 1(5) 393-98. 

Ketanserin is a serotonin (5-HT2) receptor antagonist with additional a 1-adrenoceptor blocking activity. Its antihypertensive mechanism is not understood in detail. When administered intravenously its... 

The triazolopyridine trazodone does not have an appreciable effect on the re-uptake of the neurotrans-mittors dopamine or noradrenaline. It is a weak inhibitor of serotonin re-uptake but is a potent antagonist of the serotonin 5-HT2 receptor. Clinical experience has shown unpredictable efficacy. Trazodone has little antimuscarinic activity and has little if any action on cardiac conduction. Like mianserin it can therefore safely be used in patients for which anticholinergics are contraindicated and there are no absolute contraindications for patients with concomitant diseases of the cardiovascular system. 

Several quinazoline derivatives have antihypertensive activity. Examples include prazosin 1163, doxazosin 1164, terazosin 1165, bunazosin 1166, and trimazosin 1167, which bind to Qj-adrenoreceptors, and ketanserin 1168, a serotonin 5-HT2 receptor antagonist. 

Blockade of (serotonin) 5-HT2 receptors No catalepsy, no marked antagonism of apomorphine... 

ACh M, acetylcholine muscarinic receptor ctlf alpha -adrenoceptor H1 histaminei receptor 5-HT2, serotonin 5-HT2 receptor NET, norepinephrine transporter SERT, serotonin transporter. 0/+, minimal affinity +, mild affinity ++, moderate affinity +++, high affinity. 

Buck KJ, et al. Serotonin 5-HT2 receptors and alcohol reward, withdrawal and discrimination. Alcohol Clin Exp Res 2004 28(2) 211-216. 

Mamo D, Kapur S, Shammi C, Papatheodorou G, Mann S, Therrien F, Remington G. A pet study of dopamine D2 and serotonin 5-HT2 receptor occupancy in patients with schizophrenia treated with therapeutic doses of ziprasidone. Am J Psychiatry 2004 161 818-25. 

Mirtazepine has specific noradrenergic and serotonergic receptor activity. It also has significant histamine Hi and serotonin 5-HT2 receptor blocking activity which probably underlay its propensity to cause weight gain, both acutely and in the long term (Cassano and Fava 2004). 

Kao, H.-T., Adham, N., Olsen, M.A., Weinshank, R.L., Branchek, T.A. and Hartig, P.R. (1992) Site-directed mutagenesis of a single residue changes the binding properties of the serotonin 5-HT2 receptor from a human to a rat pharmacology. FEBS Lett. 307 324-328. 

Sanders-Bush E, Fentress H, Hazelwood L. Serotonin 5-HT2 receptors molecular and genomic diversity. Mol Interventions 2003 3 319-330. 

Fig. 6 Gas chromatograms of the drug substance a-phenyl-1-(2-phenylethyl)-pipeline methanol, a serotonin 5-HT2 receptor antagonist, spiked with possible processing solvents. Three solvent levels are represented, a) 0% (w/w) b) 0.1% (w/w) spike c)...

Andersen K, Liljefors T, Gundertofte K, Perregaard J, Bogeso KP. Development of a receptor-interaction model for serotonin 5-HT2 receptor antagonists - predicting selectivity with respect to dopamine D2 receptors. J. Med. Chem. 1994 37 950-962. 

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