PMID: 8584617Oct 1, 1995Paper

The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis

Psychopharmacology
D FiorellaJ C Winter

Abstract

Investigations conducted over the past 3 decades have demonstrated that serotonergic receptors, specifically the 5-HT2A and 5-HT2C subtypes, play an important role in the behavioral effects of hallucinogenic compounds. The present study was designed to determine the respective significance of these two receptors in the stimulus effects of LSD and (-)DOM in the rat. Specifically, the interactions of a series of serotonergic antagonists (risperidone, pirenpirone, metergoline, ketanserin, loxapine, LY53857, pizotyline, spiperone, cyprohepatadine, mesulergine, promethazine, and thioridazine) with the LSD stimulus and the (-)DOM stimulus in LSD-trained subjects was defined. From these data, IC50 values were determined for the inhibition of the LSD-appropriate responding elicited by either 0.1 mg/kg LSD (15-min pretreatment time) or 0.4 mg/kg (-)DOM (75-min pretreatment). In addition, the affinities of these antagonists for 5-HT2A and 5-HT2C receptors were determined in radioligand competition studies, 5-HT2A affinity correlated significantly with IC50 values for the blockade of the LSD (r = +0.75, P < 0.05) and (-)DOM (r = +0.95, P < 0.001) stimuli in the LSD trained subjects. 5-HT2C affinity did not correlate significantly with eit...Continue Reading

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Citations

Jun 29, 2005·Psychopharmacology·William E FantegrossiJames H Woods
Jul 19, 2005·Psychopharmacology·C J ReissigJ C Winter
Nov 26, 2009·Psychopharmacology·Adam L Halberstadt, Mark A Geyer
Jan 1, 1996·Life Sciences·D FiorellaJ C Winter
Feb 6, 2004·Pharmacology & Therapeutics·David E Nichols
Dec 4, 1998·Biological Psychiatry·J A LiebermanJ E Kraus
Mar 20, 2002·Pharmacology, Biochemistry, and Behavior·Richard A RabinJ C Winter
Oct 12, 2002·Pharmacology, Biochemistry, and Behavior·J C WinterR A Rabin
Jan 25, 2003·Pharmacology, Biochemistry, and Behavior·Mireille M DoatJerrold C Winter
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Oct 9, 1999·Pharmacology, Biochemistry, and Behavior·J C WinterR A Rabin
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Jun 16, 1999·Progress in Neuro-psychopharmacology & Biological Psychiatry·S HelsleyJ C Winter
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