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

@article{citeulike:3771969, 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, cyproheptadine, 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,Pr=+0.95,P2C affinity did not correlate significantly with either series of IC50 values. These data indicate that (1) the stimulus effects of LSD, and (2) the substitution of (−)DOM for the LSD stimulus are mediated by agonist activity at 5-HT2A receptors.}, author = {Fiorella, D. and Rabin, R. and Winter, J.}, citeulike-article-id = {3771969}, citeulike-linkout-0 = {http://dx.doi.org/10.1007/BF02246074}, citeulike-linkout-1 = {http://www.springerlink.com/content/764g108531w2447x}, day = {16}, doi = {10.1007/BF02246074}, journal = {Psychopharmacology}, keywords = {5ht-2a, 5ht-2c}, month = {October}, number = {3}, pages = {347--356}, posted-at = {2008-12-11 00:47:16}, priority = {2}, title = {The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs I: Antagonist correlation analysis}, url = {http://dx.doi.org/10.1007/BF02246074}, volume = {121}, year = {1995} }

TY - JOUR ID - citeulike:3771969 L3 - citeulike-article-id:3771969 N2 - 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, cyproheptadine, 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,Pr=+0.95,P2C affinity did not correlate significantly with either series of IC50 values. These data indicate that (1) the stimulus effects of LSD, and (2) the substitution of (−)DOM for the LSD stimulus are mediated by agonist activity at 5-HT2A receptors. IS - 3 JF - Psychopharmacology EP - 356 TI - The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs I: Antagonist correlation analysis VL - 121 SP - 347 KW - 5ht-2a KW - 5ht-2c AU - Fiorella, D AU - Rabin, R AU - Winter, J PY - 1995/10/16/ UR - http://dx.doi.org/10.1007/BF02246074 ER -