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  • Antagonist correlation analysis  (2)
  • DOM (2,5-dimethoxy-4-methylamphetamine)  (1)
  • 1
    Electronic Resource
    Electronic Resource
    The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs I: Antagonist correlation analysis (1995)
    Springer
    Psychopharmacology 121 (1995), S. 347-356 
    Details
    ISSN: 1432-2072
    Keywords: Serotonin (5-HT) ; Drug-induced stimulus control (DISC) ; 5-HT2A ; 5-HT2C ; Antagonist correlation analysis ; Lysergic acid diethylamide (LSD) ; 2,5-Dimethoxy-4-methylamphetamine (DOM)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: 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,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 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.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02246074
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Role of 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs II: reassessment of LSD false positives (1995)
    Springer
    Psychopharmacology 121 (1995), S. 357-363 
    Details
    ISSN: 1432-2072
    Keywords: Drug-induced stimulus control ; Hallucinogens ; 5-HT2A ; 5-HT2C ; LSD (lysergic acid diethylamide) ; DOM (2,5-dimethoxy-4-methylamphetamine)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract In the context of animal studies of hallucinogens, an LSD-false positive is defined as a drug known to be devoid of hallucinogenic activity in humans but which nonetheless fully mimics LSD in animals. Quipazine, MK-212, lisuride, and yohimbine have all been reported to be LSD false positives. The present study was designed to determine whether these compounds also substitute for the stimulus effects of the more pharmacologically selective hallucinogen (−)DOM (0.56 mg/kg, 75-min pretreatment time). The LSD and (−)DOM stimuli fully generalized to quipazine (3.0 mg/kg) and lisuride (0.2 mg/kg), but only partially generalized to MK-212 (0.1–1.0 mg/kg) and yohimbine (2–20 mg/kg). In combination tests, pirenpirone (0.08 mg/kg), a compound with both D2 and 5-HT2A affinity, blocked the substitution of quipazine and lisuride for the (−)DOM stimulus. Ketanserin (2.5 mg/kg), an antagonist with greater than 1 order of magnitude higher affinity for 5-HT2A receptors than either 5-HT2C or D2 receptors, also fully blocked the substitution of these compounds for the (−)DOM stimulus, while the selective D2 antagonist thiothixene (0.1–1.0 mg/kg) failed to block the substitution of lisuride for the (−)DOM stimulus. These results suggest that quipazine and lisuride substitute for the stimulus properties of the phenylalkglamine hallucinogen (−)DOM via agonist activity at 5-HT2A receptors. In addition, these results suggest that 5-HT2A agonist activity may be required, but is not in itself sufficient, for indolamine and phenylalkglamine compounds to elicit hallucinations in humans. Finally, it is concluded that MK-212 and yohimbine are neither LSD nor (−)DOM false positives.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02246075
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    Paper (German National Licenses)
    Fulltext
  • 3
    Electronic Resource
    Electronic Resource
    The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects ofm-chlorophenylpiperazine (1995)
    Springer
    Psychopharmacology 119 (1995), S. 222-230 
    Details
    ISSN: 1432-2072
    Keywords: m-Chlorophenylpiperazine (mCPP) ; Serotonin (5-HT) ; Drug-induced stimulus control ; 5-HT2A ; 5-HT2C ; Antagonist correlation analysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract m-Chlorophenylpiperazine (mCPP), a major metabolite of the atypical antidepressant trazadone, has been observed to produce marked physiological and behavioral effects in both humans and animals. These effects have been attributed to the interaction of mCPP with serotonergic receptors. The present study was designed to characterize those interactions of mCPP with central serotonergic receptors which mediate mCPP-induced stimulus control. A series of serotonergic antagonists (mesulergine, pizotyline, ketanserin, spiperone, risperidone, ritanserin, metergoline, pirenpirone, and LY53857) was tested for the ability to block the mCPP stimulus. The affinity of these antagonists for 5-HT2A and 5-HT2C receptors was then correlated with maximal percent inhibition of the mCPP stimulus. Kd at the 5-HT2C receptor was inversely proportional (r=−0.75,P〈0.05), and Kd at the 5-HT2A receptor directly proportional (r=+0.67,P〈0.05) to the maximal percent inhibition of the mCPP stimulus. The 5-HT2C selectivity ratio [Kd(5-HT2A)/Kd(5-HT2C)] of the antagonists was directly proportional (r=+0.86,P〈0.01) to maximal percent inhibition of the mCPP stimulus. A multiple regressions analysis indicated that 81% of the variance in the ability of a given antagonist to block the mCPP stimulus could be predicted on the basis of its affinity for 5-HT2A and 5-HT2C receptors. It is concluded that the stimulus effects of mCPP are mediated predominantly by a combination of agonist activity at 5-HT2C receptors and antagonist activity at 5-HT2A receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02246164
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    Paper (German National Licenses)
    Fulltext
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