Studies on Accumulation of (<sup>14</sup>C)-Mescaline in Brain Homogenates: Effects of Psychotropic and Other Agents
Pharmacology – January 01, 1975
Source: OpenAlex
Summary
High concentrations of tranquilizers, such as chlorpromazine and trifluoperazine, significantly inhibit the accumulation of mescaline in rat brain samples, with a notable effect observed at 1.33 mumol/ml. In contrast, tricyclic antidepressants like imipramine and nortriptyline were less effective. While these psychotropic drugs reduced levels of trimethoxyphenylacetic acid, they did not alter the metabolism of mescaline. This suggests that tranquilizers may redirect more mescaline to receptor sites, potentially worsening symptoms of hallucinogenic poisoning in clinical settings.
Abstract
Incubation of rat brain homogenates or 14,500 g pellet isolated from the homogenate with (14C)-mescaline was associated with accumulation of (14C)-mescaline in the pellet. 1.33 mumol/ml of chlorpromazine, trifluoperazine, fluphenazine, imipramine, desmethylimipramine, nortriptyline and amitriptyline inhibited the accumulation of mescaline. Lower concentrations (0.133-0.44 mumol/ml) of the psychotropic drugs were less effective. The tricyclic antidepressants were less potent than the tranquilizers. Although the trimethoxyphenylacetic acid (TMPA) levels of the pellet were also reduced by the psychotropic drugs, the TMPA:mescaline ratios were unchanged indicating that the drugs had no effect on the metabolism of mescaline. The inhibition of accumulation of mescaline by the high concentrations of tranquilizers may divert more of the hallucinogen to the receptor site. Thus, an explanation for the reported worsening of clinical syndrome of hallucinogenic poisoning by tranquilizers is provided.