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Gessner PK, Khairallah PA, McIsaac WM, Page IH.
“The Relationship Between the Metabolic Fate and Pharmacological Actions of Serotonin, Bufotenine and Psilocybin”.
J. Pharmacol. & Exper. Therap.. 1960 Oct;130(2):126-133.
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Abstract
Experiments in rats. . 1. The pressor effect of serotonin (5-HT, 20 mcg. i.v.) lasted 2-3 minutes, that of bufotenine (20 mcg.) 30 minutes, that of Psilocybin (37.5 mcg.) more than 1 hour. BOL-148 (50 mcg.) antagonized all 3 drugs. . 2. Potentiation of barbiturates. Hexobarbital sleeping time was prolonged after pretreatment with 5-HT by 58%, bufotenine 81%, Psilocybin 126% (all in dosage 51.5 micromol/kg. i.p.) . 3. Toxicity studies showed that bufotenine was more toxic than Psilocybin. . 4. Metabolic studies. a) In vivo (urinary excretion): 5-HT was excreted mainly as 5-hydroxyindole acetic acid (HIAA), but bufotenine and Psilocybin mainly unchanged or conjugated wtih glucuronic acid. After Psilocybin, only traces of HIAA appeared in the urine, while some HIAA was formed from bufotenine, through much less than from 5-HT. Thus 5-HT is markedly effected by monoamino oxidase (MAO), bufotenine slightly, and Psilocybin nearly not at all. b) In vitro studies confirmed the greater effect of MAO on bufotenine than on Psilocybin. . The duration of the pressor effect (see 1) is inversely proportional and probably related to the rate of inactivation of the 3 compounds by MAO. The intensity of barbiturate potentiation (see 2) and the duration of pressor effects are parallel. . Regarding pressor effect: The rats were pretreated with a ganglionic blocking agent (pentolinium) as 5-HT is predominantly depressor in unblocked rats. In 5 of 6 experiments 5-HT antagonized the pressor effect of Psilocybin. . Regarding toxicity: Bufotenine 125 mg/kg i.p. was fatal within 30 minutes when given at once, but caused abnormal behavior with recovery when distributed over several hours. However, in the latter case, on the 6th or 7th day, 4 or 5 rats developed prostration, thoracic kyphosis, cervical hyperectension and rapidly died. Psilocybin, 100 mg. i.p. (at once) decreased normal activity (while responses to external stimuli were increased) with recovery within 24 hours. However, one rat died 10 days later in a manner similar to that observed with bufotenine. This delayed mortality may be caused by atrophy of the muscles. Weight loss and muscle wasting were found to be part of the syndrome.
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