Psychotropic activity

Ajulemic acid (CT3, 8.9) is the dimethylheptyl homolog of the main metabo-hte of A8-THC. It has no psychotropic activity, but has analgesic and antiinflammatory effects. 

Krsiak, M. Timid singly-housed mice Their value in prediction of psychotropic activity of drugs. Brit J Pharmacol 55 141-150, 1975. 

Snyder, S. H., and Richelson, E. (1968) Psychedelic drugs Steric factors that predict psychotropic activity. Proc. Natl. Acad. Sci. USA, 60 206-213. 

TABLE 17-1. Hormones and hormonal interventions with psychotropic activity... 

Saivia spiendens contains saiviarin and spiendidin, both diterpenes, and we shouid expect more from other species. No psychotropic activity has been reported for those but that does not ciose the case--I heard background whispers of "piacebo effect" for years when taiking about the powers of dried ska Pastora ieaves ... 

The Psychotropic Active Principles of Ololiuqui, an Ancient Aztec Narcotic, lecture delivered at the lUPAC Symposium on The Chemistry of Natural Products, in Melbourne, August 18, 1960. return... 

To test for the hallucinogenic activity of S. divinorum in human beings, we drank the infusion of the leaves and waited for the effects to occur. Within 30 min we began to see visions, which lasted for several hours. This allowed rapid confirmation of the mint s psychotropic activity. But more interesting from a therapeutic standpoint are the other properties attributed to the plant properties that are much more difficult to assess. Are these concepts that are translatable into our western (orthodox) healing theory, or is ska Maria Pastora being used as a magical treatment (for a placebo effect) Extended observations in the field by an acute observer would undoubtedly be more fruitful than immediate attempts to isolate compounds responsible for these purported activities. 

Tricyclic Silicon Containing Compounds with Potential Psychotropic Activity... 

In addition to the stereochemical structure of the tricyclic skeleton, the conformation of the amino-substituted side chain can influence the psychotropic activity of such compounds. According to the theory of Wilhelm, transmission of the basic psychotropic activity depends largely on the constellation adopted by the side chain. However, the main psychotropic action (neuroleptic or thymoleptic) is chiefly a function of the particular stereochemistry of the tricyclic framework. 

Some novel experimental results are in contradiction to the hypothesis of a stereochemical structure-activity relationship. Two research groups (Corey et al., Tacke, Wannagat et al.) are working independently from each other on silicon containing tricyclic compounds with potential psychotropic activity, to bring some light to this dilemma. 

According to the concept of Stach/Poldinger91 and Wilhelm92, such alterations in stereochemical structure should result in changed psychotropic activities. To check this theory, comparative X-ray diffraction analyses and comparative biological tests are under investigation. 

X-ray diffraction analyses of some tricyclic silicon containing compounds with potential psychotropic activity have been carried out93, 100, 101 The experimental dihedral angles a are summarized in Table 12. 

Preliminary in vitro studies with dimetacrine (120a) and sila-dimetacrine (120b) on the isolated guinea pig ileum have shown that both compounds exhibit weak histaminolytic and anticholinergic activities. Comparative studies for psychotropic activity are in progress. 

V- (a-Triethoxysilyl)ethyl pyrrolidinone, prepared by (EtO)3Si-H addition to N-vinyl pyrrolidone in the presence of acetylacetonatodicarbonylrhodium, has been evaluated in terms of its neurotropic and psychotropic activity in mice.503... 

Cannabinoids Marijuana derivatives, including dronabinol [droe NAB i nol] and nabilone, are effective against moderately emetogenic chemotherapy. However, they are seldom first-line antiemetics because of their serious side effects, including dysphoria, hallucinations, sedation, vertigo, and disorientation. In spite of their psychotropic properties (see p. 105), the antiemetic action of cannabinoids may not involve the brain synthetic cannabinoids having no psychotropic activity, nevertheless are antiemetic. 

It is generally accepted that three regions are of basic importance in defining the psychotropic activity of tricyclic cannabinoids (i) the northern part of the terpene ring (carbons 9 and 11) (ii) the free phenolic group, and (iii) the lipid side-chain [21]. 

The cannabinoid acids, which are devoid of psychotropic activity, are promising anti-inflammatory agents (31) and it is possible that the next useful therapeutic agent will come from this direction, rather than the sought-after analgesic. 

Various preparations of the plant Cannabis saliva have been used since ancient times for their behavioral and pharmacological properties. R. Mechoulam, The Pharmohistory of Cannabis Saliva, 1-19 (1986). More recently, it has been demonstrated that the active plant constituents, known as cannabinoids, produce a variety of effects including bronchodilation, increased heart rate, reduced intraocular pressure, analgesia, antiemesis, alteration in body temperature, as well as anticonvulsant and psychotropic activities. (W. L. Dewey, Cannabinoid Pharmacology, Pharmacol. Rev., 38 45 (1986)). 

The main psychotropically active compounds present in Cannabis saliva or in its preparations (marijuana, hashish, etc.) is (3R,4R)-(-)-Al -THC (I). Occasionally small quantities of the compound (3R,4R)-(-)-A6 -THC (II) are found. Both compounds have a pronounced activity on mammals and on humans, producing the typical cannabis effect. This effect can be measured in animals in a quantitative manner by various tests, two of these being the monkey test, Grunfeld et al., Psychopharmacol. 14, 200 (1969) and by the ring test, Pertwee, Brit. J. Pharmacol. 46, 753 (1972). In the monkey test the minimum giving an effect is 50ug./kg of the (3R,4R)-(-)-Al-THC while that of (3R,4R)-(-)-A6 -THC is 0.1 to 0.25 mg/kg. 

Petit, S., Nallcl, J.P., Guillard, M., Dreux, J., Chermat, R., Poncelet, M., Biilach, C., and Simon, P., Synthesis and psychotropic activity of 3,4-diarylpiperidin-2-ones. Structure-activity relationship, Eur. J. Med. Chem., 25, 641, 1990. 

Mechoulam R, Feigenbauin JJ, Lander N, Segal M, Jarbe TU, Hiltunen AJ, Consroe P (1988) Enantiomeric cannabinoids stereospecificity of psychotropic activity. Experi-entia 44 762-764... 

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