Anandamide Amidase Inhibitors as Analgesic Agents

Delta-9-Tetrahydrocannabinol (Delta-9-THC) and, to a small extent, also Delta-8-THC are the biologically active constituents in extracts of the plant Cannabis sativa (marihuana, hashish) and are responsible for the effects on the human central nervous system (CNS). Potential historical and contemporary therapeutic uses of cannahis preparations include, interalia, analgesia, emesis, anorexia, glaucoma and motor disorders. 

It is additionally known that cerebral apoplexy is a result of a sudden circulatory disorder of a human brain area with subsequent functional losses, with corresponding neurological and/or psychological symptoms. The causes of cerebral apoplexy can lie in cerebral haemorrhages (e.g. after a vascular tear in hypertension, arteriosclerosis and apoplectic aneurysms) and ischaemias (e.g. due to a blood pressure drop crisis or embolism). 

The functional losses in the brain lead to a degeneration or destruction of the brain cells (cf. Journal of Cerebral Blood Flow and Metabolism 1981, 1, 155 Chem. Eng. News 1996 (May 13), 41 Trends Pharmacol. Sci. 1996,1, 227). Craniocerebral trauma is understood as meaning covered and open cranial injuries with involvement of the brain [cf. Schweiz, med. Wschr. 1993,123 449]. 

Since the cell death in this area does not occur immediately, a therapeutic opportunity reveals itself to block the unfavourable development of the course of the disease both after stroke and after trauma. 

It has now been found that the known cannabinoid CBl receptor agonists cited above are surprisingly suitable for the prophylaxis and treatment of neurodegenerative disorders, in particular of cerebral apoplexy and craniocerebral trauma. Source Mittendorf 2001 

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