Article ; Online: Ajulemic acid (IP-751): synthesis, proof of principle, toxicity studies, and clinical trials.
The AAPS journal
2005 Volume 7, Issue 1, Page(s) E143–8
Abstract: Ajulemic acid (CT-3, IP-751, 1',1'-dimethylheptyl-Delta8-tetrahydrocannabinol-11-oic acid) (AJA) has a cannabinoid-derived structure; however, there is no evidence that it produces psychotropic actions when given at therapeutic doses. In a variety of ... ...
Abstract | Ajulemic acid (CT-3, IP-751, 1',1'-dimethylheptyl-Delta8-tetrahydrocannabinol-11-oic acid) (AJA) has a cannabinoid-derived structure; however, there is no evidence that it produces psychotropic actions when given at therapeutic doses. In a variety of animal assays, AJA shows efficacy in models for pain and inflammation. Furthermore, in the rat adjuvant arthritis model, it displayed a remarkable action in preventing the destruction of inflamed joints. A phase-2 human trial with chronic, neuropathic pain patients suggested that AJA could become a useful drug for treating this condition. Its low toxicity, particularly its lack of ulcerogenicity, further suggests that it will have a highly favorable therapeutic index and may replace some of the current anti-inflammatory/analgesic medications. Studies to date indicate a unique mechanism of action for AJA that may explain its lack of adverse side effects. |
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MeSH term(s) | Adult ; Analgesics/adverse effects ; Analgesics/chemical synthesis ; Analgesics/pharmacology ; Analgesics/therapeutic use ; Analgesics/toxicity ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/adverse effects ; Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Anti-Inflammatory Agents, Non-Steroidal/therapeutic use ; Anti-Inflammatory Agents, Non-Steroidal/toxicity ; Apoptosis/drug effects ; Arthritis, Experimental/drug therapy ; Cannabinoids/chemistry ; Cell Line, Tumor/drug effects ; Clinical Trials, Phase II as Topic ; Cytokines/physiology ; Double-Blind Method ; Dronabinol/adverse effects ; Dronabinol/analogs & derivatives ; Dronabinol/chemical synthesis ; Dronabinol/chemistry ; Dronabinol/pharmacology ; Dronabinol/therapeutic use ; Dronabinol/toxicity ; Drug Evaluation, Preclinical ; Edema/drug therapy ; Female ; Gastritis/chemically induced ; Humans ; Male ; Mice ; Middle Aged ; Molecular Structure ; Neuralgia/drug therapy ; Randomized Controlled Trials as Topic ; Rats |
Chemical Substances | Analgesics ; Anti-Inflammatory Agents, Non-Steroidal ; Cannabinoids ; Cytokines ; Dronabinol (7J8897W37S) ; lenabasum (OGN7X90BT8) |
Language | English |
Publishing date | 2005-06-29 |
Publishing country | United States |
Document type | Journal Article ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, P.H.S. ; Review |
ISSN | 1550-7416 |
ISSN (online) | 1550-7416 |
DOI | 10.1208/aapsj070115 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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