NEWS New substances which block the breakdown of the body's own cannabis may form the basis of pain killers of the future. Emmelie Björklund predicts this in the thesis she defends at Umeå University in Sweden.
"A lot of research remains before a drug is ready for sale in the market, but the fact is that we can already now highlight three substances which have the potential to work as pain killers in the future," says Emmelie Björklund, who is a doctoral student at the Department of Pharmacology and Clinical Neuroscience, Pharmacology.
Despite the fact that the body's cannabis-like substances, endocannabinoids, have shown to have a positive effect on pain and inflammation in animal models, their importance for pain in human beings is relatively unknown. Endocannabinoids is produced during different illnesses, for example, during pain and inflammation. As the body's cells quickly absorb and metabolize the endocannabinoids, their effect is short-term. Currently we do not know how the endocannabinoids are absorbed by the cells, however we know that the breakdown inside the cell takes place with the help of the enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL). Therefore Emmelie Björklund has focused on these enzymes in her research.
"The aim of my studies has been to find new substances which can have a pain relieving effect by stopping the breakdown through FAAH and MGL. The major challenge is identifying new chemical substances which can serve as start molecules for the development of drugs," says Emmelie Björklund.
One way of finding new impulses among chemical compounds which can block both enzymes is to search among substances which already are, or have been drugs. According to Emmelie Björklund, the benefit of this approach is that it can result in substances which interact with more than one biological target protein, which in turn can have a better treatment effect. The results of Emmelie Björklund's thesis show that three substances, Flu-AM1 (related to the painkiller flurbiprofen), ketoconazole and troglitazone can block FAAH or MGL, and thereby block the breakdown of endocannabinoids.
In the thesis Emmelie Björklund has also studied chronic pain and histological lesion in the Achilles' tendon. The condition is difficult and currently the cause of this pain is not completely clear. In the thesis she shows that the manifestation of cannabinoid receptor type 1 changes in painful tendons compared to tendons which do not hurt.
Emmelie BjörklundTelephone: +46 (0)73-049 10 53 or +46 (0)90-785 15 14
E-mail: emmelie.bjorklund@pharm.umu.se
On Friday 5 September Emmelie Björklund, Department of Pharmacology and Clinical Neuroscience, Pharmacology, Umeå University, will defend her thesis entitled 'The endocannabinoid system: A translational study from Achilles tendinosis to cyclooxygenase.
Editor: Mattias Grundström Mitz