Tuesday, February 9, 2010

New cyclopropane derivative as better antidepressant ?

We know that most of the antidepressants have side effects such as  constipation, dry mouth, drowsiness and hypotension, or low blood pressure. Amongst various trypes TCAs, tricyclic antidepressants also have  the above mentioned side effects. 

In recent times, the TCAs have been largely replaced in clinical use in most parts of the world by newer antidepressants such as the selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs), among others, though they are still sometimes prescribed for certain indications.

Duloxetine, is a serotonin-norepinephrine reuptake inhibitor manufactured and marketed by Eli Lilly. It is effective for major depressive disorder and it is as effective as venlafaxine in generalized anxiety disorder. Duloxetine failed the US approval for stress urinary incontinence amidst the concerns about liver toxicity and suicidal events; however, it was approved for this indication in Europe and Canada.

Interestingly, chemists at Oregon State University have discovered and synthesized a new compound  (see the structure) that in laboratory and animal tests appears to be similar to, but may have advantages over Duloxetine. As per the claim by the  lead researcher Dr. James White (Professor Emeritus of Chemistry at OSU),  the new compound has properties similar to (Cymbalta) Duloxetine in some ways, but in laboratory and animal studies does a better job at balancing body chemistry. New compound is 10 times better than Duloxetine at inhibiting the re-uptake of norepinephine and comes close to the perfectly balanced antidepressant with fewer side effects, such as concerns with constipation and hypotension. Though clinical studies are essential to substantiate the claims its a good achievement...

Ref : http://pubs.acs.org/doi/abs/10.1021/jm900847b

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