Genaera Corporation Announces MSI-1436 Data Presented at Society of Neuroscien...( - Preclinical Data Indicates MSI-1...),Health

- Preclinical Data Indicates MSI-1436 Does Not Alter Rate of Dopamine

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PLYMOUTH MEETING, Pa., March 28 /PRNewswire-FirstCall/ -- Genaera Corporation (Nasdaq: GENR) announced that preclinical data was presented Thursday at the Chicago Chapter of the Society of Neuroscience by Mitchell F. Roitman, Ph.D., a Genaera collaborator and investigator with the University of Illinois at Chicago. The abstract titled "A novel anti-obesity drug MSI-1436 does not alter the rate of dopamine uptake via the dopamine transporter," demonstrates that MSI-1436 does not inhibit the dopamine transporter in vivo by directly measuring dopamine levels in the brain of rats after MSI-1436 administration.

Dopamine is a neurotransmitter found in the brain which can have affects on locomotor function and addictive behavior. Many drugs that reduce food intake and body weight affect the rate of dopamine reuptake by inhibiting the dopamine transporter (DAT), such as amphetamine and bupropion. Such compounds, which inhibit the dopamine transporter, are considered undesirable as weight- loss drugs since they affect locomotor behavior and may have high addictive potential. MSI-1436 is a protein tyrosine phosphatase 1B inhibitor (PTP-1B), which increases insulin sensitivity and reduces food intake in animals, and is currently in clinical development for anti-obesity and anti-diabetes therapy. Preliminary in vitro studies in cells suggested that MSI-1436 may interact with the dopamine transporter but in vivo behavioral tests in rats did not show DAT-inhibitory activity. Therefore, a definitive study to resolve this discrepancy was designed.

The effects of MSI-1436 on dopamine reuptake were investigated using in viv
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