Inxight Drugs

DOV-102,677 is a “Triple” Monoamine Neurotransmitter Uptake Inhibitor being developed by Merck for treating the major depressive disorder. In preclinical studies, DOV 102,677 increased extracellular levels of DA and 5-HT in the prefrontal cortex at 100 min after administration. DA levels were stably increased for the duration (240 min) of the study, but serotonin levels declined to baseline by 200 min after administration. NE levels increased linearly to a maximum of 240 min post-dosing. Consistent with these increases in NE levels, the density of β-adrenoceptors was selectively decreased in the cortex of rats treated with DOV 102,677. DOV 102,677 dose-dependently reduced the amount of time spent immobile by rats in the forced swim test, a model predictive of antidepressant activity, with a minimum effective dose (MED) of 20 mg/kg and a maximal efficacy comparable to imipramine. However, phase I clinical trials for treatment Depression in the USA was discontinued. Instead of being developed for depression, DOV-102,677 is being developed for the treatment of alcoholism.

MESPIPERONE

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5U54JM2T8G

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Other

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CHEMICAL (ACHIRAL)

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N-Methylspiperone (NMSP) is a derivate of spiperone and high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. In the biodistribution studies in rodents, there was a high accumulation of radioactivity in the liver, lung, and kidneys, whereas the brain radioactivity was not as high N-Methylspiperone is used to study the dopamine and serotonin neurotransmitter systems. Labeled with the radioisotope carbon-11, it can be used for positron emission tomography (PET). [11C] N-Methylspiperone PET is useful for objective monitoring of D2and 5-HT2A receptor occupancy and density in patients being treated with antipsychotic drugs.