Nelotanserin
Encyclopedia
Nelotanserin is a drug
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...

 developed by Arena Pharmaceuticals
Arena Pharmaceuticals
Arena Pharmaceuticals, Inc. is a biopharmaceutical company located in San Diego, California. The company is developing oral medications that target G-protein-coupled receptors. Currently none of the drugs is approved by the U.S...

 which acts as an inverse agonist
Inverse agonist
In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist....

 on the serotonin receptor subtype 5-HT2A
5-HT2A receptor
The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor . This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT2A may also have an inhibitory effect on certain areas such...

. APD-125 was shown to be effective and well tolerated in clinical trials, but development was halted in December 2008 because the substance did not meet the trial's endpoints. Research continues on newer analogues which may potentially be more successful.
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