Sarizotan (EMD-128,130) is a selective 5-HT_1A receptor

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

and D₂ receptor

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.antipsychotic Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), p ...

effects, and has also shown efficacy in reducing

dyskinesia Dyskinesia refers to a category of movement disorders that are characterized by involuntary muscle movements, including movements similar to tics or chorea and diminished voluntary movements. Dyskinesia can be anything from a slight tremor of t ...

s resulting from long-term anti-Parkinsonian treatment with

levodopa Levodopa, also known as L-DOPA and sold under many brand names, is a dopaminergic medication which is used in the treatment of Parkinson's disease (PD) and certain other conditions like dopamine-responsive dystonia and restless legs syndrome. ...

. In June 2006, the developer

Merck KGaA The Merck Group, branded and commonly known as Merck, is a German Multinational corporation, multinational science and technology company headquartered in Darmstadt, with about 60,000 employees and a presence in 66 countries. The group include ...

announced that the development of sarizotan was discontinued, after two sarizotan Phase III studies (PADDY I, PADDY II) failed to meet the primary efficacy endpoint and neither the Phase II findings nor the results from preclinical studies could be confirmed. No statistically significant difference of the primary target variable between sarizotan and placebo could be demonstrated.

References

5-HT1A agonists 5-HT7 agonists Abandoned drugs D2 antagonists Pyridines Secondary amines 4-Fluorophenyl compounds Chromanes {{nervous-system-drug-stub

See also

References