Ordopidine
Pharmaceutical compound
From Wikipedia, the free encyclopedia
Ordopidine (INN; developmental code ACR-325) is an atypical dopamine D2 receptor antagonist and so-called "dopaminergic stabilizer" which is or was under development for the treatment of Parkinson's disease and bipolar disorder.[1][2][3][4] It is taken orally.[1]
- None
 | |
| Clinical data | |
|---|---|
| Other names | ACR325; ACR-325 |
| Routes of administration | Oral[1] |
| Drug class | Atypical dopamine D2 receptor antagonist; Dopaminergic stabilizer |
| ATC code |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C14H20FNO2S |
| Molar mass | 285.38 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
The drug acts as a competitive low-affinity dopamine D2 receptor antagonist with a fast dissociation rate in vitro.[3][4] It inhibits dextroamphetamine-induced hyperlocomotion in rodents but has little effect on locomotor activity in untreated animals and stimulates behavioral activity in states of hypoactivity.[3][4] This state-dependent profile of behavioral effects is not shared with other dopamine D2 receptor antagonists.[3][4] Ordopidine shows similar neurochemical effects as conventional dopamine D2 receptor antagonists, such as increased dopamine and/or dopamine metabolite levels in various brain areas like the frontal cortex, basal ganglia, and limbic system.[3][4]
The actions and effects of ordopidine are similar to those of its close analogue pridopidine (which it differs from only by a single methyl group).[3] Subsequent to their initial characterization, pridopidine was found to act as a sigma receptor ligand with much higher affinity than for the dopamine D2 receptor, with this balance of activities potentially explaining its atypicality and "dopaminergic stabilizer" properties.[5]
Ordopidine was first described in the scientific literature by 2009.[4] The drug was developed by Carlsson Research, NeuroSearch Sweden, and Saniona.[1][2] As of June 2019, no recent development has been reported.[1][2] Ordopidine has reached phase 1 clinical trials.[1][2]