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| Other names | ACR325; ACR-325 |
| Routes of administration | Oral[1] |
| Drug class | AtypicaldopamineD2 receptorantagonist; Dopaminergic stabilizer |
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| Formula | C14H20FNO2S |
| Molar mass | 285.38 g·mol−1 |
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Ordopidine (INNTooltip International Nonproprietary Name; developmental codeACR-325) is an atypicaldopamineD2 receptorantagonist and so-called "dopaminergic stabilizer" which is or was under development for the treatment ofParkinson's disease andbipolar disorder.[1][2][3][4] It is takenorally.[1]
The drug acts as acompetitive low-affinity dopamine D2 receptor antagonist with a fast dissociation ratein vitro.[3][4] It inhibitsdextroamphetamine-inducedhyperlocomotion in rodents but has little effect onlocomotor activity in untreated animals and stimulates behavioral activity in states ofhypoactivity.[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 increaseddopamine and/or dopaminemetabolite levels in various brain areas like thefrontal cortex,basal ganglia, andlimbic system.[3][4]
The actions and effects of ordopidine are similar to those of its closeanaloguepridopidine (which it differs from only by a singlemethyl group).[3] Subsequent to their initial characterization, pridopidine was found to act as asigma receptorligand 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 thescientific 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 reachedphase 1clinical trials.[1][2]
