Chemistry:Ordopidine
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]
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]
See also
References
- ↑ 1.0 1.1 1.2 1.3 1.4 "Ordopidine". 28 June 2019. https://adisinsight.springer.com/drugs/800025217.
- ↑ 2.0 2.1 2.2 2.3 "Delving into the Latest Updates on Ordopidine with Synapse". 31 January 2026. https://synapse.patsnap.com/drug/c7d3c176f5aa43a096fa9d706000144d.
- ↑ 3.0 3.1 3.2 3.3 3.4 3.5 "The dopaminergic stabilizers pridopidine and ordopidine enhance cortico-striatal Arc gene expression". Journal of Neural Transmission 121 (11): 1337–1347. November 2014. doi:10.1007/s00702-014-1231-1. PMID 24817271.
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 "P.l.c.043 ACR325: a dopaminergic stabiliser that displays state-dependent effects in-vivo". European Neuropsychopharmacology 19: S276. 2009. doi:10.1016/S0924-977X(09)70403-1. https://linkinghub.elsevier.com/retrieve/pii/S0924977X09704031. Retrieved 1 February 2026.
- ↑ "Pridopidine selectively occupies sigma-1 rather than dopamine D2 receptors at behaviorally active doses". Psychopharmacology 232 (18): 3443–3453. September 2015. doi:10.1007/s00213-015-3997-8. PMID 26159455.
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