Ordopidine

Ordopidine
Clinical data
Other namesACR325; ACR-325
Routes of
administration		Oral
Drug classAtypical dopamine D2 receptor antagonist; Dopaminergic stabilizer
ATC code
  • None
Identifiers
  • 1-ethyl-4-(2-fluoro-3-methylsulfonylphenyl)piperidine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC14H20FNO2S
Molar mass285.38 g·mol−1
3D model (JSmol)
  • CCN1CCC(CC1)C2=C(C(=CC=C2)S(=O)(=O)C)F
  • InChI=1S/C14H20FNO2S/c1-3-16-9-7-11(8-10-16)12-5-4-6-13(14(12)15)19(2,17)18/h4-6,11H,3,7-10H2,1-2H3
  • Key:UKUPJASJNQDHPH-UHFFFAOYSA-N

Ordopidine (INNTooltip International Nonproprietary Name; 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. It is taken orally.

The drug acts as a competitive low-affinity dopamine D2 receptor antagonist with a fast dissociation rate in vitro. 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. This state-dependent profile of behavioral effects is not shared with other dopamine D2 receptor antagonists. 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.

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). 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.

Ordopidine was first described in the scientific literature by 2009. The drug was developed by Carlsson Research, NeuroSearch Sweden, and Saniona. As of June 2019, no recent development has been reported. Ordopidine has reached phase 1 clinical trials.

See also

References

  1. 1 2 3 4 5 6 "Ordopidine". AdisInsight. 28 June 2019. Retrieved 31 January 2026.
  2. 1 2 3 4 "Delving into the Latest Updates on Ordopidine with Synapse". Synapse. 31 January 2026. Retrieved 1 February 2026.
  3. 1 2 3 4 5 6 Waters S, Ponten H, Edling M, Svanberg B, Klamer D, Waters N (November 2014). "The dopaminergic stabilizers pridopidine and ordopidine enhance cortico-striatal Arc gene expression". Journal of Neural Transmission. 121 (11): 1337–1347. doi:10.1007/s00702-014-1231-1. PMID 24817271.
  4. 1 2 3 4 5 6 Pontón H, Dyhring T, Edling M, Pettersson F, Sonesson C, Svanberg B, et al. (2009). "P.l.c.043 ACR325: a dopaminergic stabiliser that displays state-dependent effects in-vivo". European Neuropsychopharmacology. 19: S276. doi:10.1016/S0924-977X(09)70403-1. Retrieved 1 February 2026.
  5. ↑ Sahlholm K, Sijbesma JW, Maas B, Kwizera C, Marcellino D, Ramakrishnan NK, et al. (September 2015). "Pridopidine selectively occupies sigma-1 rather than dopamine D2 receptors at behaviorally active doses". Psychopharmacology. 232 (18): 3443–3453. doi:10.1007/s00213-015-3997-8. PMC 4537502. PMID 26159455.