Ordopidine

Last updated
Ordopidine
Clinical data
Other namesACR325; ACR-325
Routes of
administration 		Oral [1]
Drug class Atypical 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
Formula C14H20FNO2S
Molar mass 285.38 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 (INN Tooltip 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. [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] Subsequently, 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. 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". J Neural Transm (Vienna). 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.; Swanson, L.; Tedroff, J.; Waters, S.; Waters, N. (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, Dierckx RA, Elsinga PH, van Waarde A (September 2015). "Pridopidine selectively occupies sigma-1 rather than dopamine D2 receptors at behaviorally active doses". Psychopharmacology (Berl). 232 (18): 3443–3453. doi:10.1007/s00213-015-3997-8. PMC   4537502 . PMID   26159455.
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