BP1.4979

BP1.4979
Clinical data
Other names	BP-1.4979; BP14979; BP-14979
Routes of; administration	Oral
Drug class	Dopamine D3 receptor agonist
Pharmacokinetic data
Onset of action	1 hour (TmaxTooltip time to peak levels)
Elimination half-life	8 hours
Identifiers
	IUPAC name N-[4-[2-[4-(3-cyanophenyl)piperazin-1-yl]ethyl]cyclohexyl]-3-methoxypropanamide;
CAS Number	1000036-77-0;
PubChem CID	57964460;
DrugBank	DB16302;
ChemSpider	129321455;
UNII	XN7HA74WB0;
ChEMBL	ChEMBL4297484;
Chemical and physical data
Formula	C23H34N4O2
Molar mass	398.551 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COCCC(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=CC=CC(=C3)C#N;
	InChI InChI=1S/C23H34N4O2/c1-29-16-10-23(28)25-21-7-5-19(6-8-21)9-11-26-12-14-27(15-13-26)22-4-2-3-20(17-22)18-24/h2-4,17,19,21H,5-16H2,1H3,(H,25,28); Key:PLMAPPWZOQMTBI-UHFFFAOYSA-N;

BP1.4979 is a selective dopamine D₃ receptor agonist which is under development for the treatment of binge-eating disorder, obsessive–compulsive disorder (OCD), restless legs syndrome (RLS), and smoking withdrawal.^[1]^[3]^[2] It is taken orally.^[1] The drug acts as a highly potent weak partial agonist of the dopamine D₃ receptor (K_i = ~1 nM; EC₅₀Tooltip half-maximal effective concentration = 0.7 nM; E_maxTooltip maximal efficacy = 32%).^[2] It has around 200-fold higher affinity for the dopamine D₃ receptor than for the dopamine D₂ receptor (K_i = 192 nM), where it is an antagonist.^[2] BP1.4979 showed 66% dopamine D₃ receptor occupancy and 8% dopamine D₂ receptor occupancy with positron emission tomography (PET) imaging in a clinical study.^[3]^[2] The time to peak levels of BP1.4979 is 1 hour and its elimination half-life is about 8 hours.^[2] The drug is under development by Bioprojet.^[1] As of January 2026, it is in phase 2 clinical trials for all indications.^[1]

References

1 2 3 4 5 "BP 14979". AdisInsight. 16 January 2026. Retrieved 18 January 2026.
1 2 3 4 5 6 7 Di Ciano P, Mansouri E, Tong J, Wilson AA, Houle S, Boileau I, et al. (June 2019). "Occupancy of dopamine D₂ and D₃ receptors by a novel D3 partial agonist BP1.4979: a [¹¹C]-(+)-PHNO PET study in humans". Neuropsychopharmacology. 44 (7): 1284–1290. doi:10.1038/s41386-018-0285-4. PMC 6785153. PMID 30659274. The purpose of the present study was to investigate, for the first time in healthy controls, the in vivo occupancy of the DRD₃ and DRD₂ by a selective DRD₃ partial agonist. BP1.4979 has an affinity for the human DRD₃ of ~1 nM and presents a partial agonist behaviour with an intrinsic activity of 32% ± 2.6% and EC₅₀ of 0.7 ± 0.3 nM. In contrast, it behaves as an antagonist at the hDRD₂ with K_i of 192 nM. After oral administration in humans, it reaches peak serum concentrations in one hour and has a half-life of about 8 h.
1 2 Sokoloff P, Le Foll B (2022). "A Historical Perspective on the Dopamine D3 Receptor". Therapeutic Applications of Dopamine D3 Receptor Function. Current Topics in Behavioral Neurosciences. Vol. 60. Cham: Springer International Publishing. pp. 1–28. doi:10.1007/7854_2022_315. ISBN 978-3-031-23057-8. PMID 35467293. Retrieved 18 January 2026.

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