RTI-5152-12

RTI-5152-12, or WW-12 (in patent), is a synthetic small-molecule agonist of the atypical chemokine receptor ACKR3 (CXCR7) that was derived from the naturally occurring alkaloid conolidine.^[2][3][4][1] RTI-5152-12 has 15-fold improved potency towards ACKR3 relative to conolidine.^[2][3][1]

RTI-5152-12

Clinical data
Other names	WW-12 (patent)[1]
Drug class	ACKR3 (CXCR7) agonist; Opioid modulator
Identifiers
IUPAC name [(3E,4R)-3-ethylidene-1-pentylpiperidin-4-yl]-(1H-indol-2-yl)methanone
CAS Number	2794983-92-7 Y
PubChem CID	155927823
Chemical and physical data
Formula	C21H28N2O
Molar mass	324.468 g·mol−1
3D model (JSmol)	Interactive image
SMILES CCCCCN1CC[C@H](/C(=C\C)/C1)C(=O)C2=CC3=CC=CC=C3N2
InChI InChI=1S/C21H28N2O/c1-3-5-8-12-23-13-11-18(16(4-2)15-23)21(24)20-14-17-9-6-7-10-19(17)22-20/h4,6-7,9-10,14,18,22H,3,5,8,11-13,15H2,1-2H3/b16-4-/t18-/m1/s1 Key:MUZOMTWDNLINCG-QBSXKKPKSA-N

ACKR3 is a novel opioid receptor which functions as a broad-spectrum trap or scavenger for endogenous opioid peptides, including enkephalins, dynorphins, and nociceptin.^[2][5] The receptor acts as a negative modulator of the opioid system by decreasing the availability of opioid peptides for their classical receptors like the μ-opioid receptor.^[2][5] Ligands of ACKR3, by competitively displacing endogenous opioid peptides from ACKR3, can potentiate the actions of these endogenous opioids and produce effects like analgesia and anxiolysis in animals.^[2][3]

RTI-5152-12 is being developed as a potential pharmaceutical drug and, as of December 2021, is in the preclinical stage of development for treatment of pain.^[6][7][4] The chemical structure was not disclosed until a patent was published in June 2022.^[8][3]

See also

• LIH383