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3C-PEP is a phenylpiperazine characterised as a high-affinity, transporter-selective dopamine transporter (DAT) ligand.
It was identified during structure-activity work on sigma-2 selective phenylpiperazines. While substituents were being optimised to reduce activity at other neurotransmitter systems, the 3-chlorophenyl and phenethyl substitution pattern was found to confer preferential affinity for the dopamine transporter rather than the intended sigma-2 selectivity.
Binding constants reported in the primary literature are 0.04 nM at DAT, 53 nM at 5-HT2, 327 nM at D2-like receptors, 802 nM at SERT and 1,107 nM at NET. That is approximately 20,000-fold selectivity for DAT over SERT and 27,000-fold over NET. Binding at the PCP/NMDA site and at opioid receptors was not detected within the concentration range assayed.
Published characterisation consists of in vitro binding data. No pharmacokinetic, metabolic or in vivo characterisation has been reported, and transporter conformational preference has not been determined for this compound — DAT ligands of comparable affinity differ in the conformational state they stabilise, and that is not inferable from affinity data alone.
Supplied as an analytical reference material for transporter pharmacology. Identity may be matched against CAS 136534-45-7 and InChIKey NKMGWZZAFWDLFG-UHFFFAOYSA-N. Identity and purity are confirmed by third-party COA, and per-lot analytical documentation is published to the COA archive.
Motel WC, Healy JR, Viard E, Pouw B, Martin K, Matsumoto RR, Coop A. Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands. Bioorganic & Medicinal Chemistry Letters. 2013;23(24):6920–6922. doi:10.1016/j.bmcl.2013.09.038
Research Use Disclaimer
Research Use Only Disclaimer: This product is developed and distributed strictly as a Research Use Only (RUO) laboratory reference chemical intended exclusively for non-clinical analytical and scientific investigation. It is not an FDA-approved drug, medical treatment, dietary supplement, or food ingredient, and is strictly prohibited for human or animal consumption. Kimera Chems supplies this research material solely to qualified institutions and professional investigators for authorized laboratory research.
