3,4-Dichloromethylphenidate (also known as 3,4-CTMP or 3,4-DCMP)[1] is a
stimulant drug related to
methylphenidate. Dichloromethylphenidate is a potent psychostimulant that acts as both a
dopamine reuptake inhibitor and
norepinephrine reuptake inhibitor, meaning it effectively boosts the levels of the norepinephrine and dopamine neurotransmitters in the brain, by binding to, and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft.
3,4-DCMP, the threo-diastereomer, is approximately seven times more potent than methylphenidate in animal studies, but has weaker reinforcing effects due to its slower onset of action.[2][3][4][5][6] However, H. M. Deutsch's discrimination ratio[clarification needed] implies it to be more reinforcing than
cocaine.[4]
Legality
As of October 2015 3,4-CTMP is a controlled substance in China.[7]
^Deutsch HM, Shi Q, Gruszecka-Kowalik E, Schweri MM (March 1996). "Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs". Journal of Medicinal Chemistry. 39 (6): 1201–9.
doi:
10.1021/jm950697c.
PMID8632426.
^
abSchweri MM, Deutsch HM, Massey AT, Holtzman SG (May 2002). "Biochemical and behavioral characterization of novel methylphenidate analogs". The Journal of Pharmacology and Experimental Therapeutics. 301 (2): 527–35.
doi:
10.1124/jpet.301.2.527.
PMID11961053.
^Davies HM, Hopper DW, Hansen T, Liu Q, Childers SR (April 2004). "Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites". Bioorganic & Medicinal Chemistry Letters. 14 (7): 1799–802.
doi:
10.1016/j.bmcl.2003.12.097.
PMID15026075.
^Kim DI, Deutsch HM, Ye X, Schweri MM (May 2007). "Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate". Journal of Medicinal Chemistry. 50 (11): 2718–31.
doi:
10.1021/jm061354p.
PMID17489581.
^"关于印发《非药用类麻醉药品和精神药品列管办法》的通知" (in Chinese). China Food and Drug Administration. 27 September 2015. Archived from
the original on 1 October 2015. Retrieved 1 October 2015.