O-2172 is a drug developed by
Organix Inc, which acts as a
stimulant and potent
dopamine reuptake inhibitor. It is an analogue of
methylphenidate where the
phenyl ring has had a 3,4-dichloro substitution added, and the
piperidine ring has been replaced by
cyclopentane. It is around 1/3 the potency of
methylphenidate, demonstrating that even with the important binding group of the nitrogen lone pair removed entirely, selective
DAT binding and reuptake inhibition is still possible.[1][2]
^Meltzer PC, Wang P, Blundell P, Madras BK (April 2003). "Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate". Journal of Medicinal Chemistry. 46 (8): 1538–45.
doi:
10.1021/jm0205292.
PMID12672255.
^Runyon SP, Carroll FI (2006). "Dopamine transporter ligands: recent developments and therapeutic potential". Current Topics in Medicinal Chemistry. 6 (17): 1825–43.
doi:
10.2174/156802606778249775.
PMID17017960.
O-2172 is a drug developed by
Organix Inc, which acts as a
stimulant and potent
dopamine reuptake inhibitor. It is an analogue of
methylphenidate where the
phenyl ring has had a 3,4-dichloro substitution added, and the
piperidine ring has been replaced by
cyclopentane. It is around 1/3 the potency of
methylphenidate, demonstrating that even with the important binding group of the nitrogen lone pair removed entirely, selective
DAT binding and reuptake inhibition is still possible.[1][2]
^Meltzer PC, Wang P, Blundell P, Madras BK (April 2003). "Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate". Journal of Medicinal Chemistry. 46 (8): 1538–45.
doi:
10.1021/jm0205292.
PMID12672255.
^Runyon SP, Carroll FI (2006). "Dopamine transporter ligands: recent developments and therapeutic potential". Current Topics in Medicinal Chemistry. 6 (17): 1825–43.
doi:
10.2174/156802606778249775.
PMID17017960.