It is slightly less potent than methylphenidate and has relatively low efficacy at blocking dopamine reuptake despite its high binding affinity, which led to its investigation as a possible substitute drug for treatment of stimulant abuse (cf.

[1] On the other hand, several other simple ring-substituted derivatives of threo-methylphenidate such as the 4-fluoro and 3-chloro compounds are more potent than methylphenidate both in efficacy as dopamine reuptake inhibitors and in animal drug discrimination assays.

[2][3][4] 4-Methylmethylphenidate was banned in the UK as a Temporary Class Drug from June 2015 following its unapproved sale as a designer drug.

[5][6][7] In the United States, 4-methylmethylphenidate may be considered illegal if intended for human consumption under the federal analogue act as a structural analog of methylphenidate.

In the United States, on September 22, 2023, the DEA filed a proposed rule for placement of ethylphenidate into Schedule I status, which would include its isomers.