Benztropine (mesylate)

Benztropine is an antagonist of M₁ muscarinic acetylcholine receptors (K_i = 0.59 nM in rat brain membranes).¹ It is selective for M₁ receptors over the serotonin transporter (K_i = 5,150 nM), however, it also binds to the dopamine transporter and inhibits dopamine reuptake (K_is = 237 and 130 nM, respectively).^1,2,3 Benztropine also inhibits acid sphingomyelinase by 87% when used at a concentration of 10 mM.⁴ Formulations containing benztropine have been used in the management of Parkinson's disease symptoms such as involuntary tremor and dystonia.

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1. Zhang, Y., Joseph, D.B., Bowen, W.D., et al. Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues. J. Med. Chem. 44(23), 3937-3945 (2001).

2. Schmitt, K.C., Zhen, J., Kharkar, P., et al. Interaction of cocaine-, benztropine-, and GBR12909- like compounds with wildtype and mutant human dopamine transporters: Molecular features that differentially determine antagonist binding properties. J. Neurochem. 107(4), 928-940 (2008).

3. Ukairo, O.T., Bondi, C.D., Newman, A.H., et al. Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue. J. Pharmacol. Exp. Ther. 314(2), 575-583 (2005).

4. Kornhuber, J., Muehlbacher, M., Trapp, S., et al. Identification of novel functional inhibitors of acid sphingomyelinase. PLoS One 6(8), e23852 (2011).