Lobelane hydrochloride is a biologically active compound that has the activity of inhibiting vesicular monoamine transporter-2 (VMAT2). Lobelane hydrochloride has a low affinity for nicotinic acetylcholine receptors ( nAChR ), thereby enhancing its selectivity for VMAT2. Synthetic structural changes of lobelane hydrochloride have led to some related analogs that show mild changes in affinity for VMAT2. The most potent synthetic lobelane hydrochloride obtained after structural modification has a K(i) value of 630 nM, showing significant VMAT2 selectivity. The biological activity of lobelane hydrochloride suggests that it has the potential to be used in the development of compounds to inhibit methamphetamine abuse.
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