Table 5.

Inhibitory activity of selected analogs at dopamine transporter^*.

	Structure	% inhibition at 10 μM	Ki, nM		Structure	% inhibition at 10 μM	Ki, nM
4a		82	15	9a		68	405
4b		24	ND	9c		85	43
4l		90	6.5	11a		86	141
4o		76	609	11b		77	399
4r		79	80	13		49	ND
4s		20	ND	14		73	998
4t		58	118	15		26	ND
8a		38	ND	16		33	ND
8b		59	535	17		51	603
8c		75	40	19a		52	1589
8d		64	144	19b		24	ND

In primary screening assays, compounds were tested in triplicate or quadruplicate at a final concentration of 10 μM. Compounds with a minimum of 50% antagonist activity were subjected to secondary screening (dose-response) assays.

^*Receptor binding profiles were generously provided by the National Institute of Mental Health’s Psychoactive Drug Screening Program, Contract # HHSN-271–2013-00017-C (NIMH PDSP). The NIMH PDSP is Directed by Bryan L. Roth MD, Ph.D. at the University of North Carolina at Chapel Hill and Project Officer Jamie Driscoll at NIMH, Bethesda MD, USA. ND− not determined (Ki was not evaluated due to the less than 50% antagonist activity of a compound).