7-hydroxy DPAT (hydrobromide)

7-hydroxy DPAT is a dopamine D₃ receptor agonist.¹ It selectively binds to the dopamine D₃ over the D₂, D₁, and D₄ receptors (K_is = 0.78, 61, 650, and 5,300 nM, respectively, in radioligand binding assays). 7-hydroxy DPAT increases calcium mobilization in HEK293 cells expressing the D₃ receptor with an EC₅₀ value of 13.5 nM in a FLIPR assay.² It decreases the release of striatal dopamine and its metabolite 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) in rats when administered intraperitoneally at a dose of 0.25 mg/kg.³ 7-hydroxy DPAT (2 µg/µl for eight weeks, i.c.v.) reduces the loss of ipsilateral substantia nigra pars compacta (SNC) dopaminergic neurons in a rat model of Parkinson's disease induced by 6-OHDA (Item No. 25330).⁴ It also decreases amphetamine-induced ipsilateral rotations and increases the number of steps reached with the contralateral paw in the staircase test in the same model.

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1. Lévesque, D., Diaz, J.A., Pilon, C., et al. Identification, characterization, and localization of the dopamine D₃ receptor in rat brain using 7-[³H]hydroxy-N,N-di-n-propyl-2-aminotetralin. Proc. Natl. Acad. Sci. USA 89(17), 8155-8159 (1992).

2. Moreland, R.B., Nakane, M., Donnelly-Roberts, D., et al. Comparative pharmacology of human dopamine D₂-like receptor stable cell lines coupled to calcium flux through Gɑqo5. Biochem. Pharmacol. 68(4), 761-772 (2004).

3. Mulder, T.B.A., de Vries, J.B., Dijkstra, D., et al. Further in vitro and in vivo studies with the putative presynaptic dopamine agonist N,N-dipropyl-7-hydroxy-2-aminotetralin. Naunyn Schmiedebergs Arch. Pharmacol. 336(5), 494-501 (1987).

4. Van Kampen, J.M., and Eckman, C.B. Dopamine D₃ receptor agonist delivery to a model of Parkinson’s disease restores the nigrostriatal pathway and improves locomotor behavior. J. Neurosci. 26(27), 7272-7280 (2006).