Drug intelligence / Profile preview

SK&F-89124

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Experimental (not Established For Clinical Use; No Marketed Route; Used In Research Ex Vivo And Animal Models)
01

Overview

SK&F-89124 is a **potent and selective agonist at peripheral inhibitory prejunctional dopamine receptors (DA2 receptors)**. It is a synthetic small molecule structurally related to N,N-di-n-propyldopamine (DPDA), but with the meta-hydroxyl replaced by a cyclic amide function. It is at least an order of magnitude more potent than DPDA at DA2 receptors. Mechanistically, it inhibits norepinephrine release via DA2 receptor activation and demonstrates high selectivity for dopamine D2-like receptors with little or no activity at dopamine D1, alpha 2-adrenoceptors, or H2-histamine receptors. It has been mainly used as a research tool for studying DA2 receptor function[1][3][6].

Other names
4-(2-di-n-propylaminoethyl)-7-hydroxy-2(3H)indolone4-(2-di-n-propylaminoethyl)-7-hydroxy-2(3H)-indolone hydrobromide7-Hydroxy ropinirole (bromide)7-Hydroxy Ropinirole HBr
02

Targets

DRD3 (Dopamine receptor D3)DRD2 (Dopamine D2 Receptor)

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