Drug intelligence / Profile preview

SKF-81,297

Development stage
Preclinical
Modality
Small Molecules
01

Overview

SKF‑81,297 is a potent and selective small molecule agonist of dopamine D1-like receptors (primarily D1 and D5 subtypes). It is widely used in research to study dopaminergic neurotransmission and behavior. The compound has high affinity for the dopamine D1 receptor (Ki ≈ 2 nM) and stimulates motor activity in animal models of Parkinson’s disease. In addition to its primary action as a D1 receptor agonist—mediating excitatory neurotransmission—it has been shown to modulate NMDA receptor currents independently of D1 activation at certain concentrations. This off-target effect may have implications for interpreting experimental results using this compound[1][3][4][7]. SKF‑81,297 is not approved for clinical use; it is used exclusively as a research tool.

Other names
6-Chloro-2,3,4,5-tetrahydro-1-phenyl-1H-3-benzazepine-7,8-diol(R)-6-chloro-1-phenyl-2,3,4,5-tetrahydro-benzo[d]azepine hydrobromide
02

Targets

DRD1 (Dopamine D1 Receptor)NMDAR (Glutamate receptor ionotropic, NMDA)DRD5 (Dopamine D5 Receptor)

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