Drug intelligence / Profile preview

SB-612111

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intraperitoneal, Topical (direct To Cortex In Animal Studies)
01

Overview

**SB-612111** is a potent and highly selective nonpeptide antagonist of the **nociceptin receptor** (also known as the **NOP receptor** or ORL-1). It binds to the NOP receptor with high affinity and selectivity, blocking its activation by endogenous ligands such as nociceptin/orphanin FQ. SB-612111 has been shown in preclinical studies to inhibit the development of hyperalgesia (increased pain sensitivity), reduce binge eating of high-fat diets, and exert antidepressant-like effects. It does not possess significant analgesic (pain-relieving) effects by itself. The drug has also been studied for its ability to improve cerebral blood flow after traumatic brain injury and to modulate neurobehavioral responses[1][2][3][4][5].

Other names
(−)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol
02

Targets

NOP (Nociceptin/orphanin FQ peptide receptor)

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