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SB-612111 hydrochloride

Names

[ CAS No. ]:
371980-94-8

[ Name ]:
SB-612111 hydrochloride

[Synonym ]:
MFCD12546333
5H-Benzocyclohepten-5-ol, 7-[[4-(2,6-dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-, (5S,7S)-, hydrochloride (1:1)
(5S,7S)-7-{[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl}-1-methyl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ol hydrochloride (1:1)
SB-612111 hydrochloride

Biological Activity

[Description]:

SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[Target]

Ki: 0.33 nM (hORL-1) Ki: 57.6 nM (μ-receptor); 160.5 nM (κ-receptor); 2109 nM (δ-receptor)[1]


[In Vivo]

SB-612111 hydrochloride (intravenous injection; 0.6-10 nmol/mouse) antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED50 of 0.62 mg/kg[1]. SB-612111 hydrochloride (intravenous injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected[1]. Animal Model: Male rats[1] Dosage: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg Administration: Intravenous injection; single dose Result: Had antihyperalgesic effects on carrageenan-induced rat paw.

[References]

[1]. Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).J Pharmacol Exp Ther. 2004 Feb;308(2):454-61.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H30Cl3NO

[ Molecular Weight ]:
454.860

[ Exact Mass ]:
453.139313

Related Compounds