| Identification | Back Directory | [Name]
Dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 8-chloro-, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide | [CAS]
146033-03-6 | [Synonyms]
SC 51089 free base
Dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 8-chloro-, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide | [Molecular Formula]
C22H19ClN4O3 | [MOL File]
146033-03-6.mol | [Molecular Weight]
422.86 |
| Hazard Information | Back Directory | [Uses]
SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity[1][2][3]. | [in vivo]
SC 51089 free base (40 μg/kg; infused i.p. for 28 d) ameliorates motor coordination and balance dysfunction and rescues long-term memory deficit in R6/1 mouse model of HD[3]. | Animal Model: | R6/1 mouse model of Huntington's disease (HD), from 13 to 18 weeks of age[3] | | Dosage: | 40 μg/kg/day | | Administration: | Infused i.p. at a rate of 0.11 μL/h during 28 days by osmotic mini-pump system | | Result: | Ameliorated motor coordination and balance dysfunction.
Rescued long-term memory deficit.
Improved the expression of specific synaptic markers.
Reduced the number of huntingtin nuclear inclusions in the striatum and hippocampus. |
| [IC 50]
EP1: 1.3 μM (Ki); TP: 11.2 μM (Ki); EP3: 17.5 μM (Ki); FP: 61.1 μM (Ki) | [References]
[1] Abramovitz M, et, al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93. DOI:10.1016/s1388-1981(99)00164-x
[2] Saleem S, et, al. Effects of EP1 receptor on cerebral blood flow in the middle cerebral artery occlusion model of stroke in mice. J Neurosci Res. 2007 Aug 15;85(11):2433-40. DOI:10.1002/jnr.21399
[3] Anglada-Huguet M, et, al. Prostaglandin E2 EP1 receptor antagonist improves motor deficits and rescues memory decline in R6/1 mouse model of Huntington's disease. Mol Neurobiol. 2014 Apr;49(2):784-95. DOI:10.1007/s12035-013-8556-x |
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