| Identification | Back Directory | [Name]
ONO-8130 | [CAS]
459841-96-4 | [Synonyms]
ONO-8130
4-[[[2,3-Dihydro-6-[(2-methylpropyl)[(4-methyl-2-thiazolyl)sulfonyl]amino]-1H-indene-5yl]oxy]methyl]benzoic acid | [Molecular Formula]
C25H28N2O5S2 | [MOL File]
459841-96-4.mol | [Molecular Weight]
500.63 |
| Chemical Properties | Back Directory | [Boiling point ]
705.1±70.0 °C(Predicted) | [density ]
1.344±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤2mg/ml in ethanol;3mg/ml in DMSO;1mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
4.17±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
ONO 8130 is a selective prostanoid EP1 receptor antagonist, which relieves bladder pain in mice with cyclophosphamide-induced cystitis. | [Biological Activity]
ono-8130 is an orally bioavailable and selective antagonist of the prostaglandin e2 (pge2) receptor ep1 with ki value of 1.9 nm [1][2][3].prostaglandins contribute to the sensitization of peripheral and central nociceptive neurons during peripheral inflammation. prostaglandin e2 (pge2) is considered a dominant pronociceptive prostanoid. pge2 receptors are g protein-coupled receptors and classified into 4 general subtypes (ep1, ep2, ep3, and ep4) that are located unevenly in different tissues. ep1 receptors play a major role in processing of pain [1].in cystitis-related bladder pain mice, oral preadministration of ono-8130 at 0.3-30 mg/kg strongly prevented both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent way. ono-8130 at 30 mg/kg also reversed the established cystitis-related bladder pain. ono-8130 also blocked prostaglandin e2 caused prompt phosphorylation of erk in the l6 spinal cord [1]. in the guinea pig trachea (gpt), ono-8130 inhibited the initial contraction mediated by pge2. ono-8130 also eliminated the spontaneous tone [2]. | [in vivo]
ONO-8130 (0.3-30 mg/kg; Oral preadministration, once) strongly prevents both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent manner[1].
ONO-8130 (30 mg/kg; Orally, once) reverses the established cystitis-related bladder pain[1].
ONO-8130 (30 mg/kg; Orally, once) strongly inhibits phosphorylation of ERK in MDH, DCM, and SPN of the L6 spinal cord caused by intravesical administration of PGE2[1]. | Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old)[1] | | Dosage: | 0.3, 3, 10, and 30 mg/kg | | Administration: | Orally, once | | Result: | Strongly prevented both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent manner, but had slight effect on the increased bladder weight and vascular permeability. |
| Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old, established bladder pain caused by IP cyclophosphamide)[1] | | Dosage: | 10, 30 mg/kg | | Administration: | Orally, once (administered 2.75 hours after i.p. cyclophosphamide) | | Result: | Markedly attenuated the bladder pain-like nociceptive behavior and referred hyperalgesia in the acute phase (3.5-4 h after cyclophosphamide). |
| Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old, established bladder pain caused by IP cyclophosphamide)[1] | | Dosage: | 30 mg/kg | | Administration: | Orally, once (administered 4.75 hours after i.p. cyclophosphamide) | | Result: | Significantly suppressed the bladder pain-like nociceptive behavior and tended to reduce the referred hyperalgesia in the persistent phase, 5.5-6 hours after cyclophosphamide. |
| Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old, intravesical administration of PGE2 at 5 nmol/mouse)[1] | | Dosage: | 30 mg/kg | | Administration: | Orally, once | | Result: | Strongly inhibited phosphorylation of ERK in MDH, DCM, and SPN of the L6 spinal cord caused by intravesical administration of PGE2 at 5 nmol/mouse, exerted complete blockade in DCM, while its inhibitory effects in MDH and SPN were partial. |
| [storage]
Store at +4°C | [References]
[1]. miki t, matsunami m, nakamura s, et al. ono-8130, a selective prostanoid ep1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. pain. 2011 jun;152(6):1373-81.
[2]. sfholm j, dahlén se, adner m. antagonising ep1 and ep2 receptors reveal that the tp receptor mediates a component of antigen-induced contraction of the guinea pig trachea. eur j pharmacol. 2013 oct 15;718(1-3):277-82. |
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