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92175-57-0

中文名稱 KELATORPHAN
英文名稱 Kelatorphan
CAS 92175-57-0
分子式 C14H18N2O5
分子量 294.3
MOL 文件 92175-57-0.mol
92175-57-0 結(jié)構(gòu)式 92175-57-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T15652
英文別名
Kelatorphan
OJCFZTVYDSKXNM-GXSJLCMTSA-N
N-[(R)-4-(Hydroxyamino)-1,4-dioxo-2-(phenylmethyl)butyl]-L-alanine
(2S)-2-[[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]amino]propanoic acid

物理化學(xué)性質(zhì)

密度1.301±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)3.58±0.10(Predicted)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
Kelatorphan 是腦啡肽降解酶 (enkephalin degrading enzymes) 的全抑制劑。
靶點(diǎn)

Enkephalin degrading enzyme.

體內(nèi)研究

The administration of Kelatorphan alone (50 μg) could result in a strong increase of intact [ 3 H]enkephalin content corresponding to 80±11% of total recovered radioactivity. In normal awake rats, Kelatorphan (10±20 mg/kg i.v.) increases minute-volume. The increase in ventilation is due to a dose-dependent increase in breathing frequency. In arthritic rats Kelatorphan (20 mg/kg i.v.) increases ventilation and there is no significant difference between arthritic and non-arthritic rats. In pentobarbital-anesthetized rats, a slight (116%) but significant increase of respiration is also produced by Kelatorphan (20 mg/kg, n=6) 10±15 min after administration. The effects of Kelatorphan are not antagonized by a pretreatment with a small dose of naloxone (0.2 mg/kg i.v., 15 min before Kelatorphan), but a larger dose (1 mg/kg) significantly antagonized Kelatorphan (20 mg/kg) at 5 and 10 min in awake rats.

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