Identification | Back Directory | [Name]
Kelatorphan | [CAS]
92175-57-0 | [Synonyms]
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 | [Molecular Formula]
C14H18N2O5 | [MDL Number]
MFCD09837652 | [MOL File]
92175-57-0.mol | [Molecular Weight]
294.3 |
Chemical Properties | Back Directory | [density ]
1.301±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
3.58±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
Kelatorphan is a full inhibitor of enkephalin degrading enzymes. | [in vivo]
The administration of Kelatorphan alone (50 μg) could result in a strong increase of intact [3H]enkephalin content corresponding to 80±11% of total recovered radioactivity[2]. 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[3]. | [storage]
Store at -20°C | [References]
[1] Waksman G, et al. Kelatorphan: a full inhibitor of enkephalin degrading enzymes. Biochemical and pharmacological properties, regional distribution of enkephalinase in rat brain by use of a tritiated derivative. Neuropeptides. 1985 Feb;5(4-6):529-32. DOI:10.1016/0143-4179(85)90071-x [2] Waksman G, et al. In vitro and in vivo effects of kelatorphan on enkephalin metabolism in rodent brain. Eur J Pharmacol. 1985 Nov 5;117(2):233-43. [3] Boudinot E, et al. Effects of the potent analgesic enkephalin-catabolizing enzyme inhibitors RB101 and kelatorphan on respiration. Pain. 2001 Feb 1;90(1-2):7-13. DOI:10.1016/s0304-3959(00)00382-1 |
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