Kelatorphan

Modify Date: 2024-01-09 10:32:38

Kelatorphan Structure
Kelatorphan structure
Common Name Kelatorphan
CAS Number 92175-57-0 Molecular Weight 294.30300
Density 1.301g/cm3 Boiling Point N/A
Molecular Formula C14H18N2O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Kelatorphan


Kelatorphan is a full inhibitor of enkephalin degrading enzymes.

 Names

Name (2S)-2-[[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]amino]propanoic acid
Synonym More Synonyms

 Kelatorphan Biological Activity

Description Kelatorphan is a full inhibitor of enkephalin degrading enzymes.
Related Catalog
Target

Enkephalin degrading enzyme[1].

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].
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.

[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.

 Chemical & Physical Properties

Density 1.301g/cm3
Molecular Formula C14H18N2O5
Molecular Weight 294.30300
Exact Mass 294.12200
PSA 115.73000
LogP 1.11190
Index of Refraction 1.567

 Safety Information

Hazard Codes Xi

 Synonyms

kelatorphan
L-Alanine,N-(4-(hydroxyamino)-1,4-dioxo-2-(phenylmethyl)butyl)-,(R)
(3-(N-Hydroxy)carboxamido-2-benzylpropanoyl)alanine
n-[(2r)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]-l-alanine
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