Page last updated: 2024-12-11

metkephamid

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

metkephamid: systemically active analog of methionine enkephalin; RN refers to parent cpd (L-Tyr-D-Ala-Gly-L-Phe)-(L-Met)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5464184
CHEMBL ID2220405
SCHEMBL ID329997
MeSH IDM0091019

Synonyms (19)

Synonym
metkephamid
(2s)-2-[[(2s)-2-[[2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]-methylamino]-4-methylsulfanylbutanamide
66960-34-7
metkefamidum
mnl20fxh9y ,
l-tyrosyl-d-alanylglycyl-l-phenylalanyl-n2-methyl-l-methioninamide
unii-mnl20fxh9y
metkefamida [inn-spanish]
metkefamida
metkefamidum [inn-latin]
metkephamide
metkefamide
metkefamide [inn]
l-methioninamide, l-tyrosyl-d-alanylglycyl-l-phenylalanyl-n2-methyl-
SCHEMBL329997
CHEMBL2220405
AKOS030610296
Q6824163
(s)-2-((s)-2-(2-((r)-2-((s)-2-amino-3-(4-hydroxyphenyl)propanamido)propanamido)acetamido)-n-methyl-3-phenylpropanamido)-4-(methylthio)butanamide

Research Excerpts

Overview

Metkephamid is an analog of methionine enkephalin. It retains high affinity for the delta receptor and is a systemically active analgesic.

ExcerptReferenceRelevance
"Metkephamid is an analog of methionine enkephalin that retains high affinity for the delta receptor and is a systemically active analgesic. "( Metkephamid, a systemically active analog of methionine enkephalin with potent opioid alpha-receptor activity.
Bemis, KG; Frederickson, RC; Shuman, R; Smithwick, EL, 1981
)
3.15
"Metkephamid is an analog of methionine enkephalin. "( Metkephamid and meperidine analgesia after episiotomy.
Barden, TP; Bloomfield, SS; Mitchell, J, 1983
)
3.15

Bioavailability

ExcerptReferenceRelevance
" For YAGFM, the apparent absorption rate was slower than the elimination rate, thus obeying "flip-flop" pharmacokinetics."( Systemic absorption of ocularly administered enkephalinamide and inulin in the albino rabbit: extent, pathways, and vehicle effects.
Carson, LW; Dodda-Kashi, S; Lee, VH; Stratford, RE, 1988
)
0.27
" Based on the permeability data alone and under the assumption of no presystemic metabolism, complete bioavailability would be predicted for metkephamid."( Oral absorption of peptides: the effect of absorption site and enzyme inhibition on the systemic availability of metkephamid.
Amidon, GL; Langguth, P; Merkle, HP, 1994
)
0.7
" In contrast, the fraction of TRH metabolized in the liver was less than 10%, indicating a remarkably low contribution of first-pass metabolism to the bioavailability of TRH."( First-pass metabolism of peptide drugs in rat perfused liver.
Amidon, GL; Langguth, P; Nadai, T; Sakane, T; Sezaki, H; Taki, Y; Yamashita, S, 1998
)
0.3

Dosage Studied

ExcerptRelevanceReference
" Full dose-response curves show a 4-fold shift to the right (P less than ."( Separation of opioid analgesia from respiratory depression: evidence for different receptor mechanisms.
Ling, GS; Lockhart, SH; Pasternak, GW; Spiegel, K, 1985
)
0.27
" In a further series of tests, a 50 mg/kg dose of naloxazone 20 hr prior to the assessment of morphine or metkephamid analgesia in the mouse hot plate test substantially shifted the dose-response curve for morphine to the right, while leaving the dose-response curve for metkephamid unchanged."( Cross-tolerance studies distinguish morphine- and metkephamid-induced analgesia.
Frederickson, RC; Hynes, MD,
)
0.6
" ICI 154,129 was proconvulsant in the mouse picrotoxin potentiation test; the dose-response curve had a low ceiling and was biphasic."( In vivo studies with ICI 154,129, a putative delta receptor antagonist.
Cowan, A; Gmerek, DE,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (26)

TimeframeStudies, This Drug (%)All Drugs %
pre-199016 (61.54)18.7374
1990's10 (38.46)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (10.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]