Page last updated: 2024-12-04

phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)threoninamide

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

Description

phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)threoninamide: cyclic somatostatin octapeptide analog with high affinity & selectivity toward mu opioid receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2884
SCHEMBL ID1239661
MeSH IDM0141458

Synonyms (12)

Synonym
ctop
ctopa
l-threoninamide, d-phenylalanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-ornithyl-l-threonyl-3-mercapto-l-valyl-, cyclic (2-7)-disulfide
ctop-nh2
phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)threoninamide
L000207
103429-31-8
n-(1-amino-3-hydroxy-1-oxobutan-2-yl)-19-[(2-amino-3-phenylpropanoyl)amino]-10-(3-aminopropyl)-7-(1-hydroxyethyl)-16-[(4-hydroxyphenyl)methyl]-13-(1h-indol-3-ylmethyl)-3,3-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbox
C20160
SCHEMBL1239661
fcywxtxt
phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Due to low central nervous system (CNS) bioavailability of delta-opioid peptides, little is known about the effect of systemic administration of delta-opioid receptor ligands."( Spinal delta-opioid receptors mediate suppression of systemic SNC80 on excitability of the flexor reflex in normal and inflamed rat.
Cao, CQ; Dray, A; Hong, Y; Perkins, M, 2001
)
0.31
" They may open new perspectives for the development of opiorphin analogues with greater bioavailability and physicochemical characteristics in the pursuit of new medications for the treatment of panic disorder."( Opiorphin causes a panicolytic-like effect in rat panic models mediated by μ-opioid receptors in the dorsal periaqueductal gray.
Audi, EA; Bonfim, AJ; Graeff, FG; Kitayama, M; Maraschin, JC; Rangel, MP; Zangrossi, H, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
" Diazoxide (2 microg/mouse) shifted morphine's dose-response curve 47-fold, while levcromakalim (0."( ATP-gated K(+) channel openers enhance opioid antinociception: indirect evidence for the release of endogenous opioid peptides.
Lohmann, AB; Welch, SP, 1999
)
0.3
" The failure of naloxone to completely antagonize the effect of the higher concentration of EM-1 or EM-2 could be due to insufficient dosage or might indicate the involvement of non-opiate receptor mechanisms."( Effect of endomorphin on somatostatin secretion in the isolated perfused rat stomach.
Allescher, HD; Lippl, F; Schusdziarra, V,
)
0.13
" In the presence of fixed doses of 1 or 10 microg CTAP, increasing doses of naltrexone produced dose-dependent shifts to the right in the morphine dose-response curve."( In vivo pharmacological resultant analysis reveals noncompetitive interactions between opioid antagonists in the rat tail-withdrawal assay.
Walker, EA, 2006
)
0.33
" Subclinical MOR activation (10 nM DAMGO) produced a leftward shift in (D-Ala2)-Deltorphin II dose-response curve in non-ligated rats (IC50 16."( Depression of C fibre-evoked spinal field potentials by the spinal delta opioid receptor is enhanced in the spinal nerve ligation model of neuropathic pain: involvement of the mu-subtype.
Aguilera, L; Aira, Z; Azkue, JJ; Bilbao, J; Buesa, I; Mozas, M; Salgueiro, M; Urrutia, A; Zimmermann, M, 2008
)
0.35
" These effects were not associated with alterations in ethanol pharmacokinetic properties or with shifts in the biphasic ethanol dose-response curve."( Ethanol-induced social facilitation in adolescent rats: role of endogenous activity at mu opioid receptors.
Spear, LP; Varlinskaya, EI, 2009
)
0.35
" The same sequence of experiments was repeated in the isolated heart model using the maximal protective dose of remifentanil from the dose-response studies."( Remifentanil post-conditioning attenuates cardiac ischemia-reperfusion injury via kappa or delta opioid receptor activation.
Irwin, MG; Jiang, LL; Li, R; Wong, GT, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (221)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (3.17)18.7374
1990's82 (37.10)18.2507
2000's78 (35.29)29.6817
2010's50 (22.62)24.3611
2020's4 (1.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.20

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.20 (24.57)
Research Supply Index5.42 (2.92)
Research Growth Index5.62 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other225 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]