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enkephalin, leucine

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Description

Leucine enkephalin is a naturally occurring opioid peptide that is found in the brain and spinal cord. It is a pentapeptide with the amino acid sequence Tyr-Gly-Gly-Phe-Leu. Leucine enkephalin is synthesized from a precursor protein called proenkephalin. It is believed to be involved in the modulation of pain perception, as well as other physiological processes such as mood, stress, and addiction. Leucine enkephalin exerts its effects by binding to opioid receptors, particularly the delta opioid receptor. It is studied because of its potential role in pain management, as well as its involvement in the development of opioid addiction. Research is ongoing to develop synthetic enkephalin analogs that have improved analgesic properties and fewer side effects.'

Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Leu-enkephalin : A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
GlycinegenusA non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.[MeSH]FabaceaeThe large family of plants characterized by pods. Some are edible and some cause LATHYRISM or FAVISM and other forms of poisoning. Other species yield useful materials like gums from ACACIA and various LECTINS like PHYTOHEMAGGLUTININS from PHASEOLUS. Many of them harbor NITROGEN FIXATION bacteria on their roots. Many but not all species of beans belong to this family.[MeSH]

Cross-References

ID SourceID
PubMed CID461776
CHEMBL ID218452
CHEMBL ID8234
CHEBI ID89656
SCHEMBL ID631959
MeSH IDM0007454
PubMed CID3903
CHEBI ID91634
SCHEMBL ID631958
MeSH IDM0007454

Synonyms (110)

Synonym
enkephalins
58822-25-6
leucine-enkephalin
einecs 261-457-1
nsc 350588
ccris 6338
enkephalin, leucine
n-(n-(n-(n-l-tyrosylglycyl)glycyl)-l-phenylalanyl)-l-leucine
leu-enkephalin
tyrglyglypheleu
[leu 5]enkephalin
l-leucine, n-(n-(n-(n-l-tyrosylglycyl)glycyl)-l-phenylalanyl)-
[leu]enkephalin
NCGC00167126-01
tyr-gly-gly-phe-leu
bdbm50128075
chembl218452
tyr-gly-pro-phe-leu-arg-arg-ile-arg-arg-lys-nh2
(2s)-2-[[(2s)-2-[[2-[[2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid
[leu5]-enkephalin ,
CHEMBL8234 ,
chebi:89656 ,
enkephalin
leucine- enkephalin
(enkephalin)2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid
2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid
leu5-enkephalin
([leu]-enkephalin)2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid
2-[1-[1-amino-2-(4-hydroxyphenyl)-(1s)-ethylcarboxamidomethylcarboxamidomethylcarboxamido]-2-phenyl-(1s)-ethylcarboxamido]-4-methyl-(2s)-pentanoic acid
tyr-gly-gly-phe-leu-oh
2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid(enkephalin)
2-{1-[1-amino-2-(4-hydroxyphenyl)ethylcarboxamidomethylcarboxamidomethylcarboxamido]-2-phenylethylcarboxamido}-4-methylpentanoic acid
bdbm50001465
(s)-2-[(s)-2-(2-{2-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid
2-[(s)-2-(2-{2-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-1-oxo-3-phenyl-propylamino]-4-methyl-pentanoic acid
2-[(s)-2-(2-{2-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid
14-18-6
59141-40-1
leucyl-enkephalin
ri01r707r6 ,
unii-ri01r707r6
enkephalin l
[5-leucine]enkephalin
sh-pentapeptide-5 [inci]
l-leucine, l-tyrosylglycylglycyl-l-phenylalanyl-
pentapeptide-5 [inci]
sh-pentapeptide-5
ici-114740
sm-peptide-1
pentapeptide-5
SCHEMBL631959
ici 114740
dynorphin-(1-5)
AKOS024456832
mfcd00076406
(2s)-2-[(2s)-2-(2-{2-[(2s)-2-amino-3-(4-hydroxyphenyl)propanamido]acetamido}acetamido)-3-phenylpropanamido]-4-methylpentanoic acid
l-enk
[leu(5)]enkephalin
leu-enk
y-g-g-f-l
h-tyr-gly-gly-phe-leu-oh
l-tyrosylglycylglycyl-l-phenylalanyl-l-leucine
[leu(5)]-enkephalin
leuenk
l-tyr-gly-gly-l-phe-l-leu
HY-P0288
URLZCHNOLZSCCA-VABKMULXSA-N
DTXSID00905127
(2s,5s,14s)-14-amino-5-benzyl-15-(4-hydroxyphenyl)-2-isobutyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecan-1-oic acid
Q6533903
leu-enkephalin;leucine enkephalin;leucyl-enkephalin
(2s)-2-[[(2s)-2-[[2-[[2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]
leu-enkephalin; leucine enkephalin; leucyl-enkephalin
MS-30127
[leu]-enkephalin
gtpl1613
KBIO1_001010
DIVK1C_001010
nsc-350588
14-amino-5-benzyl-15-(4-hydroxyphenyl)-2-isobutyl-4,10,13-tetraoxo-3,6,9,12-tetraazapentadecan-1-oic acid
nsc350588
SPECTRUM_001429
SMP1_000176
IDI1_001010
SPECTRUM5_000656
NCGC00178398-01
BSPBIO_002902
leucine enkephalin
KBIOGR_001316
KBIO2_004477
KBIO2_007045
KBIO2_001909
KBIOSS_001909
KBIO3_002402
SPECTRUM2_001177
NINDS_001010
SPECTRUM3_001521
SPECTRUM4_001048
SPBIO_001193
L000867
HMS503I21
2-[[2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid
CCG-40269
BRD-A32836748-001-01-1
SCHEMBL631958
yggfl
CHEBI:91634
FT-0770723
Q27080195
1-5-b-neoendorphin (human)

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Naltrexone (10 mg/kg, ip) given 5 min before pentobarbital did not alter the LD50 of the latter."( Studies of the possible role of brain endorphins in pentobarbital anesthesia and toxicity in mice.
Bhargava, HN, 1979
)
0.26
" Thus, the toxic effects were structure selective but not mediated through opioid receptors."( Cytotoxic effects of dynorphins through nonopioid intracellular mechanisms.
Aguilar-Santelises, M; Bakalkin, G; Cebers, G; Gileva, I; Hauser, KF; Hoon Goh, B; Reznikov, K; Tan-No, K; Terenius, L; Yakovleva, T, 2001
)
0.31
" R6W and wt Dyn A peptides were most toxic to primary cerebellar neurons."( Altered secondary structure of Dynorphin A associates with loss of opioid signalling and NMDA-mediated excitotoxicity in SCA23.
Bakalkin, G; Dooley, C; Marrink, SJ; McLaughlin, J; Melo, MN; Reits, E; Sinke, RJ; Smeets, CJ; Stargardt, A; Verbeek, DS; Zmorzyńska, J, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
"8 ml/min per kg, the mean circulating half-life was 52 min and the mean volume of distribution was 190 ml/kg."( Metabolic clearance rate in sheep of a met-enkephalin analogue estimated by radioimmunoassay.
Bolton, JE; Donald, RA; Livesey, JH, 1982
)
0.26
" Pharmacokinetic synergism promotes the accumulation of lithium in brain tissues during cerebrolysin treatment."( [Pharmacokinetic and pharmacodynamic synergism between neuropeptides and lithium in the neurotrophic and neuroprotective action of cerebrolysin].
Alexandrova, OP; Demidov, VI; Genrikhs, EE; Gogoleva, IV; Gromova, OA; Isaev, NK; Khaspekov, GL; Pronin, AV; Stelmashuk, EV; Torshin, IY; Volkov, AY, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
" An in vitro autoradiographic (ARG) method for [3H]-norepinephrine (NE) or [3H]-dopamine (DA) was combined with a post-embedding immunogold cytochemical technique for Met-enkephalin (Met-enk) in colchicine-treated animals."( Catecholamine innervation of enkephalinergic neurons in guinea pig hypothalamus: demonstration by an in vitro autoradiographic technique combined with a post-embedding immunogold method.
Beauvillain, JC; Mazzuca, M; Mitchell, V; Poulain, P, 1988
)
0.27
" The ability of intrathecally administered clonidine alone or in combination with morphine, DPDPE, or U50,488H to alter thresholds for the production of the visceromotor response was examined."( Visceral antinociceptive effects of spinal clonidine combined with morphine, [D-Pen2, D-Pen5] enkephalin, or U50,488H.
Collins, JG; Harada, Y; Kishikawa, K; Kitahata, LM; Nishioka, K, 1995
)
0.29
" A post-embedding immunogold cytochemical technique for Leu-enk, CHH and the CHH neurohormone related moult inhibiting hormone (MIH) was combined with a scintillator intensified autoradiographic method to demonstrate binding of the opioid antagonist [3H] naloxone."( Autoradiographic localization of opioid binding sites combined with immunogold detection of Leu-enkephalin, crustacean hyperglycaemic hormone and moult inhibiting hormone at the electron microscopic level in the sinus gland of the shore crab, Carcinus mae
Hanke, J; Jaros, PP; Willig, A, 1993
)
0.29
" Using in situ hybridization combined with ABC immunocytochemistry for serotonin (5-HT) in the same pineal sections, the PPEnk mRNA labeling cells are found not to be serotonin-immunoreactive cells."( Cells expressing preproenkephalin mRNA in the rat pineal gland are not serotonin-producing pinealocytes: evidence using in situ hybridization combined with immunocytochemistry for serotonin.
Pappas, GD; Sagen, J; Unnerstall, JR; Wang, XT, 1996
)
0.29
" The purpose of the present study was to determine the effect of natural sunlight combined with salt water bathing in the Dead Sea on the methionine-enkephalin (e."( Increased levels of enkephalin following natural sunlight (combined with salt water bathing at the Dead Sea) and ultraviolet A irradiation.
Avrach, WW; Hansen, ES; Kragballe, K; Nissen, JB; Stengaard-Pedersen, K, 1998
)
0.3

Bioavailability

ExcerptReferenceRelevance
" administration, large amounts of [3H]DPDPE were found in the small intestine and flush, but not until 60 min postadministration, suggesting a slower rate of absorption from the site of administration."( Whole body and brain distribution of [3H]cyclic [D-Pen2,D-Pen5] enkephalin after intraperitoneal, intravenous, oral and subcutaneous administration.
Davis, TP; Greene, DL; Hruby, VJ; Porreca, F; Weber, SJ; Yamamura, HI, 1992
)
0.28
"The peptidase-resistance and bioavailability of BUBU [H-Tyr-D."( Brain passage of BUBU, a highly selective and potent agonist for delta opioid receptors: in vivo binding and mu versus delta receptors occupancy.
Baamonde, A; Delay-Goyet, P; Gacel, G; Morgat, JL; Roques, BP; Ruiz-Gayo, M, 1991
)
0.28
" All these data emphasize the interest in developing delta-agonists and mixed inhibitors with appropriate bioavailability for clinical evaluation."( Novel approaches in the development of new analgesics.
Baamonde, A; Calenco, G; Coric, P; Daugé, V; Fournié-Zaluski, MC; Gacel, G; Roques, BP; Turcaud, S, 1990
)
0.28
"Aminopeptidase inhibitors may be useful for improving the systemic bioavailability of peptide drugs administered nasally or by other routes."( Recovery of rat nasal mucosa from the effects of aminopeptidase inhibitors.
Aungst, BJ; Hussain, MA; Koval, CA; Shenvi, AB, 1990
)
0.28
" Bioavailability was estimated following intramuscular (i/m) and intranasal (i/n) routes of administration of 3H-dalargin in anesthetized dogs."( [Bioavailability of dalargin and its metabolism during intranasal administration to rats].
Kalenikova, EI; Sokolov, AS; Vinogradov, VA, 1988
)
0.27
" Absorption studies were performed to determine the absorption rate of DGGFL, by measuring percentage recovery of nasal doses vs time."( Nasal mucosal metabolism and absorption of pentapeptide enkephalin analogs having varying N-terminal amino acids.
Aungst, BJ; Hussain, MA; Kettner, CA; Seetharam, R; Wilk, RR, 1995
)
0.29
" As a 'profile' of pharmacological actions of enkephalin-degrading enzymes emerges, it is becoming apparent that bioavailability rather than a high degree of specificity or inhibitory potency may be the most important factor."( Inhibitors of enkephalin-degrading enzymes as potential therapeutic agents.
Patel, A; Sewell, RD; Smith, HJ, 1993
)
0.29
"Based on the physicochemical and pharmacological properties of drugs having an adamantane skeleton, an adamantane-based moiety was evaluated as a drug carrier for poorly absorbed compounds, including peptides, active towards the central nervous system (CNS)."( Synthesis and antinociceptive activity of [D-Ala2]Leu-enkephalin derivatives conjugated with the adamantane moiety.
Futaki, S; Hama, T; Hibi, T; Kitagawa, K; Konishi, R; Mizobuchi, N, 1997
)
0.3
" The absorption rate (clearance) of CcpLEamide was comparable with that of CcpLE in the presence of these peptidase inhibitors."( Intestinal absorption and analgesic activity of aminopeptidase-resistant cellobiose-coupled leucine enkephalinamide.
Awazu, S; Mizuma, T; Ohta, K, 1998
)
0.3
" The improved analgesia profile shown by the glycosylated peptide is due in part to an improvement in bioavailability to the central nervous system."( Improved blood-brain barrier penetration and enhanced analgesia of an opioid peptide by glycosylation.
Davis, TP; Egleton, RD; Huber, JD; Mitchell, SA; Palian, MM; Polt, R, 2001
)
0.31
" Regional differences in bioavailability (F), first-pass metabolism, and absorption rate were found for TArPP after delivery to the respiratory tract."( Regional differences in bioavailability of an opioid tetrapeptide in vivo in rats after administration to the respiratory tract.
Bengtsson, UH; Eirefelt, S; Ekström, G; Forsmo-Bruce, H; Krondahl, E; Lennernäs, H; Tronde, A, 2002
)
0.31
" The inclusion of aminopeptidase inhibitors in buccal bioadhesive delivery systems could improve buccal bioavailability of Leu-enkephalin."( Peptidase activity on the surface of the porcine buccal mucosa.
Bernkop-Schnürch, A; Langoth, N; Walker, GF, 2002
)
0.31
" Our results provide information which could lead to the rational design of agents capable to modulate the bioavailability of enkephalin and other endogenous aminopeptidase-degraded peptides believed to be involved in the etiology and/or pathophysiology associated with various disease conditions."( In vitro human plasma leucine(5)-enkephalin degradation is inhibited by a select number of drugs with the phenothiazine molecule in their chemical structure.
Diamond, S; Mosnaim, AD; Puente, J; Saavedra, R; Wolf, ME, 2003
)
0.32
" To increase the stability and bioavailability of MERF, new synthetic derivatives with D-amino acid substitutions were prepared and studied."( Synthesis and binding characteristics of a novel enkephalin analogue, [3H]Tyr-D-Ala-Gly-Phe-D-Nle-Arg-Phe.
Benyhe, S; Borsodi, A; Farkas, J; Tóth, F; Tóth, G; Wollemann, M, 2003
)
0.32
" These results provide additional support for the utility of glycosylation to increase central nervous system bioavailability of small peptides and compliment our ongoing stability and blood-brain barrier penetration studies."( Antinociceptive structure-activity studies with enkephalin-based opioid glycopeptides.
Bilsky, EJ; Davis, P; Dhanasekaran, M; Egleton, RD; Elmagbari, NO; Hruby, VJ; Keyari, CM; Lowery, JJ; Navratilova, E; Palian, MM; Polt, R; Porreca, F; Schmid, WR; Yamamura, HI, 2004
)
0.32
"In an effort to improve the bioavailability of the non-selective, cyclic enkephalin analogues H-Dmt-c[d-Cys-Gly-Phe-d(or L)-Cys]NH(2) (Dmt = 2',6'-dimethyltyrosine), analogues N-methylated at the Phe(4) and/or Cys(5) residue were synthesized."( N-methylated cyclic enkephalin analogues retain high opioid receptor binding affinity.
Berezowska, I; Chung, NN; Lemieux, C; Schiller, PW; Weltrowska, G; Wilkes, BC, 2010
)
0.36
"Phosphorylation of l-serine-containing enkephalin analogs has been explored as an alternative to glycosylation in an effort to increase blood-brain barrier permeability and CNS bioavailability of peptide pharmacophores."( Phosphorylation of enkephalins: NMR and CD studies in aqueous and membrane-mimicking environments.
Abrell, L; Bidlack, JM; Bilsky, EJ; Knapp, BI; Lin, G; Lowery, JJ; Martinez, HN; Muthu, D; Polt, R; Strom, K; Yeomans, L, 2011
)
0.37
"Glycosylation by simple sugars is a drug discovery alternative that has been explored with varying success for enhancing the potency and bioavailability of opioid peptides."( Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides.
Arévalo, JC; Arsequell, G; Barreto-Valer, K; Calle, LP; Gonzalez-Nunez, V; Jiménez-Barbero, J; Marcelo, F; Rodríguez, RE; Rosa, M; Sánchez-Sánchez, J; Valencia, G, 2017
)
0.46
" In analogy to nonpeptidic small-molecule counterparts, they can sometimes suffer from disadvantages such as their low bioavailability and poor metabolic stability."( Oxetanyl Amino Acids for Peptidomimetics.
Carreira, EM; Möller, GP; Müller, S; Schepmann, D; Wolfrum, S; Wolfstädter, BT; Wünsch, B, 2017
)
0.46

Dosage Studied

ExcerptRelevanceReference
"05) without affecting exogenously applied acetylcholine dose-response curves."( Role of K+ channels in the modulation of cholinergic neural responses in guinea-pig and human airways.
Barnes, PJ; Belvisi, MG; Miura, M; Stretton, CD; Yacoub, MH, 1992
)
0.28
" This observation can be interpreted as indication that within this dosage range there is an absence of morphine-like subjective effects."( Analogs of the delta opioid receptor selective cyclic peptide [2-D-penicillamine,5-D-penicillamine]-enkephalin: 2',6'-dimethyltyrosine and Gly3-Phe4 amide bond isostere substitutions.
Anthony, E; Beardsley, PM; Chandrakumar, NS; Drury, B; Lopez, OT; Reichman, M; Savage, MA; Stapelfeld, A; Williamson, LN, 1992
)
0.28
" Different potencies in stimulating the low Km GTPase was observed at sub-maximal agonist concentrations, although the shallow dose-response behavior did not allow accurate determination of ED50s."( Assessment of delta-opioid receptor activation by a series of peptides in cultured cells.
Costa, EM; Hoffman, BB; Loew, GH, 1992
)
0.28
" 1) In the presence of a fixed dose of DPDPE (150 nmol), there was a left shift in the dose-response curve of the mu agonist, with the magnitude of the shifts being greater than those anticipated from a simple additive interaction: PL017 (31-fold) > or = DAMGO (20-fold) > morphine (6."( Isobolographic and dose-response analyses of the interaction between intrathecal mu and delta agonists: effects of naltrindole and its benzofuran analog (NTB).
Malmberg, AB; Yaksh, TL, 1992
)
0.28
" We now report that LiCl pretreatment shifted the antinociceptive dose-response curve produced by the opioid agonists morphine, [D-Ala2, MePhe4, Gly5-ol]enkephalin (DAMGO) and sufentanil in inverse order of their intrinsic efficacy."( Opioid efficacy is linked to the LiCl-sensitive, inositol-1,4,5-trisphosphate-restorable pathway.
Connelly, CD; Martinez, RP; Raffa, RB, 1992
)
0.28
" agonist dose-response curves by theophylline (i."( Involvement of adenosine in antinociception produced by spinal or supraspinal receptor-selective opioid agonists: dissociation from gastrointestinal effects in mice.
DeLander, GE; Mosberg, HI; Porreca, F, 1992
)
0.28
" The opioid antagonist naloxone and the alpha-2 adrenergic antagonist idazoxan were given as intrathecal pretreatments at doses chosen to shift the dose-response curves of their corresponding agonist (given alone) 4- to 10-fold to the right; this always resulted in a smaller, but significant (2- to 4-fold) shift in the dose-response curve of the other agonist given alone."( Spinal interactions between opioid and noradrenergic agonists in mice: multiplicativity involves delta and alpha-2 receptors.
Hylden, JK; Kitto, K; Lei, S; Roerig, SC; Wilcox, GL, 1992
)
0.28
" It was found that Tyr-Gly-Gly (16 and 53 micrograms/kg) and [leu]enkephalin (30 and 100 micrograms/kg) administered in this fashion both significantly impaired retention; the dose-response functions for both peptides were U-shaped."( [Leu]enkephalin and its metabolite, Tyr-Gly-Gly, impair active avoidance retention.
Martinez, JL; Schulteis, G, 1992
)
0.28
" The enkephalin dose-response line was shifted to the right, considered a sign of the development of cross-tolerance."( Oxytocin blocks the development of heroin-enkephalin cross-tolerance in mice.
Kovács, GL; Kriván, M; Sarnyai, Z; Szabó, G; Telegdy, G, 1992
)
0.28
" Interleukin-1 beta also regulated a proenkephalin-chloramphenicol acetyltransferase fusion gene transiently transfected into astrocytes, with a dose-response similar to that active in proenkephalin mRNA."( Interleukin-1 beta regulates proenkephalin gene expression in astrocytes cultured from rat cortex.
Callegaro, L; Facci, L; Negro, A; Skaper, SD; Tavella, A, 1992
)
0.28
" The mid-points of the dose-response curves for (1)-naloxone and (d)-naloxone were 10 micrograms/kg and 100 micrograms/kg, respectively."( Significance of an opiate mechanism in the adjustment of cerebrocortical oxygen consumption and blood flow during hypercapnic stress.
Dora, E; Hines, K; Kunos, G; McLaughlin, AC, 1992
)
0.28
" The mean digoxin dosage at the development of fatal arrhythmias after the 100 micrograms/kg of FK 33,824 was 30% lower than the control group."( Opioid receptor agonists D-Ala-2-Me-Phe-4-Met-(O)-ol enkephalin and ethylketocyclazocine in the brain accentuate digoxin-induced arrhythmias.
Rabkin, SW,
)
0.13
" Before AOS exposure, the opioid peptides suppressed the PMA-stimulated respiratory burst in human PMNs and a U-shaped dose-response relationship was observed."( Reciprocal effects between opioid peptides and human polymorphonuclear leukocytes--II. Enhancement of phorbol myristate acetate-induced respiratory burst in human polymorphonuclear leukocyte by opioid peptides previously exposed to activated oxygen specie
Guerin, MC; Le Doucen, C; Loubatiere, J; Slaoui-Hasnaoui, A; Torreilles, J, 1992
)
0.28
" catheters, dose-response curves were carried out using the hot plate (HP) test for a number of receptor-preferring opioids."( Characteristics of dose-dependent antagonism by beta-funaltrexamine of the antinociceptive effects of intrathecal mu agonists.
Mjanger, E; Yaksh, TL, 1991
)
0.28
"8-fold rightward shift in the dose-response curve."( Lack of antinociceptive cross-tolerance between [D-Pen2, D-Pen5]enkephalin and [D-Ala2]deltorphin II in mice: evidence for delta receptor subtypes.
Mattia, A; Mosberg, HI; Porreca, F; Vanderah, T, 1991
)
0.28
" To test for a specific toxic effect on the neurons of the ciliary ganglion, we generated a dose-response curve for toxicity in vitro and determined that naltrexone was not toxic over concentration ranges that are likely to exist in vivo."( Endogenous opioids modulate neuronal survival in the developing avian ciliary ganglion.
Ford, MJ; Meriney, SD; Oliva, D; Pilar, G, 1991
)
0.28
" Dose-response curves for intrathecally administered agonists with mu- and/or delta-opioid activity were shifted to the left for inflamed hindpaws when compared to contralateral non-inflamed paws."( Spinal opioid analgesic effects are enhanced in a model of unilateral inflammation/hyperalgesia: possible involvement of noradrenergic mechanisms.
Dubner, R; Hylden, JL; Iadarola, MJ; Nahin, RL; Thomas, DA, 1991
)
0.28
" Regression analyses failed to reflect significant shifts in the dose-response functions for either agonist on either measure."( Gender effects and central opioid analgesia.
Bodnar, RJ; Kepler, KL; Kest, B; Pasternak, GW; Paul, D; Standifer, KM, 1991
)
0.28
" Upon pretreatment with morphine over greater than or equal to 12 h, a fourfold shift of the PGE1-morphine dose-response curve was observed, whether or not IBMX was added."( Regulation of cyclic AMP by the mu-opioid receptor in human neuroblastoma SH-SY5Y cells.
Duan, DS; Eiger, S; Lameh, J; Sadée, W; Yu, VC, 1990
)
0.28
" On the basis of our dose-response data, we suggest that, in mice, kappa and mu, but not delta, opioid receptors modulate tonic pain perception at both spinal and supraspinal loci."( Tonic pain perception in the mouse: differential modulation by three receptor-selective opioid agonists.
Cowan, A; Murray, CW, 1991
)
0.28
" In dose-response studies, beta-FNA antagonized all the actions with similar potencies (ID50 values of 12."( Comparison of naloxonazine and beta-funaltrexamine antagonism of mu 1 and mu 2 opioid actions.
Pasternak, GW; Paul, D; Pick, CG, 1991
)
0.28
"The effect of intravenous infusion of agonists of mu-(DAGO) and delta-(DADL, DAAE) opiate receptors on mean arterial pressure and heart rate was studied in experiments on rats with dosed blood loss of up to 30% of calculated blood volume."( [The effect of opiate receptor agonists on the blood circulation in rats with hemorrhagic shock].
Grossler, Iu; Sheĭkh, DV; Slepushkin, VD,
)
0.13
" A dose-response study demonstrated that the maximum growth hormone release was obtained with 10 micrograms/kg while higher doses were less or not effective."( The growth hormone secretory response to fentanyl in rat: an involvement of mu type receptors.
Buydens, P; Finné, E; Govaerts, J; Matton, A; Vanhaelst, L, 1990
)
0.28
" The depressive effects induced by the mu agonist PL017 (5 micrograms), delta agonist DADLE (25 micrograms) and kappa agonist 66A-078 (1 microgram) were antagonized by CCK-8 within a dosage of 10 micrograms in a dose dependent manner."( [Cholecystokinin-octapeptide antagonizes the central depressive effect of opioid peptides in rats].
Han, JS; Mei, L, 1991
)
0.28
" In Long-Evans rats, BW942C produced a biphasic dose-response curve for urine output with lower doses increasing and higher doses suppressing output."( Kappa opioid partial agonist activity of the enkephalin-like pentapeptide BW942C based on urination and in vitro studies in humans and animals.
Cone, EJ; Johnson, RE; Su, TP; Vaupel, DB, 1990
)
0.28
" However, when the dose-response curves for both U50, 488H and DPDPE in the presence of a low-analgesic dose of the other agent were compared with the dose-response curves for the respective agonist administered alone, the curves for the combination regimens were shifted to the left."( Kappa- and delta-opioid agonists synergize to produce potent analgesia.
Levine, JD; Miaskowski, C; Taiwo, YO, 1990
)
0.28
" On day 6, the magnitude of tolerance was assessed by establishing IT dose-response lines for the effect of the chronic drug given as bolus injections (probe)."( Tolerance to delta- but not mu-opioid receptors in the spinal cord attenuates inhibition of the tail-flick response induced by beta-endorphin administered intracerebroventricularly in mice.
Suh, HH; Tseng, LF, 1990
)
0.28
" Proglumide both shifted the dose-response curve for morphine analgesia to the left and prolonged morphine's duration of action."( Proglumide selectively potentiates supraspinal mu 1 opioid analgesia in mice.
Bodnar, RJ; Pasternak, GW; Paul, D, 1990
)
0.28
" The FHR response to DADLE was similar to DAGO in both dose-response and time-action characteristics."( Central opioid modulation of fetal cardiovascular function: role of mu- and delta-receptors.
Cai, LQ; Szeto, HH; Zhu, YS, 1990
)
0.28
") injected 1 min before each agonist produced a significant parallel shift to the right of the dose-response curves for morphine and DAMGO, but only partly antagonized the effects of DADLE and DSLET."( Role of peripheral mu, delta and kappa opioid receptors in opioid-induced inhibition of gastrointestinal transit in rats.
La Regina, A; Petrillo, P; Sbacchi, M; Tavani, A, 1990
)
0.28
" morphine dose-response line was shown to be displaced progressively to the right with decreasing maximal effect (i."( Modulation of the potency and efficacy of mu-mediated antinociception by delta agonists in the mouse.
Mosberg, HI; Porreca, F; Qi, JN, 1990
)
0.28
" Graded dose-response curves (DRC) were constructed from tail-flick latencies converted to % maximal possible effect (%MPE), and the ED50 calculated."( Spinal antinociceptive synergy between clonidine and morphine, U69593, and DPDPE: isobolographic analysis.
Green, J; Harris, S; Lloyd, P; Lozito, R; Messineo, E; Ossipov, MH, 1990
)
0.28
" morphine dose-response line."( Modulation of morphine antinociception by peripheral [Leu5]enkephalin: a synergistic interaction.
Jiang, Q; Porreca, F; Tallarida, RJ, 1990
)
0.28
" Dose-response curves at 1 hr revealed similar potencies of oxymorphone and the derivatives, with the exception of OxyPNPH which was significantly less potent."( Irreversible opiate agonists and antagonists. IV. Analgesic actions of 14-hydroxydihydromorphinone hydrazones.
Bodnar, RJ; Burks, TF; Clark, JE; Hahn, EF; Pasternak, GW; Williams, CL, 1988
)
0.27
" dose-response curves for the effect of the chronic drug given as a bolus."( Potency of infused spinal antinociceptive agents is inversely related to magnitude of tolerance after continuous infusion.
Stevens, CW; Yaksh, TL, 1989
)
0.28
" Both the morphine and normorphine dose-response lines were displaced to the left in the presence of DPDPE."( Modulation of mu-mediated antinociception by delta agonists in the mouse: selective potentiation of morphine and normorphine by [D-Pen2,D-Pen5]enkephalin.
Haaseth, RC; Heyman, JS; Mosberg, HI; Porreca, F; Vaught, JL, 1989
)
0.28
" Naloxonazine shifted the supraspinal DAGO dose-response curve 4-fold to the right without changing the curve for spinal DAGO."( Different mu receptor subtypes mediate spinal and supraspinal analgesia in mice.
Bodnar, RJ; Gistrak, MA; Pasternak, GW; Paul, D, 1989
)
0.28
" The slopes of the dose-response lines were parallel, but the delta compound was about 250 times less potent than DAMGO."( Sympathoadrenal, cardiovascular and blood gas responses to highly selective mu and delta opioid peptides.
Kiritsy-Roy, JA; Marson, L; Van Loon, GR, 1989
)
0.28
" However, in mice tested with the naltrexone pellets still implanted, the 15 mg naltrexone pellet was able to shift the dose-response function for morphine analgesia more than 300-fold."( Chronic opioid antagonist treatment: assessment of receptor upregulation.
Lutfy, K; Sierra, V; Yoburn, BC, 1989
)
0.28
", DPDPE displaced the morphine dose-response line to the left and also potentiated the effects of normorphine and etorphine."( Differential modulation by [D-Pen2, D-Pen5]enkephalin and dynorphin A-(1-17) of the inhibitory bladder motility effects of selected mu agonists in vivo.
Nunan, L; Porreca, F; Sheldon, RJ, 1989
)
0.28
" As is seen for [Leu]enkephalin when tested in a one-way active avoidance task, the dose-response function for the impairment produced by DPen2-[DPen5]enkephalin in the automated shelf-jump task is U-shaped."( DPen2-[DPen5]enkephalin, a delta opioid receptor-selective analog of [Leu]enkephalin, impairs avoidance learning in an automated shelf-jump task in rats.
Gehrig, CA; Martinez, JL; Weinberger, SB, 1989
)
0.28
" Antinociceptive dose-response curves were constructed for mu ([D-Ala2,NMePhe4,Gly-ol]enkephalin, DAGO; morphine) and delta ([D-Pen2,D-Pen5]enkephalin, DPDPE)-agonists in the absence, and in the presence of the mu non-surmountable antagonist, beta-funaltrexamine (beta-FNA) or the delta-antagonist ICI 174,864 (N,N-diallyl-Tyr-Aib-Aib-Phe-Leu-OH, where Aib is alpha-amino-isobutyric acid)."( Opioid delta-receptor involvement in supraspinal and spinal antinociception in mice.
Heyman, JS; Mosberg, HI; Mulvaney, SA; Porreca, F, 1987
)
0.27
" The dose-response curves of the preferential mu- ligands morphine and [D-Ala2, MePhe4, Gly-ol5] enkephalin (DAGO) were shifted by naloxone at low doses but not by ICI 174,864."( The role of mu- and delta- opioid receptors on the intestinal propulsion in rats.
La Regina, A; Petrillo, P; Sbacchi, M; Tavani, A, 1986
)
0.27
" The dose-response curves were shifted to the right in a non-parallel fashion with increasing calcium concentration (0."( Comparison of the effects of calcium concentration on mu and kappa agonist actions in the guinea pig ileum.
Hill, RG; Hughes, J; Johnson, MA, 1986
)
0.27
"5 microgram/hr) for 5 days caused 61- and 6-fold shifts to the right of the dose-response curves for PL-17 and DPDPE, respectively."( Interaction between highly selective mu and delta opioids in vivo at the rat spinal cord.
Chang, KJ; Leslie, JB; Russell, RD; Su, YF; Watkins, WD, 1986
)
0.27
" In an effort to examine the receptor subtypes responsible for opioid analgesia in specific brain regions, we examined dose-response relationships and naloxonazine sensitivity of morphine and two enkephalin derivatives in the above 4 brain regions."( Role of mu 1-opiate receptors in supraspinal opiate analgesia: a microinjection study.
Bodnar, RJ; Lee, SJ; Pasternak, GW; Williams, CL, 1988
)
0.27
" Slightly conflicting results have been obtained, depending on the dosage of naloxone used."( Endorphins: what are they? How are they measured? What is their role in exercise?
Grossman, A; Sutton, JR, 1985
)
0.27
" The dose-response curves were monotonic and the slopes were log-linear."( Epidural injections of bupivacaine, morphine, fentanyl, lofentanil, and DADL in chronically implanted rats: a pharmacologic and pathologic study.
Durant, PA; Yaksh, TL, 1986
)
0.27
" Naloxonazine (10 mg/kg) shifted the morphine hyperphagia dose-response curve to the right."( Differential sensitivity of opioid-induced feeding to naloxone and naloxonazine.
Arjune, D; Bodnar, RJ; Hahn, EF; Mann, PE; Pasternak, GW; Romero, MT, 1988
)
0.27
" Similar blockade was observed for EKC and U 50488 at doses of 10 and/or 20 ng/kg, but DAGO was unable to affect the AS-induced gastric inhibition at any dosage tested (20-200 ng/kg icv)."( CNS blockade of acoustic stress-induced gastric motor inhibition by kappa-opiate agonists in dogs.
Alvinerie, M; Bueno, L; Gue, M; Honde, C; Junien, JL; Pascaud, X, 1988
)
0.27
" Dose-response curves for neurotensin-induced secretion revealed an EC50 of 1x10(-6)M, thereby being in the range of that for acetylcholine or nicotine."( Neurotensin affects metabolism of opioid peptides, catecholamines and inositol phospholipids in bovine chromaffin cells.
Bommer, M; Herz, A, 1989
)
0.28
" This correlated with the dose-response required to stimulate phosphorylase activity in intact hepatocytes and suggests that the effects of the opioid peptides on carbohydrate metabolism in liver are the result of cross-reactivity of the peptides with angiotensin II receptors."( [Leu]enkephalin stimulates carbohydrate metabolism in isolated hepatocytes and kidney tubule fragments by interaction with angiotensin II receptors.
Hothi, SK; Randall, DP; Titheradge, MA, 1989
)
0.28
" An inverted-U dose-response curve was obtained."( Pharmacological evidence of a central effect of naltrexone, morphine, and beta-endorphin and a peripheral effect of met- and leu-enkephalin on retention of an inhibitory response in mice.
Baratti, CM; Introini, IB; McGaugh, JL, 1985
)
0.27
" A dose-response relationship between inhibition of alpha-MSH secretion and the concentration of Leu-enkephalin, with ED50 approximately 10(-9) M, was observed."( Modulation by Leu-enkephalin of peptide release from perifused neurointermediate pituitary. II. Inhibition of calcium-mediated secretion of alpha-MSH and beta-endorphin.
Al Zein, M; Koch, B; Lutz-Bucher, B, 1986
)
0.27
" 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
" Incubation of increasing concentrations of ICI 174,864 (10,30,100 and 300 nM) produced a dose-related and parallel rightward displacement of the DPDPE dose-response curve in the MVD."( Studies in vitro with ICI 174,864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO).
Burks, TF; Hirning, LD; Hruby, VJ; Hurst, R; Mosberg, HI; Porreca, F, 1985
)
0.27
" The dose-response curves for the biological response were suggestive of positive cooperativity and systematically occurred at lower ligand concentrations than those for the binding of [3H] [D-Ala2, D-Leu5]enkephalin (DADLE), which were instead shallow and suggestive of a site heterogeneity or of a cooperative phenomenon."( Multiple states of opioid receptors may modulate adenylate cyclase in intact neuroblastoma X glioma hybrid cells.
Costa, T; Gramsch, C; Herz, A; Wüster, M, 1985
)
0.27
" pairs of time-response curves, pairs of dose-response lines were constructed at various times; these lines showed decreasing displacement with time, indicative of the disappearance of naloxone."( Estimation of the affinity of naloxone at supraspinal and spinal opioid receptors in vivo: studies with receptor selective agonists.
Heyman, JS; Koslo, RJ; Mosberg, HI; Porreca, F; Tallarida, RJ, 1986
)
0.27
" The slope of the analgesic dose-response curve for the highly specific delta agonist, cyclic [D-Penicillamine2, D-Penicillamine5]enkephalin (DPDPE), was significantly different (flatter) from those of mu agonists or DADLE."( Continuous intrathecal opioid analgesia: tolerance and cross-tolerance of mu and delta spinal opioid receptors.
Chang, KJ; Leslie, JB; Russell, RD; Su, YF; Watkins, WD, 1987
)
0.27
"The effects of the delta-selective antagonist ICI 174864 and naltrexone on the dose-response curves to the mu-selective agonist RX 783006 and D-ala-D-leucine enkephalin (DADL) have been investigated in the rat isolated vas deferens preparation (RVD) set up in Krebs solution containing half the normal Ca++ concentration."( Delta receptors in the rat vas deferens.
Carter, A; Smith, CF, 1986
)
0.27
" The thresholds of inhibition and slopes of the dose-response curves for inhibition by MnCl2 and LiCl vary."( Effects of cations on binding, in membrane suspensions, of various opioids at mu-sites of rabbit cerebellum and kappa-sites of guinea-pig cerebellum.
Kosterlitz, HW; Paterson, SJ; Robson, LE; Traynor, JR, 1987
)
0.27
" Like [leu]enkephalin from which it may be formed, tyr-gly-gly impaired avoidance acquisition, and its dose-response function for this effect was U-shaped."( Differential effects on active avoidance performance and locomotor activity of two major enkephalin metabolites, tyr-gly-gly and des-tyr-[leu]enkephalin.
Martinez, JL; Weinberger, SB, 1988
)
0.27
" The dose-response function was U-shaped, with neither 100 nor 600 micrograms/kg having any effect."( Leu-enkephalin impairs memory of an appetitive maze response in mice.
Linden, D; Martinez, JL, 1986
)
0.27
"025), bismuth subsalicylate (Pepto-Bismol) taken orally at a dosage of as low as 30 ml every half hour for eight doses was shown to be effective in reducing the frequently of episodes of diarrhea."( Nonantibiotic therapy for travelers' diarrhea.
DuPont, HL; Ericsson, CD; Johnson, PC,
)
0.13
" Kelatorphan (20 microM) produced a 7-fold shift to the left of the Met-enkephalin dose-response curve."( Potentiation of enkephalin action by peptidase inhibitors in rat locus ceruleus in vitro.
Christie, MJ; North, RA; Roques, BP; Williams, JT, 1987
)
0.27
" Dose-response and time-course experiments were carried out using both static incubation of paired hemipituitary glands and perifusion of whole glands."( Effects of two enkephalin analogues, morphine sulphate, dopamine and naloxone on prolactin secretion from rat anterior pituitary glands in vitro.
Bentley, AM; Wallis, M, 1986
)
0.27
" A similar effect was obtained only with a dose 25 times higher (500 ng X kg-1) administered intravenously; at this dosage DALAMIDE administered intravenously also reduced the colonic motility index by 66%."( Central and peripheral control of gastrointestinal and colonic motility by endogenous opiates in conscious dogs.
Bueno, L; Fargeas, MJ; Fioramonti, J; Hondé, C; Primi, MP, 1985
)
0.27
" This method is simple and sensitive enough to determine p-hydroxybestatin in serum (200 microliters) from muscular dystrophic patients and from healthy subjects dosed with bestatin."( Determination of p-hydroxybestatin in human serum by high-performance liquid chromatography using fluorescence detection.
Ishida, J; Kai, M; Ohkura, Y, 1985
)
0.27
") produced a dose-response curve with a reduced maximum effect."( Relative involvement of receptor subtypes in opioid-induced inhibition of intestinal motility in mice.
Takemori, AE; Ward, SJ,
)
0.13
" However, by selecting the correct dosage analgesic effects approximately equivalent to those of 10 mg morphine can be achieved with most of these drugs."( Opioid drugs and their receptors. A summary of the present state of knowledge.
Offermeier, J; van Rooyen, JM, 1984
)
0.27
" As dosage was increased, the hyperthermias diminished and in some cats hypothermia developed."( Thermoregulatory effects of (D-ala2)-methionine-enkephalinamide in the cat. Evidence for multiple naloxone-sensitive opioid receptors.
Clark, WG; Ponder, SW,
)
0.13
" The dose-response curve for naloxone against seizure activity induced by leucine enkephalin was the same as that in gamma-hydroxybutyrate-induced petit mal."( Anticonvulsants specific for petit mal antagonize epileptogenic effect of leucine enkephalin.
Bearden, LJ; Snead, OC, 1980
)
0.26
" The parallelism of the dose-response curves of opiates in the presence and absence of naloxone indicated competitive reversible antagonism."( Opiate receptors in the rabbit iris.
Dal Bello, A; Drago, F; Gorgone, G; Moro, F; Panissidi, G; Scapagnini, U; Spina, F, 1980
)
0.26
" Thus, both sites demonstrated similar dose-response relationships, both responding to at least 100 times lower doses of enkephalins than MS."( Characterization of opiate-mediated responses of the feline ileum and ileocecal sphincter.
Clain, CJ; Cohen, S; Ouyang, A; Snape, WJ, 1982
)
0.26
" Ethylketazocine produced a biphasic dose-response curve."( Characterization of the opiate receptor in the guinea-pig ileal mucosa.
Kachur, JF; Miller, RJ, 1982
)
0.26
") shifted the dose-response curve for both responses to the right more for the beta-EP than for DADL."( Inhibition of tail-flick and shaking responses by intrathecal and intraventricular D-Ala2-D-Leu5-enkephalin and beta-endorphin in anesthetized rats.
Cheng, SS; Fujimoto, JM; Tseng, LF, 1983
)
0.27
" Dose-response curves were plotted with naloxone against the changes produced by each agonist, and the effect of a number of anticonvulsant drugs on agonist-induced seizures was ascertained."( The epileptogenic spectrum of opiate agonists.
Bearden, LJ; Snead, OC, 1982
)
0.26
" Uptake of [3H]DADLE was a receptor-mediated process, since it was inhibited by opiate receptor ligands and the (i) time course, (ii) dose-response curve, and (iii) temperature dependence of uptake were similar to those for enkephalin-receptor down regulation."( Characterization of the association of tritiated enkephalin with neuroblastoma cells under conditions optimal for receptor down regulation.
Blanchard, SG; Chang, KJ; Cuatrecasas, P, 1983
)
0.27
" 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
" It increased the IC50 values and slopes of their dose-response curve for enkephalins and their analogs, and shifted to the right the curves for FK33824, levorphanol and normorphine."( Functional opiate receptor in mouse vas deferens: evidence for a complex interaction.
Garzón, J; Lee, NM; Sánchez-Blázquez, P, 1983
)
0.27
" Some improvements were observed after 1 week of treatment; the most improvement occurred at 6 weeks, when the mean doxepin dosage was approximately 200 mg/day and plasma doxepin and nordoxepin averaged 80 ng/ml."( Doxepin's effects on chronic pain and depression: a controlled study.
Cork, RC; Crago, BR; Davis, TP; Hameroff, SR; Lerman, JC; Neuman, CP; Watts, KS; Weiss, JL; Womble, JR, 1984
)
0.27
" In conscious man essentially similar results were found following intravenous dosing with a stable met-enkephalin analogue (DAMME, FK33824) or naloxone with decreases and increases respectively in the sensitivity of baroreflex responses to sodium nitroprusside."( Opioid peptides and central control of blood pressure.
Petty, MA; Reid, JL; Rubin, PC, 1984
)
0.27
" Respiratory frequency was dose-dependently depressed by FK-33824 and DADLE ; dose-response curves with morphine and D-Ser2- Thr6 could not be obtained for technical reasons."( A comparative study in rats of the respiratory depression and analgesia induced by mu- and delta-opioid agonists.
Flórez, J; Pazos, A, 1984
)
0.27
", delayed nociceptive reaction on a 55 degrees C hot-plate with a dose-response curve not readily fitting a single straight line; this effect was antagonized by high doses of naloxone."( Bremazocine induces antinociception, but prevents opioid-induced constipation and catatonia in rats and precipitates withdrawal in morphine-dependent rats.
Gambino, MC; Petrillo, P; Tavani, A, 1984
)
0.27
" Simultaneous application of Hi and 10 micrograms of diphenhydramine, pyrilamine or promethazine, apparently causing no analgesic effect from a single administration, caused a parallel shift of the dose-response curve of Hi to the right."( Analgesic effect of histamine induced by intracerebral injection into mice.
Chung, YH; Kamei, C; Miyake, H; Tasaka, K, 1984
)
0.27
" Dose-response curves for the increase in the content of proenkephalin mRNA and of enkephalin-containing peptides were essentially identical."( Enkephalin biosynthesis in adrenal medulla. Modulation of proenkephalin mRNA content of cultured chromaffin cells by 8-bromo-adenosine 3',5'-monophosphate.
Costa, E; Guidotti, A; Kageyama, H; Meek, JL; Mocchetti, I; Quach, TT; Schwartz, JP; Tang, F, 1984
)
0.27
"Insulin and glucagon release from monolayer pancreatic islet cell cultures were inhibited in a dose-response fashion by various enkephalins."( Disparate effects of enkephalin and morphine upon insulin and glucagon secretion by islet cell cultures.
Ensinck, JW; Fujimoto, WY; Kanter, RA, 1980
)
0.26
" Each of the biologically active catecholamines inhibited the measured enzyme activity, and dose-response curves indicated that dopamine was most effective and epinephrine least effective."( Inhibition of the enzymatic degradation of Met-enkephalin by catecholamines.
Caffrey, JL; Hodges, DH, 1982
)
0.26
" Other experiments involving intracisternal dosing with this long acting form at higher levels (0."( Effects of enkephalins versus opiates on locomotor activity of the horse.
Burns, P; Combie, JD; Nugent, TE; Tobin, T; Weld, JM, 1982
)
0.26
" Since the log dose-response curves were displaced to the right in quasi-parallel fashion, and Lineweaver-Burk plots of the data showed an intersection very close to the origin of the horizontal axis, the antagonism between naloxone and the three peptides appears to be competitive."( Retrograde amnesia caused by Met-, Leu- and des-Try-Met-enkephalin in the rat and its reversal by naloxone.
Dias, RD; Izquierdo, I, 1981
)
0.26
" 2 The dose-response curves to naloxone obtained in tissues individually exposed to different opiates showed that their relative potency in increasing sensitivity to naloxone was as follows: levorphan greater than morphine greater than Met-enkephalin greater than nalorphine greater than pentazocine."( Pharmacological characterization of opiate physical dependence in the isolated ileum of the guinea-pig.
Luján, M; Rodríguez, R, 1981
)
0.26
"3 Pretreatment of the mice with naloxone caused a dose-dependent shift to the right of the dose-response curve to morphine."( Evidence for an action of morphine and the enkephalins on sensory nerve endings in the mouse peritoneum.
Bentley, GA; Newton, SH; Starr, J, 1981
)
0.26
" The heptapeptide Leu5-enkephalin-Arg6-Phe7 and the Met5-analogue, both in the amidized form, displayed dose-response relationship with a sensitivity of about 10 nmol."( Enkephalin-related peptides: direct action on the octopus heart.
Frösch, D; Kiehling, C; Martin, R; Schiebe, M; Voigt, KH, 1981
)
0.26
" For neurons exhibiting each of these three patterns, the mean T100, a modification of the T50 which is analogous to a dose-response curve, correlated with the effects of the drugs on evoked firing."( Morphine and methionine-enkephalin: different effects on spontaneous and evoked neuronal firing in the mesencephalic reticular formation of the rat.
Haigler, HJ; Hosford, DA, 1980
)
0.26
", the morphine dose-response curve shifted to the left and the ED50 value of morphine decreased."( Effects of a highly selective nonpeptide delta opioid receptor agonist, TAN-67, on morphine-induced antinociception in mice.
Endoh, T; Misawa, M; Mori, T; Nagase, H; Suzuki, T; Tsuji, M, 1995
)
0.29
"Quantitative in situ hybridization histochemistry was used to compare the effects of AMPH administration on mRNAs coding for zif/268, a member of the zinc finger family of immediate early genes, and the opioid peptides, preprodynorphin (PPD) and preproenkephalin (PPE), in rat striatum after 3 dosing schedules: (1) acute; (2) once a day for 5 days, and (3) once a day for 5 days followed 10 days later by a challenge dose."( Alterations in striatal zif/268, preprodynorphin and preproenkephalin mRNA expression induced by repeated amphetamine administration in rats.
McGinty, JF; Wang, JQ, 1995
)
0.29
" However, the response of preproenkephalin, c-fos and zif/268 mRNAs to such a dosing regimen is unknown."( Cocaine binges differentially alter striatal preprodynorphin and zif/268 mRNAs.
Daunais, JB; McGinty, JF, 1995
)
0.29
" The pellets were removed and 24 h later, mice were sacrificed and binding studies were conducted, or mice were tested in analgesia (tail-flick) dose-response studies."( Supersensitivity to opioid analgesics following chronic opioid antagonist treatment: relationship to receptor selectivity.
Chan, K; Davis, T; Duttaroy, A; Shah, S; Yoburn, BC,
)
0.13
" Bicuculline (GABAA receptor antagonist) and picrotoxin (chloride ion channel blocker) given intrathecally produced rightward shifts in the dose-response curves of DPDPE and heroin given intracerebroventricularly."( Spinal GABA receptors mediate brain delta opioid analgesia in Swiss Webster mice.
Fujimoto, JM; Rady, JJ, 1995
)
0.29
"5 micrograms), parallel rightward shifts of both morphine and RB 101 (mixed enkephalin-degrading-enzyme inhibitor) dose-response curves, were observed, but the concentration of beta-FNA required to reduce the analgesic responses was about 10 times higher for RB 101 (0."( Assessment of endogenous enkephalins efficacy in the hot plate test in mice: comparative study with morphine.
Noble, F; Roques, BP, 1995
)
0.29
" Pretreatment also shifted to the right the dose-response function for DALA intra-accumbens."( Mesoaccumbens dopamine-opiate interactions in the control over behaviour by a conditioned reinforcer.
Everitt, BJ; Phillips, GD; Robbins, TW, 1994
)
0.29
" In contrast, caudal ventral pallidal DPDPE microinjections showed a dose-response effect with reward increases of 19, 22 and 31% (-0."( Comparison of delta opiate receptor agonist induced reward and motor effects between the ventral pallidum and dorsal striatum.
Johnson, PI; Stellar, JR, 1994
)
0.29
" Second, intrathecal administration of 2-hydroxysaclofen, a GABAB antagonist (which inhibited antinociception induced by a GABAB agonist, baclofen, given IT), produced a shift of the dose-response curve for ICV DPDPE to the right."( [D-Pen2-D-Pen5]enkephalin, a delta opioid agonist, given intracerebroventricularly in the mouse produces antinociception through medication of spinal GABA receptors.
Fujimoto, JM; Holmes, BB, 1994
)
0.29
" This EEG activation was greatly attenuated at DPDPE doses greater than 154 nmol/h, resulting in a U-shaped dose-response curve."( Effects of the delta-opioid agonist, [D-Pen2,D-Pen5]-enkephalin, on fetal lamb EEG.
Cheng, PY; Soong, Y; Szeto, HH; Wu, DL, 1994
)
0.29
" The most potent analogue, D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2, caused a parallel rightward shift of the NMB dose-response curve, the Schild plot slope was not significantly different from unity, and the affinity was 230 nM."( Discovery of a novel class of neuromedin B receptor antagonists, substituted somatostatin analogues.
Battey, JF; Coy, DH; Jensen, RT; Mantey, SA; Moreau, JP; Mrozinski, JE; Orbuch, M; Taylor, JE, 1993
)
0.29
" In addition, opioid dose-response curves with preemptive administration were compared with early and late postadministrations."( Electrophysiologic analysis of preemptive effects of spinal opioids on N-methyl-D-aspartate receptor-mediated events.
Chapman, V; Dickenson, AH; Haley, JE, 1994
)
0.29
" Naloxone shifted to the right the dose-response curves for each opioid peptide significantly enhancing the ED50 values."( Modulation of non-adrenergic non-cholinergic inhibitory transmission in rat duodenum: role of opiates and 5-hydroxytryptamine.
Adamo, EB; Di Giovanni, G; Marini, R; Mulè, F; Postorino, A; Serio, R, 1993
)
0.29
" Dose-response curves were generated for both delta 9-THC (i."( Interactions between delta 9-tetrahydrocannabinol and kappa opioids in mice.
Martin, BR; Smith, PB; Welch, SP, 1994
)
0.29
" [Leu]enkephalin produced a U-shaped dose-response function because both lower and higher doses of LE did not affect avoidance responding."( [Leu]enkephalin enhances active avoidance conditioning in rats and mice.
Janak, PH; Manly, JJ; Martinez, JL, 1994
)
0.29
"01-micrograms dosage was associated with hyperactivity."( Behavioral effects of the mu-opioid peptide agonists DAMGO, DALDA, and PL017 on locomotor activities.
Meyer, ME, 1993
)
0.29
"To determine the influence of stimulation intensity on dose-response curves of three analgesics in halothane-anesthetized rats, continued immersion of the tail in 52."( Suppression of nociceptive responses by spinal mu opioid agonists: effects of stimulus intensity and agonist efficacy.
Saeki, S; Yaksh, TL, 1993
)
0.29
"03 microgram of DAMGO resulting in a steeper dose-response relationship."( Evidence for delta opioid receptor subtypes in rat spinal cord: studies with intrathecal naltriben, cyclic[D-Pen2, D-Pen5] enkephalin and [D-Ala2, Glu4]deltorphin.
Hammond, DL; Stewart, PE, 1993
)
0.29
" The time course and dose-response relationships between mu receptor phosphorylation and agonist-induced desensitization display interesting parallels."( Differential mu opiate receptor phosphorylation and desensitization induced by agonists and phorbol esters.
Mackin, S; Uhl, GR; Wang, JB; Weight, FF; Yu, Y; Zhang, L, 1996
)
0.29
" This close temporal and dose-response relationship strongly suggests that delta-opioid receptor-mediated increases in intracellular [Ca2+] results from inositol 1,4,5-trisphosphate-induced Ca2+ release from intracellular stores, in undifferentiated NG108-15 cells."( delta-Opioids stimulate inositol 1,4,5-trisphosphate formation, and so mobilize Ca2+ from intracellular stores, in undifferentiated NG108-15 cells.
Lambert, DG; Smart, D, 1996
)
0.29
" Initial dose-response curves revealed that dopamine was approximately equipotent at producing motor activity after microinjection into the core and shell, AMPA was more effective in the core, whereas DAMGO was more potent in the shell."( Involvement of the ventral tegmental area in locomotion elicited from the nucleus accumbens or ventral pallidum.
Churchill, L; Hooks, MS; Johnson, K; Kalivas, PW; Klitenick, MA, 1996
)
0.29
" In the present study, dose-response effects of acute administration of these stimulants on preproenkephalin (PPE) mRNA expression in the rat striatum were investigated with quantitative in situ hybridization histochemistry 3 h after injection."( D1 and D2 receptor regulation of preproenkephalin and preprodynorphin mRNA in rat striatum following acute injection of amphetamine or methamphetamine.
McGinty, JF; Wang, JQ, 1996
)
0.29
" However, [D-Pen2,D-Pen5]enkephalin (DPDPE), a delta 1-opioid receptor agonist, and [D-Ala2,Cys4]deltorphin, a delta 2-opioid receptor agonist, at doses which exhibit no intrinsic effects (10(-8) and 10(-7) M), shifted the dose-response curve for mu-opioid receptor-evoked adenosine release to the left in a dose-dependent manner."( Synergy between mu/delta-opioid receptors mediates adenosine release from spinal cord synaptosomes.
Cahill, CM; Sawynok, J; White, TD, 1996
)
0.29
" Buprenorphine, when injected systemically, revealed a potent analgesic effect by tailflick assay, with a biphasic dose-response curve, which was reversed by naloxone."( Pharmacological characterization of buprenorphine, a mixed agonist-antagonist with kappa 3 analgesia.
Peter, Y; Pick, CG; Schreiber, S; Weizman, R, 1997
)
0.3
" Fentanyl pumps and placebo pellets were removed on the third day following implantation and 4 h later mu-opioid receptor saturation binding studies in whole brain ([3H][D-Ala2,MePhe4,Gly-ol5]enkephalin: DAMGO) or fentanyl analgesic dose-response studies (tailflick assay) were conducted."( Magnitude of tolerance to fentanyl is independent of mu-opioid receptor density.
Chan, KW; Duttory, A; Yoburn, BC, 1997
)
0.3
" However, inhibition reached the maximal level only at 50 mM sodium, and typical sigmoidal dose-response curves were obtained only in the presence of 118 mM sodium."( Regulation of mu-opioid receptor in neural cells by extracellular sodium.
Medzihradsky, F; Yabaluri, N, 1997
)
0.3
" Pairing Delt II (5 microg) with low (100-200 mg/kg) 2DG doses significantly enhanced intake, producing a leftward (3-fold) shift in 2DG's hyperphagic dose-response curve."( Delta and kappa opioid receptor subtypes and ingestion: antagonist and glucoprivic effects.
Bodnar, RJ; Ruegg, H; Yu, WZ, 1997
)
0.3
" injections of morphine or fentanyl, produced antinociceptive tolerance as shown by a significant rightward displacement of the agonist dose-response curves compared to controls."( Competitive and non-competitive NMDA antagonists block the development of antinociceptive tolerance to morphine, but not to selective mu or delta opioid agonists in mice.
Bilsky, EJ; Hruby, VJ; Inturrisi, CE; Porreca, F; Sadée, W, 1996
)
0.29
"055 nmol from the dose-response curve."( Central regulation of urine production by a selective mu-opioid agonist, [D-Ala2, N-Me-Phe4, Gly5-ol]-enkephalin, in rats.
Matsuda, T; Mori, M; Tsushima, H, 1997
)
0.3
" Naloxone (1 microM) or norbinaltorphimine (10 nM) shifted the dose-response curve of (-)-U50,488H to the right by 100-fold."( Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Chen, C; Li, JG; Liu-Chen, LY; Luo, LY; Zhu, J, 1997
)
0.3
" Prolonged exposure to agonists induced desensitization of the receptor as estimated by a reduction in the maximal stimulation of GTP[gamma-35S] binding by DAMGO and rightward shifts in the dose-response curves."( Down-regulation of mu-opioid receptor by full but not partial agonists is independent of G protein coupling.
Medzihradsky, F; Yabaluri, N, 1997
)
0.3
" These results indicate that the mode of administration of a D2 dopamine receptor agonist, such as U91356A, although at a roughly equivalent dosage influences the extent of inhibition of the expression of PPE in the denervated striatum of monkeys."( Preproenkephalin mRNA expression in the caudate-putamen of MPTP monkeys after chronic treatment with the D2 agonist U91356A in continuous or intermittent mode of administration: comparison with L-DOPA therapy.
Bédard, PJ; Blanchet, PJ; Calon, F; Di Paolo, T; Goulet, M; Morissette, M; Soghomonian, JJ, 1997
)
0.3
"0 mg/kg clocinnamox displaced the morphine dose-response curve 4-fold to the right of the control curve and 10 mg/kg clocinnamox eliminated morphine's antinociceptive effects at doses up to 1000 mg/kg for at least seven days."( Clocinnamox dose-dependently antagonizes morphine-analgesia and [3H]DAMGO binding in rats.
Paronis, CA; Woods, JH, 1997
)
0.3
" Administration of morphine, DPDPE, or U50,488H three times daily for 3 days according to an escalating dosing schedule resulted in analgesic tolerance as indicated by an increase in analgesic ED50 values using the tail-flick test in mice."( The competitive alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist LY293558 attenuates and reverses analgesic tolerance to morphine but not to delta or kappa opioids.
Inturrisi, CE; Kao, B; Kest, B; McLemore, G, 1997
)
0.3
" Similarly, the progressive and complete loss of analgesia in CD-1 mice seen with repeated dosing of the delta ligand [D-Pen2, D-Pen5]enkephalin is not observed in 129/SvEv mice."( Lack of morphine and enkephalin tolerance in 129/SvEv mice: evidence for a NMDA receptor defect.
Jain, S; Kolesnikov, Y; Pasternak, GW; Wilson, R, 1998
)
0.3
" After NMDA treatment, the DPDPE dose-response curve shifted to the right (EC50 value increased approximately 7-fold, from 6 to 40 nM), and the maximal response induced by DPDPE was reduced by approximately 60%."( N-Methyl-D-aspartate attenuates opioid receptor-mediated G protein activation and this process involves protein kinase C.
Fan, GH; Jing, Q; Lou, LG; Ma, L; Pei, G; Wu, YL; Zhang, Z; Zhao, J, 1998
)
0.3
" Dose-response curves for 1DMe in the presence of naltrindole or naltrexone, delta- and mu-opioid selective antagonists respectively, indicate that 1DMe preferentially reversed mu-receptor-mediated but increased delta-receptor-mediated analgesia."( Differential modulation of mu- and delta-opioid antinociception by neuropeptide FF receptors in young mice.
Desprat, C; Zajac, JM, 1997
)
0.3
" Whereas the dose-response curves to Ins(1,4,5)P3 formation and cyclic AMP inhibition remained largely unaffected by C-terminal truncation, there were large differences in the pEC/IC50 values, with cyclic AMP inhibition being the more potent, perhaps indicating G(i alpha) coupling to adenylyl cyclase and G(i beta/gamma) coupling to PLC."( Effects of C-terminal truncation of the recombinant delta-opioid receptor on phospholipase C and adenylyl cyclase coupling.
Devi, LA; Hirst, RA; Lambert, DG; Smart, D, 1998
)
0.3
" the dose-response curve is bell-shaped."( The C-terminal tetrapeptide of beta-endorphin (MPF) enhances lymphocyte proliferative responses.
Ensor, DM; Miles, JB; Morley, JS; Owen, DL, 1998
)
0.3
" The isoeffect doses to produce moist desquamation on the dose-response curves were calculated with 95% confidence limits."( Mouse skin reactions following fractionated irradiation with carbon ions.
Ando, K; Ando, S; Chen, YJ; Kanai, T; Kobayashi, N; Koike, S; Nojima, K; Ohbuchi, T; Ohira, C; Shimizu, W, 1998
)
0.3
") pretreatment with calcium and thapsigargin, which increase intracellular calcium, reduced [D-Ala2,N-MePhe4,Gly-ol5]-enkephalin (DAMGO)-induced antinociception by shifting its dose-response curve to the right."( Role of intracellular calcium in modification of mu and delta opioid receptor-mediated antinociception by diabetes in mice.
Kamei, J; Nagase, H; Ohsawa, M, 1998
)
0.3
" A subsequent dose-response experiment examined the impact of P-gp on DPDPE antinociception."( Altered disposition and antinociception of [D-penicillamine(2,5)] enkephalin in mdr1a-gene-deficient mice.
Chen, C; Pollack, GM, 1998
)
0.3
" Finally, shifts in the morphine dose-response lines after 24-h pretreatment with the four dihydrocodeinone compounds suggest that the nitrocinnamoylamino derivatives may produce a greater magnitude long-term antagonism of morphine-induced antinociception than the chlorocinnamoylamino analogs."( Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity.
Archer, S; Bidlack, JM; Hill, KP; Jiang, Q; McLaughlin, JP; Sebastian, A, 1999
)
0.3
" At doses of cocaine on the descending limb of the cocaine dose-response curve, the mu-selective agonist DAMGO produced a dose-related decrease in cocaine self-administration when delivered by microinfusion into the VTA."( The mu opioid agonist DAMGO alters the intravenous self-administration of cocaine in rats: mechanisms in the ventral tegmental area.
Adamson, KL; Chow, BL; Coen, KM; Corrigall, WA, 1999
)
0.3
" Morphine analgesia was inhibited by dynorphin as shown by a rightward shift of the morphine dose-response curve."( Antianalgesic action of dynorphin A mediated by spinal cholecystokinin.
Fujimoto, JM; Holmes, BB; Rady, JJ, 1999
)
0.3
" The dose-response curves for C-fibre evoked response and post-discharge of the neurones were not different in rats aged P14 and P21."( Electrophysiological studies on the postnatal development of the spinal antinociceptive effects of the delta opioid receptor agonist DPDPE in the rat.
Dickenson, AH; Rahman, W, 1999
)
0.3
" Endomorphin-1 potentiated viral expression, in a bell-shaped dose-response manner with maximal enhancement approximately equal to 35% at 10(-10) M, in both mixed glial/neuronal cell and purified microglial cell cultures."( Endomorphin-1 potentiates HIV-1 expression in human brain cell cultures: implication of an atypical mu-opioid receptor.
Chao, CC; Gekker, G; Hu, S; Lokensgard, J; Peterson, PK; Portoghese, PS, 1999
)
0.3
" with a placebo or 15 mg naltrexone pellet for 8 days, the pellets removed and 24 hr later opioid receptor density (mu, delta) and receptor mRNA level (mu) determined in whole brain; or morphine dose-response studies conducted."( Opioid receptor upregulation in mu-opioid receptor deficient CXBK and outbred Swiss Webster mice.
Carroll, J; Chen, B; Duttaroy, A; Sehba, F; Shah, S; Shen, J; Yoburn, BC, 1999
)
0.3
" 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
" Both shifted the dose-response curve of morphine to the right and these actions were eliminated by intrathecal PGD(2."( Antianalgesic action of nociceptin originating in the brain is mediated by spinal prostaglandin E(2) in mice.
Campbell, WB; Fujimoto, JM; Rady, JJ, 2001
)
0.31
" Dose-response curves for the octapeptide were generated using two aequorin-octapeptide fusion proteins with the octapeptide fused to the N-terminus in one case, and to the C-terminus in the other."( C-terminal and n-terminal fusions of aequorin with small peptides in immunoassay development.
Daunert, S; Deo, SK; Lewis, JC,
)
0.13
" Microinfusions of naloxone alone in similar dosage completely blocked the predatory attack response as indicated by an increase in the threshold current strength for somatomotor as well as affective display components."( Enkephalinergic involvement in substantia nigra in the modulation of hypothalamically-induced predatory attack behavior.
Bhatia, SC; Nayar, U; Saha, SN, 2003
)
0.32
" These two compounds also exhibited nanomolar potencies in dose-response experiments performed on wild-type, M262T, Y308H, and C328R CAM receptors."( Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.
Befort, K; Décaillot, FM; Filliol, D; Kieffer, BL; Lazarus, LH; Schiller, PW; Schmidhammer, H; Tryoen-Tóth, P, 2005
)
0.33
"09 mg/kg/injection in a within-session dose-response curve (0."( Blunted response to cocaine in the Flinders hypercholinergic animal model of depression.
Fagergren, P; Goiny, M; Hurd, YL; Overstreet, DH, 2005
)
0.33
" We determined the dose-response relationship for amphetamine-induced psychomotor activity and Fos expression in nucleus accumbens and caudate-putamen 1 week after repeated administration of amphetamine or saline in locomotor activity chambers."( Repeated amphetamine administration outside the home cage enhances drug-induced Fos expression in rat nucleus accumbens.
Crombag, HS; Hope, BT; Kreuter, JD; Mattson, BJ; Mitchell, T; Morales, M; Simmons, DE, 2007
)
0.34
", conditioned place preference, conditioned taste aversion, ethanol-induced behavioral sensitization) alcohol dosing is precisely controlled by the experimenter."( Behavioral and neurochemical studies in distinct animal models of ethanol's motivational effects.
Boerngen-Lacerda, R; Camarini, R; Méndez, M; Pautassi, RM; Quadros, IM; Souza-Formigoni, ML, 2010
)
0.36
" There was a significant dose-response relationship between higher doses of EP 94 and reduced infarct size."( Dose-dependent cardioprotection of enkephalin analogue Eribis peptide 94 and cardiac expression of opioid receptors in a porcine model of ischaemia and reperfusion.
Akyürek, LM; Bergh, N; Bissessar, E; Bobrova, I; Grip, L; Gross, GJ; Karlsson, LO; Li, L, 2012
)
0.38
" Here, we used clinically relevant dosing to examine the effects of maternally administered sustained-release naltrexone on the rat brain by examining offspring at birth and in adulthood."( Maternally administered sustained-release naltrexone in rats affects offspring neurochemistry and behaviour in adulthood.
Dunlop, SA; Farid, WO; Hulse, GK; Krstew, EV; Lawrence, AJ; Tait, RJ, 2012
)
0.38
" The aim of the present study was to define the optimal timing and dosing of the administration of EP94 during ischemia and reperfusion in a rat model."( Cardioprotection of the enkephalin analog Eribis peptide 94 in a rat model of ischemia and reperfusion is highly dependent on dosing regimen and timing of administration.
Bergh, N; Bobrova, I; Grip, L; Karlsson, LO; Omerovic, E; Redfors, B; Shao, Y; Spanos, E, 2015
)
0.42
"5 mg/kg) or MP-10 (3-30 mg/kg) did not produce cataleptic behavior when dosed alone, but co-administration of haloperidol with MP-10 (3 and 10 mg/kg) induced cataleptic behaviors."( The PDE10A inhibitor MP-10 and haloperidol produce distinct gene expression profiles in the striatum and influence cataleptic behavior in rodents.
Gentzel, RC; Hershey, J; Kandebo, M; Koser, AJ; Renger, JJ; Roberts, R; Smith, SM; Toolan, D; Uslaner, J, 2015
)
0.42
" Seventy-two Specific pathogen-free (SPF) male Kunming mice were randomly divided into six groups: normal group, positive control group, AEPH of low dosage (100mg/kg) group, AEPH of medium dose (200mg/kg) group, AEPH of high dosage (400mg/kg) group and model group."( Effects of aqueous extracts from Panax ginseng and Hippophae rhamnoides on acute alcohol intoxication: An experimental study using mouse model.
Gong, XY; Hu, XY; Jia, LY; Lin, W; Luo, JX; Wang, YY; Wen, DC, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (6)

RoleDescription
delta-opioid receptor agonistnull
mu-opioid receptor agonistA compound that exhibits agonist activity at the mu-opioid receptor.
neurotransmitterAn endogenous compound that is used to transmit information across the synapse between a neuron and another cell.
analgesicAn agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
rat metaboliteAny mammalian metabolite produced during a metabolic reaction in rat (Rattus norvegicus).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
peptide zwitterionZwitterionic form of any peptide where, in general, the amino terminus is positively charged and the carboxy terminus is negatively charged.
pentapeptideAny molecule that contains five amino-acid residues connected by peptide linkages.
peptideAmide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another with formal loss of water. The term is usually applied to structures formed from alpha-amino acids, but it includes those derived from any amino carboxylic acid. X = OH, OR, NH2, NHR, etc.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency63.09570.010039.53711,122.0200AID1479
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Opioid receptor, delta 1b Danio rerio (zebrafish)Ki0.17500.04500.47591.4270AID1432897
Opioid receptor homologueDanio rerio (zebrafish)Ki0.07300.07300.28730.5658AID1432896
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.01420.00010.729810.0000AID132686; AID145926; AID145931; AID1755979; AID1853216
Delta-type opioid receptorMus musculus (house mouse)Ki0.00460.00000.53939.4000AID149069; AID1727060; AID1727079
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00320.00000.60689.2330AID149348; AID149948; AID149949; AID772822
Kappa-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.04170.00131.538010.0000AID145926; AID145931
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.01430.00000.38458.6000AID149301; AID151622; AID151911
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki10.00000.00000.18683.9500AID148570
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)9.50000.00010.813310.0000AID150417
Mu-type opioid receptorHomo sapiens (human)Ki1.21480.00000.419710.0000AID150419; AID150975; AID1853214
Delta-type opioid receptorHomo sapiens (human)Ki0.00620.00000.59789.9300AID149069; AID149898; AID149913; AID1572986; AID1600457; AID1755976; AID1853213
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki10.00000.00000.20186.4240AID149409
Kappa-type opioid receptorHomo sapiens (human)Ki1.00000.00000.362410.0000AID148006
Mu-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.03080.00081.699210.0000AID145926; AID145931; AID1853219
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.24600.00020.660310.0000AID1323816
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.38000.00000.27869.0000AID148045
Mu-type opioid receptorDanio rerio (zebrafish)Ki1.31700.18700.52891.3170AID1432895
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Proenkephalin-BHomo sapiens (human)Kd0.00710.00710.00710.0071AID101199
Delta-type opioid receptorMus musculus (house mouse)EC50 (µMol)0.07400.00110.40144.8000AID1727061
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.58950.00000.32639.4000AID1600459; AID1676256; AID1676258; AID1727071; AID1853220
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)0.02460.00000.43328.3000AID1600457; AID1676261; AID1676263; AID1727070; AID1755982; AID1853217; AID1865319
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.08000.00000.22448.9900AID1572990; AID1600460; AID1727072
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)Ke0.00590.00010.14726.1080AID148951
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
chemical synaptic transmissionProenkephalin-BHomo sapiens (human)
sensory perceptionProenkephalin-BHomo sapiens (human)
neuropeptide signaling pathwayProenkephalin-BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
opioid peptide activityProenkephalin-BHomo sapiens (human)
opioid receptor bindingProenkephalin-BHomo sapiens (human)
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
hippocampal mossy fiber to CA3 synapseProenkephalin-BHomo sapiens (human)
neuronal dense core vesicleProenkephalin-BHomo sapiens (human)
extracellular regionProenkephalin-BHomo sapiens (human)
plasma membraneProenkephalin-BHomo sapiens (human)
axon terminusProenkephalin-BHomo sapiens (human)
dendriteProenkephalin-BHomo sapiens (human)
plasma membraneProenkephalin-BHomo sapiens (human)
neuronal cell bodyProenkephalin-BHomo sapiens (human)
plasma membraneKappa-type opioid receptorMus musculus (house mouse)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (215)

Assay IDTitleYearJournalArticle
AID1727060Inhibition of [3H]-Deltorphin 2 binding to mouse delta opioid receptor expressed in rat GH3 cell membranes by Cheng-Prusoff analysis2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID234905Relative potency was determined between the GPI assay and the [3H]DAGO binding assay1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID79361The relative potency of compound was measured by comparing with [Leu]enkephalin in Guinea pig ileum(GPI) assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID1249926Displacement of [3H]diprenorphine from zebrafish delta1a opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
AID1206653Binding affinity to human delta opioid receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID197670Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 30 degree celsius at 260 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID772819Selectivity for delta opioid receptor (unknown origin) transfected in african green monkey COS1 cells over mu opioid receptor (unknown origin) transfected in african green monkey COS1 cells2013Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
Systematic replacement of amides by 1,4-disubstituted[1,2,3]triazoles in Leu-enkephalin and the impact on the delta opioid receptor activity.
AID1572986Binding affinity to delta opioid receptor (unknown origin)2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID1206651Intrinsic efficacy at human delta opioid receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID1600453Drug metabolism assessed as angiotensin converting enzyme (unknown origin)-mediated Gly3-Phe4 cleavage by measuring half life2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Applications of amide isosteres in medicinal chemistry.
AID132844Opioid agonist potencies was determined by mouse vas deferens (MVD)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
AID476638Selectivity ratio of Ki for mu opioid receptor in rat brain membrane to Ki for kappa opioid receptor in guinea pig brain membrane2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
"Carba"-analogues of fentanyl are opioid receptor agonists.
AID148655Inhibitory potency against Opioid receptor delta 1 in the mouse vas deferens assay1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID145931Concentration required to inhibit the specific binding of tritiated ligand [3H]-naloxone to opiate receptor by 50%1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Replacement of the peptide-backbone amides connecting Tyr-Gly and Gly-Gly in leucine-enkephalin with ketomethylene groups: synthesis and biological activity.
AID152058Potency towards Opioid receptor mu 1 relative to [Leu5 enkephalin]1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
AID151918Ratio of binding affinity towards mu to delta opioid receptors1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
AID680024TP_TRANSPORTER: inhibition of Deltorphin II uptake (Deltorphin II: 50 uM, Leu-enkephalin: 200 uM) in Xenopus laevis oocytes2000The Journal of pharmacology and experimental therapeutics, Jul, Volume: 294, Issue:1
Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier.
AID230646Ki (delta)/ Ki (mu) ratio of the compound1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID152052Selectivity ratio was determined by taking the ratio of Opioid receptor mu 1 to that of Opioid receptor delta 12001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
AID1676264Potency index, ratio of EC50 for N/OFQ(1-13)-NH2 to EC50 for test compound for agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incuba
AID149658Binding affinity against delta opioid receptor by displacement of radioligand [3H]DSLET in rat brain membrane1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID1600460Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cells2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Applications of amide isosteres in medicinal chemistry.
AID197665Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 15 degree celsius at 260 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID759747Agonist activity at delta opioid receptor in mouse vas deferens2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
AID1135800Relative binding affinity to Sprague-Dawley rat cerebellum opioid receptor assessed as inhibition of [3H]naloxone by scintillation counting relative to [Met5]enkephalin1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis, opiate receptor affinity, and conformational parameters of [4-tryptophan]enkephalin analogues.
AID149521Inhibition of binding of [3H][D-Ala2,D-Leu5]enkephalin to Opioid receptor delta 1 in the rat brain homogenate1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID615024Half life in human plasma2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
QSAR models for predicting enzymatic hydrolysis of new chemical entities in 'soft-drug' design.
AID1323816Antagonist activity at MOR in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists.
AID151441Inhibition of binding of [3H]naloxone to Opioid receptor mu 1 in the rat brain homogenate1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID226903Potency ratio was evaluated for mu receptor binding1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID229963IC50 ratio (GPI/MVD)1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID150066Potency towards Opioid receptor delta 1 relative to [Leu5 enkephalin]1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
AID1727072Agonist activity at human kappa opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID78158Concentration inhibiting electrically induced contraction of guinea pig ileum(GPI) at an ED50 >100(ug/kg).1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Synthesis and conformational properties of the lanthionine-bridged opioid peptide [D-AlaL2,AlaL5]enkephalin as determined by NMR and computer simulations.
AID187204Percentage content of phosphor in femur tested in the compound using male ICR rats2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
AID149951Ki ratio measured as the inhibitory effect against delta/mu receptor.1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID149745In vitro inhibitory activity was determined against Opioid receptor mu 1 in guinea pig ileum2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
AID476637Selectivity ratio of Ki for mu opioid receptor in rat brain membrane to Ki for delta opioid receptor in rat brain membrane2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
"Carba"-analogues of fentanyl are opioid receptor agonists.
AID229530Ratio of IC50 value using MVD to that of GPI assays.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID149781Binding affinity of Opioid receptor delta 1 by the displacement of delta-selective [3H]DSLET from brain membrane preparations.1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
AID152080Tested for binding affinity towards Opioid receptor mu 1 in rat and guinea pig brain membrane binding assays2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
AID1249925Displacement of [3H]diprenorphine from zebrafish mu opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
AID197672Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 35 degree celsius at 260 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID78684Relative narcotic agonistic activity was performed by inhibition of electrically evoked contractions compared with [Met5]-enkephalin (100%) in guinea pig ileum1980Journal of medicinal chemistry, Mar, Volume: 23, Issue:3
Synthesis, in vitro opiate activity, and intramolecular tyrosine--tryptophan distances of [4-tryptophan]enkephalin analogues. A reassessment of conformational models of enkephalin in solution.
AID476634Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
"Carba"-analogues of fentanyl are opioid receptor agonists.
AID101199Dissociation constant when the monoclonal antibody 3-E7 bound tightly to [Leu]enkephalin1998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
Investigations of azapeptides as mimetics of Leu-enkephalin.
AID1853220Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID1865318Agonist activity at human DOR-Galpha i/o assessed as phosphorylation of ERK 1/2 incubated for 5 mins in presence of pertussis toxin by Envision multilabel plate reader based alphascreen assay
AID1676262Potency index, ratio of EC50 for N/OFQ(1-13)-NH2 to EC50 for test compound for agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mi
AID1853214Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membrane incubated for 90 mins by liquid scintillation counting method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID150419Binding affinity towards non-selective opiate receptor2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Synthesis and binding affinity of neuropeptide Y at opiate receptors.
AID148006In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement.2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID149409Binding affinity against Opioid receptor kappa 1 of guinea pig brain membranes using 1 nM of (-)-[3H]ethylketazocine as radioligand1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Peptides as receptor selectivity modulators of opiate pharmacophores.
AID476632Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
"Carba"-analogues of fentanyl are opioid receptor agonists.
AID150068Binding affinity was determined by displacement of [3H]- DSLET at Opioid receptor delta 1 in rat brain membrane homogenates2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.
AID772822Displacement of [3H]-deltorphin 2 from delta opioid receptor in rat GH3 cells after 60 mins by scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
Systematic replacement of amides by 1,4-disubstituted[1,2,3]triazoles in Leu-enkephalin and the impact on the delta opioid receptor activity.
AID189557Relative potency in displacing [3H]- labeled DADLE in mouse brain homogenate1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
AID1572987Lipophilicity, log D of the compound at pH 7.42018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID1727081Stability in human plasma assessed as aminopeptidase N-mediated cleavage of Tyr1-Gly2 by measuring half life2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID232034Selectivity Ratio of IC50 of MVD to IC50 of GPI1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Synthesis and conformational properties of the lanthionine-bridged opioid peptide [D-AlaL2,AlaL5]enkephalin as determined by NMR and computer simulations.
AID138522Ke value for naloxone as antagonist (compound) was measured by using Mouse vas deferens (MVD) assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID680761TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.004 uM, Leu-enkephalin: 1000 uM) in Xenopus laevis oocytes2003The Journal of pharmacy and pharmacology, Jul, Volume: 55, Issue:7
Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1676261Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
AID476636Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
"Carba"-analogues of fentanyl are opioid receptor agonists.
AID1727071Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID150097Tested for binding affinity towards Opioid receptor delta 1 in rat and guinea pig brain membrane binding assays2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
AID149929Inhibition of [3H][D-Ala2,D-Leu5]enkephalin binding to Opioid receptor delta 1 in the rat brain homogenate1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID1206649Binding affinity to human delta opioid receptor-1 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID230842MVD/GPI IC50 ratio of the compound1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID141637Binding affinity for mu opioid receptors by displacement of [3H]-DAMGO from rat brain membrane binding site1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID1323818Metabolic stability in rat plasma assessed as compound remaining at 37 degC measured after 15 mins by reverse-phase HPLC analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists.
AID78307In vitro inhibition of electrically evoked contractions of the guinea pig ileum (GPI)1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID231502Ratio of binding affinity of mu and delta opioid receptor1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID1755982Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay2021Journal of natural products, 01-22, Volume: 84, Issue:1
Isolation and Pharmacological Characterization of Six Opioidergic
AID150975In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement.2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID149948The compound was tested for the ability to displace delta-receptor specific radioligand [3H]DPDPE1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
AID149216IC50 ratio measured as inhibitory potencies in mouse vas deferens and guinea pig ileum assays1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID148642In vitro inhibitory activity was determined against Opioid receptor delta 1 in mouse vas deferens2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
AID1676258Agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
AID1853219Agonist activity at FLAG-tagged mouse mu opioid receptor expressed in human HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by GloSensor assa2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID151767Evaluated for its ability to displace [3H]DAGO binding to Opioid receptor mu 1 from rat brain homogenate1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID1600452Drug metabolism in human plasma assessed as aminopeptidase N-mediated Tyr1-Gly2 cleavage by measuring half life2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Applications of amide isosteres in medicinal chemistry.
AID226902Potency ratio was evaluated for delta receptor binding1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID79049The compound was tested In vitro for the ability to inhibit electrically induced contractions of the guinea pig ileum1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
AID79045Tested for inhibition of electrically evoked contractions of the guinea pig ileum(GPI).1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID150259Displacement of [3H]naloxone from rat brain opioid receptors relative to [Met5]-enkephalin (100%)1980Journal of medicinal chemistry, Mar, Volume: 23, Issue:3
Synthesis, in vitro opiate activity, and intramolecular tyrosine--tryptophan distances of [4-tryptophan]enkephalin analogues. A reassessment of conformational models of enkephalin in solution.
AID192036Weight of rat body tested after intramuscular administration of 18 ug/kg of compound when compared to vehicle2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
AID1853213Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cell membrane measured after 90 mins by liquid scintillation counting method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID1727070Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID234885Potency to inhibit GPI relative to [Leu]enkephalin1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID1600459Agonist activity at mu opioid receptor (unknown origin) expressed in CHO cells2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Applications of amide isosteres in medicinal chemistry.
AID1727079Inhibition of [3H]-Deltorphin 2 binding to mouse delta opioid receptor expressed in HEK293 cell membranes incubated for 60 mins by Cheng-Prusoff analysis2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID80149Potency to inhibit electrically induced contraction of guinea pig ileum(GPI) relative to [Leu5]-enkephalin.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Synthesis and conformational properties of the lanthionine-bridged opioid peptide [D-AlaL2,AlaL5]enkephalin as determined by NMR and computer simulations.
AID1432895Displacement of [3H]DPN from zebrafish mu opioid receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides.
AID1206655Intrinsic efficacy at human delta opioid receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 45 mins by time-resolved fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID1755976Displacement of [3H]-DPDPE from human delta opioid receptor expressed in CHO-K1 cells by radioligand binding assay2021Journal of natural products, 01-22, Volume: 84, Issue:1
Isolation and Pharmacological Characterization of Six Opioidergic
AID149241Relative potency to induce 50% of maximal effect in mouse vas deferens expressing Opioid receptor delta 11983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
AID1755979Agonist activity at mouse FLAG-tagged delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent b2021Journal of natural products, 01-22, Volume: 84, Issue:1
Isolation and Pharmacological Characterization of Six Opioidergic
AID192047Weight of rat femur tested after intramuscular administration of 18 ug/kg of compound when compared to vehicle, prednisone, estradiol and estrone2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
AID197669Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 25 degree celsius1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID1432896Displacement of [3H]DPN from zebrafish delta 1a opioid receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides.
AID171530Percentage content of calcium in femur tested in the compound using male ICR rats2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
AID149239Ability to induce 50% of maximal effect in mouse vas deferens expressing Opioid receptor delta 11983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
AID149950Relative potency to that of [Leu5]- enkephalin1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
AID78306In vitro inhibition of electrically evoked contractions of guinea pig ileum(GPI)2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
AID151282Binding affinity was determined by displacement of [3H]- DAMGO at Opioid receptor mu 1 in rat brain membrane homogenates2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.
AID176221Effective dose was measured using in vivo rat hot plate test after intrathecal injection1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Synthesis and conformational properties of the lanthionine-bridged opioid peptide [D-AlaL2,AlaL5]enkephalin as determined by NMR and computer simulations.
AID1676259Potency index, ratio of EC50 for N/OFQ(1-13)-NH2 to EC50 for test compound for agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incuba
AID574414Apparent permeability across human Caco2 cells by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Feb-15, Volume: 19, Issue:4
Lipophilic derivatives of leu-enkephalinamide: in vitro permeability, stability and in vivo nasal delivery.
AID145926Concentration required to inhibit the specific binding of tritiated ligand [3H]DADL to opiate receptor by 50%1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Replacement of the peptide-backbone amides connecting Tyr-Gly and Gly-Gly in leucine-enkephalin with ketomethylene groups: synthesis and biological activity.
AID1206661Binding affinity to human delta opioid receptor expressed in CHO cells assessed as ERK1/2 phosphorylation2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID147912Binding affinity of Opioid receptor mu 1 mu 1 by the displacement of mu-selective [3H]DAGO from brain membrane preparations.1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
AID181511Ability to displace 50% of [3H]- labeled DADLE in mouse brain homogenate1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
AID76239Opioid agonist potencies was determined by electrically stimulated guinea pig ileum (GPI)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
AID1727061Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electric-field induced measured after 5 mins2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID152051The relative potency of compound was measured against mu opioid receptor to that of [Leu]enkephalin in [3H]DAGO binding assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID1249927Displacement of [3H]diprenorphine from zebrafish delta1b opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
AID149939Tested for binding affinity against delta opioid receptor by displacing [3H]- DSLET radioligand from rat brain membrane preparations1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
AID149301Inhibition of [3H]- ]DAMGO binding to opioid receptor mu from rat brain membrane1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID1676256Agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
AID224591Tested for binding affinity against mu opioid receptor fby displacing [3H]- DAMGO radioligand from rat brain membrane preparations1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
AID759745Agonist activity at mu opioid receptor in guinea pig ileum2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
AID149959The relative potency of compound was measured against delta opioid receptor to that of [Leu]enkephalin in [3H]DSLET binding assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID229266Ratio of IC50 in Mouse vas deferens and Guinea pig ileum assay1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID476633Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
"Carba"-analogues of fentanyl are opioid receptor agonists.
AID1676265Bias factor, selectivity for agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation to agonist activity at NOP (unknown origin) expressed in
AID1853216Agonist activity at FLAG-tagged mouse delta opioid receptor expressed in human HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by GloSensor a2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID132686Inhibition of electrically evoked contractions in mouse vas deferens1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID234886Potency to inhibit MVD relative to [Leu]enkephalin1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID224413In vitro inhibition of electrically evoked contractions of mouse vas deferens(MVD)2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
AID1676257Potency index, ratio of EC50 for N/OFQ(1-13)-NH2 to EC50 for test compound for agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mi
AID1572990Activation of kappa opioid receptor (unknown origin) expressed in CHO cells2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID151586Binding affinity for Opioid receptor mu 1 determined by displacing [3H]DAMGO from rat brain membrane binding sites1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
AID1600457Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Applications of amide isosteres in medicinal chemistry.
AID77779Ke value for naloxone versus compound in the guinea pig ileum (GPI) in order to distinguish between mu- and delta-mediated effects1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
AID1432897Displacement of [3H]DPN from zebrafish delta 1b opioid receptor expressed in HEK293 cell membranes after 4 hrs by scintillation counting method2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides.
AID149069In vitro binding affinity to human Opioid receptor delta 1 on CHO cell membranes using [3H]diprenorphine displacement.2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID132522Concentration inhibiting electrically induced contraction of mouse vas deferens(MVD) at an ED50 >100(ug/kg).1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Synthesis and conformational properties of the lanthionine-bridged opioid peptide [D-AlaL2,AlaL5]enkephalin as determined by NMR and computer simulations.
AID149813Displacement of [3H]DSLET from Opioid receptor delta 1 from rat brain homogenate1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID141638Potency against mu opioid receptors relative to [Leu5]-enkephalin1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID151752Binding affinity was determined towards Opioid receptor mu 1 in rat brain synaptosomes using [3H]DAMGO as radioligand.2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
AID149249Binding affinity for delta opioid receptors was determined by displacement of [3H]DSLET from rat brain membrane binding site1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID476635Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
"Carba"-analogues of fentanyl are opioid receptor agonists.
AID138361The compound was tested In vitro for the ability to inhibit electrically induced contractions of the mouse vas deferens1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
AID149316Potency to inhibit 3H ]DAMGO binding to opioid receptor mu relative to [Leu]enkephalin1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID150417Inhibitory activity against non-selective opiate receptor2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Synthesis and binding affinity of neuropeptide Y at opiate receptors.
AID1853217Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID168222Activity of alkaline phosphatase (ALP) tested in serum of rat when 18 ug/kg of compound was administered intramuscularly2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
AID79204Tested for sensitivity to naloxone in the guinea pig ileum assay.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID76094Inhibition of electrically evoked contractions in Guinea pig ileum1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID1676263Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
AID1865319Agonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation level
AID149660Binding affinity for Opioid receptor delta 1 determined by displacing [3H]-DSLET from rat brain membrane binding sites1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
AID197666Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 15 degree celsius at 284 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID138345Concentration of compound to inhibit 50% (IC50) electrically evoked contractions was tested in Mouse vas deferens (MVD) assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID148570Binding affinity towards Opioid receptor kappa 1 was determined using U69,593 as the radioligand.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.
AID228162Binding affinity towards human kappa,mu,delta receptors was calculated as the ratio; 1/<0.06/<0.00072003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
AID1727062Half life in Sprague-Dawley rat plasma measured after 60 mins by HPLC method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID233603Ratio of Ki value towards delta receptor to that of mu receptor.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID232431Ratio of inhibition of electrically induced contractions in GPI and MVD1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
AID197667Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 20 degree celsius at 260 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID224710Relative potency to that of [Leu5]- enkephalin1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
AID149221Potency relative to [Leu5]-enkephalin in mouse vas deferens1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID1853215Selectivity ratio, ratio of Ki for displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membrane to Ki for displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cell membrane2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID149314Selectivity ratio against Opioid receptor mu and delta binding1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID1853221Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring maximum efficacy measured after 90 mins by PathHunter assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID1600456Half life in rat plasma2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Applications of amide isosteres in medicinal chemistry.
AID1206647Intrinsic efficacy at human delta opioid receptor-1 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID197673Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 35 degree celsius at 284 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID149252Potency against delta opioid receptors relative to [Leu5]-enkephalin1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID197668Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 20 degree celsius at 284 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID1206659Intrinsic efficacy at human delta opioid receptor expressed in F1pIn CHO cells assessed as ERK1/2 phosphorylation2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID151911The compound was tested for the ability to displace Opioid receptor mu 1 specific radioligand [3H]DAGO1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
AID1727073Selectivity ratio of EC50 for human mu opioid receptor expressed in CHO-K1 cells to EC50 for human delta opioid receptor expressed in CHO-K1 cells2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID138360Tested for inhibition of electrically evoked contractions of the mouse vas deferens(MVD).1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID1853218Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring maximum efficacy measured after 90 mins by PathHunter assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.
AID234361Ratio was determined by taking the value of guinea pig ileum to that of mouse vas deferens2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
AID140433Potency to inhibit electrically induced contraction of mouse vas deferens(MVD) relative to [Leu5]-enkephalin.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Synthesis and conformational properties of the lanthionine-bridged opioid peptide [D-AlaL2,AlaL5]enkephalin as determined by NMR and computer simulations.
AID149348Inhibition of [3H]- ]DSLET binding to opioid receptor delta from rat brain membrane1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID151600Binding affinity against mu opioid receptor by displacement of radioligand [3H]DAGO in rat brain membrane1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID197671Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 30 degree celsius at 284 nm1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID149913Binding affinity against Opioid receptor delta 1 of guinea pig brain membranes using 1 nM of [3H]DADLE as radioligand1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Peptides as receptor selectivity modulators of opiate pharmacophores.
AID151622Binding affinity towards Opioid receptor mu 1 was determined using ([d-Ala2,MePhe4, Gly5-ol]-enkephalin (DAMGO) as the radioligand.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.
AID79202Ke value for naloxon as antagonist (compound) was measured by using Guinea pig ileum assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID1727074Selectivity ratio of EC50 for human kappa opioid receptor expressed in CHO-K1 cells to EC50 for human delta opioid receptor expressed in CHO-K1 cells2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID149357Potency to inhibit [3H]- ]DSLET binding to delta receptor relative to [Leu]enkephalin1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Conformationally restricted deltorphin analogues.
AID141518Potency relative to [Leu5]-enkephalin in guinea pig ileum1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID151891Inhibition of binding of [3H]naloxone to Opioid receptor mu 1 in the rat brain homogenate1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID1206657Binding affinity to human delta opioid receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 45 mins by time-resolved fluorescence assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
AID148045Binding affinity against Opioid receptor mu 1 of guinea pig brain membranes using 0.5 nM of [3H]naloxone as radioligand1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Peptides as receptor selectivity modulators of opiate pharmacophores.
AID1676260Bias factor, selectivity for agonist activity at MOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation to agonist activity at NOP (unknown origin) expressed in
AID148951Inhibition of naloxone activity in mouse vas deferens assay for Opioid receptor delta 11982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID149898Binding affinity towards Opioid receptor delta 1 was determined using [d-Ser2, Leu5, Thr6] enkephalin (DSLET) as the radioligand.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.
AID231530Ratio of binding affinity towards Mu opioid receptor to delta opioid receptor2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
AID149867Inhibitory potency against Opioid receptor mu 1 in the guinea pig ileum assay1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID1727077Half-life in Sprague-Dawley rat plasma at 50 uM measured by LC-MS/MS analysis2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID197674Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) and expressed as apparent dissociation constant at 5 degree celsius1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide.
AID149949The compound was tested for the ability to displace delta-receptor specific radioligand [3H]DSLET1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
AID147893Sensitivity to naloxone against Opioid receptor mu 1 in the guinea pig ileum assay1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
AID149797Binding affinity was determined towards Opioid receptor delta 1 in rat brain synaptosomes using [3H]deltorphin II as radioligand.2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
AID132668In vitro inhibition of electrically evoked contractions of the mouse vas deferens (MVD)1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
AID171529Activity tested for the content of calcium in serum of rat when 18 ug/kg of compound was administered intramuscularly when compared to vehicle and prednisone2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
AID192040Weight of rat femur ash tested after intramuscular administration of 18 ug/kg of compound when compared to vehicle2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
AID1727078Half-life in human plasma at 50 uM measured by LC-MS/MS analysis2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID138530The relative potency of compound was measured by comparing with [Leu]enkephalin in Mouse vas deferens (MVD) assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID234906Relative potency was determined between the MVD assay and the [3H]DSLET binding assay.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
AID78873Concentration of compound to inhibit 50% (IC50) electrically evoked contractions was tested in Guinea pig ileum(GPI) assay.1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
AID1346364Human mu receptor (Opioid receptors)1998NIDA research monograph, Mar, Volume: 178Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1346411Rat kappa receptor (Opioid receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21
Cloning and pharmacological characterization of a rat kappa opioid receptor.
AID1346373Mouse delta receptor (Opioid receptors)1994Molecular pharmacology, Feb, Volume: 45, Issue:2
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
AID1346361Human delta receptor (Opioid receptors)1998NIDA research monograph, Mar, Volume: 178Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10,836)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905045 (46.56)18.7374
1990's3748 (34.59)18.2507
2000's1203 (11.10)29.6817
2010's702 (6.48)24.3611
2020's138 (1.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.95

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index44.95 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index63.00 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (44.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials80 (0.69%)5.53%
Trials0 (0.00%)5.53%
Reviews672 (5.83%)6.00%
Reviews1 (20.00%)6.00%
Case Studies42 (0.36%)4.05%
Case Studies0 (0.00%)4.05%
Observational10 (0.09%)0.25%
Observational0 (0.00%)0.25%
Other10,720 (93.02%)84.16%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]