Assay ID | Title | Year | Journal | Article |
AID256772 | Selectivity for rat mu opioid receptor over delta opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1). |
AID139793 | Delta or Mu antagonist activity tested in mouse vas deferens (MVD) along with, naloxone | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
| Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties. |
AID235157 | Selectivity ratio for mu and delta opioid receptors | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. |
AID149401 | Inhibition of [3H][p-Cl-Phe-]DPDE binding to rat brain homogenate delta-opioid receptor | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. |
AID151609 | Binding affinity against Opioid receptor mu 1 using [3H]DAMGO in rat brain synaptosomes was determined | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity. |
AID148079 | Binding affinity at cloned human delta-opioid receptor | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID224551 | Concentration required to inhibit electrically induced twitch by 50% in mouse vas deferens(MVD). | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites. |
AID256771 | Displacement of [3H]DAMGO from rat mu opioid receptor in brain P2 synaptosomes | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1). |
AID148154 | Agonist potency using GTP-gamma [35S]- binding assay for opioid receptor kappa 1; Inactive | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID149319 | Ratio of the binding constant against opioid receptor mu and opioid receptor delta | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites. |
AID233440 | Selectivity ratio measured as the Ki value of mu receptor to that of delta receptor | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues. |
AID398174 | Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membrane | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
| Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2. |
AID148640 | In vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferens | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. |
AID149348 | Inhibition of [3H]- ]DSLET binding to opioid receptor delta from rat brain membrane | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID239304 | Inhibition of [3H]naloxone binding to rat brain homogenate Opioid receptor delta | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
| 6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides. |
AID147905 | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of guinea pig brain | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
| Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids. |
AID234202 | Ratio of the inhibitory concentrations against MVD and GPI. | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites. |
AID132686 | Inhibition of electrically evoked contractions in mouse vas deferens | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID270135 | Agonist activity at delta opioid receptor assessed as inhibition of electrically-evoked contraction of mouse vas deferens | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore. |
AID149301 | Inhibition of [3H]- ]DAMGO binding to opioid receptor mu from rat brain membrane | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID108533 | Antinociceptive activity after subcutaneous administration in mice. | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
| Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration. |
AID151765 | Displacement of [3H]DAGO (1.28 nM) from Opioid receptor mu 1 | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
| Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides. |
AID149357 | Potency to inhibit [3H]- ]DSLET binding to delta receptor relative to [Leu]enkephalin | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID224591 | Tested for binding affinity against mu opioid receptor fby displacing [3H]- DAMGO radioligand from rat brain membrane preparations | 1993 | Journal 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. |
AID149729 | Agonist activity was evaluated in guinea pig ileum (GPI) preparations at Opioid receptor mu 1 | 1997 | Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
| Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) |
AID277680 | Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID76378 | Tested for inhibition of amplification of electrically induced twitch in guinea pig ileum (GPI) | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. |
AID141643 | Inhibition of [3H]CTOP binding to rat brain homogenate mu-opioid receptor | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. |
AID148516 | Agonist activity was evaluated in guinea pig ileum (GPI) preparations at Opioid receptor delta 1 | 1997 | Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
| Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) |
AID149119 | Inhibition of [3H]- U 69593 from Opioid receptor kappa 1 of guinea pig brain | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
| Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids. |
AID149796 | Binding affinity was determined on delta [3H]DPDPE site in rat brain synaptosomes by radioreceptor assay | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. |
AID148532 | Functional biological activity for Opioid receptor delta 1 was determined in vitro, on mouse vas deferens (MVD). | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues. |
AID149316 | Potency to inhibit 3H ]DAMGO binding to opioid receptor mu relative to [Leu]enkephalin | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID149091 | Displacement of [3H]NLT from Opioid receptor delta 1 of adult male mouse brain. | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
| Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration. |
AID228359 | Ratio of delta-Opioid receptor to the mu-opioid receptor | 1997 | Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
| Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. |
AID148639 | In vitro biological activity by electrically induced smooth muscle contractions in mouse vas deferens (Opioid receptor delta 1); inhibitory concentration was evaluated | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity. |
AID138349 | In vitro concentration required to inhibit electrically evoked twitch in isolated mouse vas deferens. | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
| Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration. |
AID149350 | Binding affinity against opioid receptor delta in rats by displacing [3H]DPDPE | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites. |
AID149812 | Displacement of [3H]DPDPE (0.63 nM) from Opioid receptor delta 1 | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
| Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides. |
AID310939 | Displacement of [3H]naltrindole from rat delta opioid receptor expressed in C6 cells | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity. |
AID152235 | Agonist potency using GTP-gamma [35S]- binding assay for mu-opioid receptor | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID138857 | In vitro inhibition of electrically evoked contractions in guinea pig ileum longitudinal muscle myenteric plexus | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. |
AID227065 | IC50 ratio measured as the IC50 value of GPI to that of MVD. | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues. |
AID314190 | Antagonist activity at delta opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
| Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
AID235354 | Relative binding to mu and delta opioid receptors (ratio of Ki) | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
| Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids. |
AID151611 | Binding affinity for rat brain P2 synaptosome Opioid receptor mu 1 | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
| Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties. |
AID147950 | Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID149308 | Binding affinity against opioid receptor mu in rats by displacing [3H]-DAGO | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites. |
AID23166 | Half-life time of enzymatic breakdown in mouse brain. | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
| Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration. |
AID149939 | Tested for binding affinity against delta opioid receptor by displacing [3H]- DSLET radioligand from rat brain membrane preparations | 1993 | Journal 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. |
AID229963 | IC50 ratio (GPI/MVD) | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID229342 | Ratio of inhibitory concentration of guinea pig ileum to mouse vas deferens was determined | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity. |
AID151895 | Opioid receptor mu 1 binding affinity by displacement of radioligand [3H][DAla,MePhe,Gly-ol]enkephalin (DAGO) from rat brain membrane synaptosomes | 1997 | Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
| Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. |
AID223198 | Concentration required to inhibit electrically induced twitch by 50% in guinea pig ileum(GPI). | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites. |
AID149935 | Opioid receptor delta 1 binding affinity by displacement of radioligand [3H][D-Pen]-enkephalin (DPDPE) from rat brain membrane synaptosomes | 1997 | Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
| Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. |
AID224710 | Relative potency to that of [Leu5]- enkephalin | 1993 | Journal 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. |
AID231652 | Binding ratio between delta and mu receptor was determined | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. |
AID139792 | Delta or Mu antagonist activity tested in mouse vas deferens (MVD) along with N,N-dimethyl-Dmt-Tic-OH | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
| Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties. |
AID149950 | Relative potency to that of [Leu5]- enkephalin | 1993 | Journal 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. |
AID229970 | IC50 ratio on Mu receptor of GPI to the delta receptor MVD | 1997 | Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
| Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) |
AID235155 | Selectivity ratio against guinea pig ileum and mouse vas deferens contractions | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. |
AID151268 | Displacement of [3H]-DAGO from Opioid receptor mu 1 of adult male mouse brain. | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
| Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration. |
AID79023 | In vitro concentration required to inhibit electrically evoked twitch in isolated guinea pig ileum. | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
| Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration. |
AID230636 | Ratio, binding to cloned human kappa-opioid versus delta-opioid receptor (IC50) | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID234886 | Potency to inhibit MVD relative to [Leu]enkephalin | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID149296 | Inhibition of [3H]DAGO binding to trat brain opioid receptor mu in P2 membrane | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Function of negative charge in the "address domain" of deltorphins. |
AID149651 | Affinity was assessed using competitive binding assay labeled with [3H]DPDPE (6.3 nM) for Opioid receptor delta 1 | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues. |
AID78287 | Functional biological activity for mu opioid receptor was determined in vitro, on guinea pig ileum (GPI). | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues. |
AID138859 | Inhibitory concentration against electrically evoked contractions of guinea pig ileum longitudinal muscle-myenteric plexus | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors. |
AID149670 | Binding affinity against Opioid receptor delta 1 using [3H]DT in rat brain synaptosomes was determined | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity. |
AID152236 | Compound was tested for maximum stimulation of mu opioid receptor by GTP-gamma [35S]- binding assay | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID149344 | Inhibition of [3H]-DADLE binding to opioid receptor delta in P2 membrane preparation of rat brain | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Function of negative charge in the "address domain" of deltorphins. |
AID239267 | Inhibition of [3H]naloxone binding to rat brain homogenate Opioid receptor mu | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
| 6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides. |
AID149672 | Binding affinity at Opioid receptor delta 1 using rat brain receptor (P2 synaptosome) assay | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
| Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties. |
AID149777 | Inhibition of [3H]- DPDPE binding to delta opioid receptor of guinea pig brain | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
| Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids. |
AID256770 | Displacement of [3H]deltorphin II from rat delta opioid receptor in brain P2 synaptosomes | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1). |
AID231661 | Bioselectivity ratio of compound as guinea pig ileum to mouse vas deferens was determined | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. |
AID23167 | Half-life time of enzymatic breakdown in mouse liver. | 1999 | Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
| Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration. |
AID148071 | Maximum stimulation of delta opioid receptor by GTP-gamma [35S]- binding assay | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID105933 | Negative logarithm of the molar concentration required to produce 50% of the maximum effect in mu receptor from mouse vas deferens (MVD) | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
| Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties. |
AID310938 | Agonist activity at rat delta opioid receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to BW373U86 | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity. |
AID147812 | Agonist activity for Opioid receptor delta 1 | 1997 | Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
| Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity. |
AID76094 | Inhibition of electrically evoked contractions in Guinea pig ileum | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID151595 | Affinity was assessed using competitive binding assay labeled with [3H]- DAGO (1.28 nM) for Opioid receptor mu 1 | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues. |
AID167727 | Bioactivity in vitro in rabbit jejunum (RJ) isolated organ preparation | 1997 | Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
| Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. |
AID256773 | Functional bioactivity against delta opioid receptor in mouse vas deferens | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1). |
AID152240 | Binding affinity at cloned human mu-opioid receptor | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID228347 | Ratio of Ki values for mu and delta opioid receptors. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Function of negative charge in the "address domain" of deltorphins. |
AID256774 | Functional bioactivity against mu opioid receptor in guinea-pig ileum | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1). |
AID234885 | Potency to inhibit GPI relative to [Leu]enkephalin | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID131044 | Compound was tested in vivo by a mouse tail-flick assay after intracerebroventricular (icv) injection | 1997 | Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
| Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. |
AID147860 | Binding affinity at cloned human opioid receptor kappa 1 | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID149736 | Compound was evaluated for its inhibitory activity towards Opioid receptor mu 1 of guinea pig ileum (GPI) | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
| Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides. |
AID314186 | Displacement of [3H]naltrindole from delta opioid receptor in rat brain membranes | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
| Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
AID231027 | Ratio, binding to cloned human mu-opioid versus delta-opioid receptor (IC50) | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
| Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors. |
AID224589 | Binding affinity was determined on mu [3H]DAGO site in rat brain synaptosomes by radioreceptor assay | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. |
AID152083 | The selectivity ratio as the ratio of Ki of Opioid receptor mu 1 to Ki of Opioid receptor delta 1 | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity. |
AID148525 | Inhibitory activity against Opioid receptor delta 1 of mouse vas deferens (MVD) | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
| Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides. |
AID149314 | Selectivity ratio against Opioid receptor mu and delta binding | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Conformationally restricted deltorphin analogues. |
AID148649 | Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors. |
AID149743 | In vitro biological activity by electrically induced smooth muscle contractions in guinea pig ileum (Opioid receptor mu 1); inhibitory concentration was evaluated | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity. |
AID132850 | Tested for inhibition of amplification of electrically induced twitch in mouse vas deferens (MVD) | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. |
AID235156 | Selectivity ratio (GPI/MVD) of the compound | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |