biphalin: enkephalin dimer; two fragments of Ala(2)-enkephalin are connected by a diamine bridge to form above cpd; structure given in first source
ID Source | ID |
---|---|
PubMed CID | 5487663 |
CHEMBL ID | 200199 |
MeSH ID | M0151984 |
Synonym |
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83916-01-2 |
enkephalin dimer |
(tyr-ala-gly-phe-nh2)2 |
biphalin |
bdbm21014 |
chembl200199 , |
(2s)-2-amino-n-[(1r)-1-[({[(1s)-1-{n''-[(2s)-2-{2-[(2r)-2-[(2s)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]hydrazinecarbonyl}-2-phenylethyl]carbamoyl}methyl)carbamoyl]ethyl]-3-(4-hydroxyphenyl)propanamide |
bis(tyr-ala-gly-phenh2)hydrazide |
d-enk-o |
bis(tyrosyl-alanyl-glycyl-phenylalaninamide)hydrazide |
l-phenylalanine, n-(n-(n-l-tyrosyl-d-alanyl)glycyl)-, 2-(n-(n-(n-l-tyrosyl-d-alanyl)glycyl)-l-phenylalanyl)hydrazide |
d-enk |
(tyrosyl-alanyl-glycyl-phenylalaninamide)dimer |
dala(2) |
(2s)-2-amino-n-[(2r)-1-[[2-[[(2s)-1-[2-[(2s)-2-[[2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]-3-(4-hydroxyphen |
DTXSID80232802 |
Q3639770 |
(2s,2's)-n,n'-((2r,8s,13s,19r)-8,13-dibenzyl-3,6,9,12,15,18-hexaoxo-4,7,10,11,14,17-hexaazaicosane-2,19-diyl)bis(2-amino-3-(4-hydroxyphenyl)propanamide) |
AKOS040746625 |
Biphalin, is a palindromic peptide in which two opioid pharmacophores are connected "tail-to-tail" Biphalin is a new type of opioid peptide analog with high analgesic potency.
Biphalin is a highly potent analgesic, as potent as or more than ethorphine. Biphalin has also been shown to cross both the blood-brain and blood-cerebrospinal fluid barriers.
Excerpt | Reference | Relevance |
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"Biphalin has excellent binding affinity for μ and δ receptors and it is a highly potent analgesic, as potent as or more than ethorphine." | ( Structure-activity relationships of biphalin analogs and their biological evaluation on opioid receptors. Cacciatore, I; Costante, R; Feliciani, F; Lucente, G; Mollica, A; Pinnen, F; Stefanucci, A, 2013) | 1.39 |
"Biphalin has also been shown to cross both the blood-brain and blood-cerebrospinal fluid barriers." | ( Brain and spinal cord distribution of biphalin: correlation with opioid receptor density and mechanism of CNS entry. Abbruscato, TJ; Davis, TP; Hruby, VJ; Thomas, SA, 1997) | 1.29 |
Biphalin did not cause any toxic effect on HCECs at concentrations lower than 100μM. Biphalin displays a strong affinity for μ and δ-opioid receptors, and a significant to κ-receptor.
Excerpt | Reference | Relevance |
---|---|---|
"Biphalin did not cause any toxic effect on HCECs at concentrations lower than 100μM at various incubation time points. " | ( The opioid peptide biphalin modulates human corneal epithelial wound healing in vitro. Gedar Totuk, OM; Kabadayi, K; Mollica, A; Sahin, A; Yildiz, E, 2021) | 2.39 |
"Biphalin displays a strong affinity for μ and δ-opioid receptors, and a significant to κ-receptor." | ( Biphalin analogs containing β(3)-homo-amino acids at the 4,4' positions: Synthesis and opioid activity profiles. Frączak, O; Kosson, P; Lasota, A; Leśniak, A; Lipkowski, AW; Muchowska, A; Olma, A, 2015) | 2.58 |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Substance-P receptor | Rattus norvegicus (Norway rat) | Ki | 0.0014 | 0.0007 | 0.1298 | 1.0000 | AID1798027; AID1798029 |
Substance-P receptor | Homo sapiens (human) | Ki | 0.0014 | 0.0000 | 0.7936 | 8.7470 | AID1798027 |
Substance-P receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0026 | 0.0013 | 0.6913 | 3.4000 | AID288852 |
Delta-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 0.0104 | 0.0001 | 0.7298 | 10.0000 | AID258261; AID275396; AID749871 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0060 | 0.0001 | 0.8874 | 10.0000 | AID258263 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0016 | 0.0000 | 0.3845 | 8.6000 | AID1798026; AID1798027; AID1798028; AID1798029; AID288853; AID320354; AID391164; AID422077; AID452777; AID497530; AID592524; AID749873 |
Mu-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0014 | 0.0001 | 0.8133 | 10.0000 | AID141766; AID258261 |
Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0120 | 0.0000 | 0.4197 | 10.0000 | AID1497783 |
Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0022 | 0.0002 | 0.7521 | 8.0140 | AID150084; AID258260; AID258262; AID275394 |
Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.0027 | 0.0000 | 0.5978 | 9.9300 | AID1497784; AID1798026; AID1798028; AID1798029; AID288852; AID391163; AID422076; AID452776; AID497531; AID592523; AID749872 |
Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.2700 | 0.0000 | 0.3624 | 10.0000 | AID1497785 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0025 | 0.0002 | 0.6603 | 10.0000 | AID258262 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0014 | 0.0000 | 0.2786 | 9.0000 | AID749873 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Delta-type opioid receptor | Mus musculus (house mouse) | EC50 (µMol) | 0.0215 | 0.0011 | 0.4014 | 4.8000 | AID1164344; AID1164347; AID320353; AID497533 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0090 | 0.0000 | 0.0647 | 0.9320 | AID1164347; AID749865 |
Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0010 | 0.0000 | 0.3263 | 9.4000 | AID1379397 |
Delta-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0012 | 0.0000 | 0.4332 | 8.3000 | AID1379398; AID261096; AID275394; AID288855; AID320353; AID320360; AID391169; AID422082; AID452780; AID497533; AID592532; AID749867 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | EC50 (µMol) | 0.0011 | 0.0000 | 0.0493 | 0.9320 | AID288855; AID320360 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID729093 | Antinociceptive activity in CD1 mouse assessed as tail withdrawal latency at 3000 nmol, iv measured after 15 to 60 mins by tail flick test relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID391174 | Agonist activity at mu opioid receptor in Hartley guinea pig ileum longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID749873 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membranes | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID241678 | In vitro inhibition of [3H]DAMGO binding to Opioid receptor mu | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers. |
AID1497783 | Binding affinity to MOR (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors. |
AID452781 | Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding relative to untreated basal control | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
AID391164 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membrane by liquid scintillation counting | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID1497784 | Binding affinity to DOR (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors. |
AID261096 | Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. |
AID1379396 | Half life in human plasma at 100 ug/ml by HPLC method | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID258264 | Activity at delta opioid receptor in mouse vas deferens | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Synthesis and biological activity of the first cyclic biphalin analogues. |
AID592532 | Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
AID729094 | Antinociceptive activity in CD1 mouse assessed as paw licking and jumping latency at 3000 nmol, iv measured after 15 to 60 mins by hot plate test relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID422077 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membrane | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID1497785 | Binding affinity to KOR (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors. |
AID422082 | Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID150084 | In vitro binding affinity towards Opioid receptor delta 1 was determined using [3H]-DAMGO or [3H]CTOP | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18 | Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin. |
AID275394 | Activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2007 | Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1 | Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. |
AID729101 | Displacement of [3H]Deltorphin from DOR in Sprague-Dawley rat brain membrane after 180 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID592524 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cells | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
AID288860 | Agonist activity at mu opioid receptor in Hartley guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID729099 | Inhibition of DOR in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction after 3 mins | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID1379389 | Agonist activity at heteromeric G-protein in Wistar rat whole brain membranes after 30 mins by [35S]GTPgammaS binding assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID261098 | Agonist activity at delta opioid receptor by inhibition of muscle contraction in electrically stimulated isolated mouse vas deferens | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. |
AID1604708 | Antinociceptive activity in CD1 mouse assessed as reduction in thermal nociception at 1.5 umol/kg, iv dosed 15 mins before test and measured after 15 to 120 mins post compound dose by hot plate test | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID288855 | Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID749876 | Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID1164349 | Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID1379398 | Binding affinity to DOR (unknown origin) | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID258265 | Activity at mu opioid receptor in longitudinal muscle myenteric plexus from guinea pig ileum | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Synthesis and biological activity of the first cyclic biphalin analogues. |
AID391169 | Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID749864 | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay relative to control | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID391170 | Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay relative to control | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID288852 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID1164347 | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID422147 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID320363 | Agonist activity at mu opioid receptor in Hartley guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID452780 | Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
AID592525 | Selectivity ratio of Ki for rat mu opioid receptor to Ki for human delta opioid receptor | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
AID422078 | Selectivity ratio, Ki for rat mu opioid receptor to Ki for human delta opioid receptor | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID422076 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membrane | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID1379388 | Selectivity ratio of Ki for displacement of [3H]lleDelt2 from DOR in Wistar rat whole brain membranes to displacement of [3H]DAMGO from MOR in Wistar rat whole brain membranes | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID241045 | In vitro agonist activity against Opioid receptor delta in mouse vas deferens | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers. |
AID241774 | In vitro inhibition of [3H]DPDPE binding to Opioid receptor delta | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers. |
AID391173 | Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID1164345 | Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to untreated control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID729095 | Antinociceptive activity in CD1 mouse assessed as paw licking and jumping latency at 0.6 nmol, icv measured after 30 to 45 mins by hot plate test relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID320362 | Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID320360 | Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID592533 | Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
AID320354 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cells | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID1604711 | Antinociceptive activity in CD1 mouse assessed as reduction in nociception response during early phase at 0.15 umol,sc dosed 15 mins before test by formalin test | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID1379387 | Displacement of [3H]lleDelt2 from DOR in Wistar rat whole brain membranes after 45 mins by liquid scintillation counting method | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID1633379 | Analgesic activity in CD1 mouse at 1.5 nmol, iv measured after 45 mins by hot plate test relative to control | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
AID1164355 | Antinociceptive activity in CD1 mouse assessed as reduction in thermal nociception by at 0.1 nmol, icv measured 15 mins post dose by hot plate test | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID1379397 | Binding affinity to MOR (unknown origin) | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID1164344 | Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID422083 | Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay relative to basal level | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID749867 | Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID749872 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membranes | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID1164343 | Displacement of [3H]U69593 from kappa opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID258262 | Agonistic efficacy at human delta opioid receptor by [35S]GTP-gammaS binding assay | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Synthesis and biological activity of the first cyclic biphalin analogues. |
AID138328 | Concentration of compound required for evaluating efficacy in mouse vas deferens (MVD) | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18 | Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin. |
AID497532 | Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding relative to control | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
AID452785 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated contraction | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
AID391163 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membrane by liquid scintillation counting | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID422149 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID729097 | Inhibition of MOR in Hartley guinea pig ileum longitudinal muscle myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction after 3 mins | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID592530 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
AID275397 | Activity at mu opioid receptor assessed as contraction of electrically-stimulated Hartley guinea pig ileum | 2007 | Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1 | Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. |
AID288861 | Ratio of IC50 for mu opioid receptor in GPI assay to IC50 for delta opioid receptor in MVD assay | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID320358 | Ratio of Ki for human delta opioid receptor over Ki for rat mu opioid receptor | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID141766 | In vitro binding affinity towards mu opioid receptors was determined using [3H][p-Cl-Phe]- 4] DPDPE or [3H]deltorphin II | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18 | Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin. |
AID258263 | Agonistic efficacy at rat mu opioid receptor by [35S]GTPgammaS binding assay | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Synthesis and biological activity of the first cyclic biphalin analogues. |
AID1164348 | Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to untreated control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID261099 | Agonist activity at mu opioid receptor by inhibition of muscle contraction in electrically stimulated isolated guinea pig ileum | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. |
AID749871 | Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID729098 | Selectivity ratio of Ki for MOR in Sprague-Dawley rat brain membrane to Ki for DOR in Sprague-Dawley rat brain membrane | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID729091 | Antinociceptive activity in CD1 mouse assessed as paw licking and jumping latency at 0.6 nmol, icv measured after 15 to 30 mins by hot plate test | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID264439 | Agonist activity at delta opioid receptor assessed as inhibition of electrically stimulated ICR mouse vas deferens contraction | 2006 | Journal of medicinal chemistry, May-18, Volume: 49, Issue:10 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
AID452776 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
AID729090 | Antinociceptive activity in CD1 mouse assessed as tail withdrawal latency at 0.6 nmol, icv measured after 15 to 30 mins by tail flick test | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID1379386 | Displacement of [3H]DAMGO from MOR in Wistar rat whole brain membranes after 45 mins by liquid scintillation counting method | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID749865 | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID497533 | Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
AID497531 | Displacement of [3H]DPDPE from human delta opioid receptor | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
AID1633378 | Analgesic activity in CD1 mouse at 0.15 nmol, icv measured after 60 mins by hot plate test relative to control | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
AID749866 | Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay relative to control | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID320353 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID729096 | Ratio of IC50 for MOR in Hartley guinea pig ileum longitudinal muscle myenteric plexus to IC50 for DOR in ICR mouse vas deferens | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID288865 | Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay relative to control | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID288853 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID497530 | Displacement of [3H]DPDPE from rat mu opioid receptor | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
AID1164341 | Displacement of [3H]Ile5,6deltorphin II from delta opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID1164346 | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to untreated control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID275396 | Activity at delta opioid receptor in ICR mouse by MVD assay | 2007 | Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1 | Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. |
AID1164350 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-induced smooth muscle contraction | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID1164356 | Antinociceptive activity in CD1 mouse assessed as reduction in thermal nociception by measuring tail-flick latency at 0.1 nmol, icv measured 15 mins post dose by tail-flick assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID78835 | Concentration of compound required for evaluating efficacy in guinea pig ileum (GPI) | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18 | Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin. |
AID258260 | Displacement of [3H]DPDPE from delta opioid receptor | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Synthesis and biological activity of the first cyclic biphalin analogues. |
AID729100 | Displacement of [3H]DAMGO from MOR in Sprague-Dawley rat brain membrane after 180 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides. |
AID1164342 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID1379395 | Analgesic activity in formalin-induced nociception Harlan CD-1 mouse model assessed as reduction in time spent in licking or biting formalin injected hind paw during inflammatory phase at 0.1 nmol, sc pretreated for 15 mins followed by formalin induction | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID288859 | Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID264440 | Agonist activity at mu opioid receptor assessed as inhibition of electrically stimulated Hartley guinea pig ileum contraction | 2006 | Journal of medicinal chemistry, May-18, Volume: 49, Issue:10 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
AID391165 | Ratio of Ki for rat mu opioid receptor to Ki for human delta opioid receptor | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID258261 | Displacement of [3H]DAMGO from mu opioid receptor | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Synthesis and biological activity of the first cyclic biphalin analogues. |
AID592523 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
AID241971 | In vitro agonist activity against Opioid receptor mu in guinea pig ileum/longitudinal muscle myenteric plexus | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers. |
AID592529 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
AID1604712 | Antinociceptive activity in CD1 mouse assessed as reduction in nociception response during late phase at 0.15 umol,sc dosed 15 mins before test by formalin test | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID1164352 | Agonist activity at mu opioid receptor in Hartley guinea pig ileum longitudinal muscle myenteric plexus assessed as inhibition of electrically-induced smooth muscle contraction | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
AID452777 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
AID1379394 | Analgesic activity in formalin-induced nociception Harlan CD-1 mouse model assessed as reduction in time spent in licking or biting formalin injected hind paw during neurogenic phase at 0.1 nmol, sc pretreated for 15 mins followed by formalin induction me | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
AID452784 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
AID1798027 | Radioligand Labeled Binding Assay from Article 10.1021/jm070332f: \\A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Recep | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID1798028 | Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay from Article 10.1021/jm061369n: \\Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 re | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
AID1798026 | Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay from Article 10.1021/jm070332f: \\A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Recept | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
AID1798029 | Radioligand Labeled Binding Assay from Article 10.1021/jm061369n: \\Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.\\ | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 1 (1.27) | 18.7374 |
1990's | 15 (18.99) | 18.2507 |
2000's | 23 (29.11) | 29.6817 |
2010's | 32 (40.51) | 24.3611 |
2020's | 8 (10.13) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (20.65) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 5 (5.95%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 79 (94.05%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |