endomorphin 2: isolated from bovine brain [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5311081 |
| CHEMBL ID | 333357 |
| MeSH ID | M0274738 |
| Synonym |
|---|
| endomorphin-2 , |
| endomorphin 2 |
| NCGC00163677-01 |
| NCGC00163677-02 |
| l-tyrosyl-l-prolyl-l-phenylalanyl-l-phenylalaninamide |
| tetrapeptide-15 |
| l-tyrosyl-l-prolyl-l-phenylalanyl-l-phenylalaninamide, (-)- |
| tyrosyl-prolyl-phenylalanyl-phenylalaninamide |
| tyr-pro-phe-phe-nh2 |
| l-phenylalaninamide, l-tyrosyl-l-prolyl-l-phenylalanyl- |
| bdbm50139013 |
| (s)-1-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid [(s)-1-((s)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-phenyl-ethyl]-amide |
| 1-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylicacid[1-((s)-(s)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-phenyl-ethyl]-amide |
| (s)-n-((s)-1-((s)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-1-oxo-3-phenylpropan-2-yl)-1-((s)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide |
| h-tyr-pro-phe-phe-nh2 |
| CHEMBL333357 , |
| (2s)-1-[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]-n-[(2s)-1-[[(2s)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamide |
| 141801-26-5 |
| gtpl3668 |
| tetrapeptide-15 [inci] |
| 3PH5M0466G , |
| l-phenylalaninamide,l-tyrosyl-l-prolyl-l-phenylalanyl- |
| DTXSID70415506 |
| AKOS024456356 |
| unii-3ph5m0466g |
| (2s)-2-{[(2s)-1-[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidin-2-yl]formamido}-n-[(1s)-1-carbamoyl-2-phenylethyl]-3-phenylpropanamide |
| HY-P0186 |
| c32h37n5o5 |
| HB2411 |
| Q19597070 |
| (s)-1-(l-tyrosyl)-n-((s)-1-(((s)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)pyrrolidine-2-carboxamide |
Endomorphin 2 is a newly discovered peptide that has high affinity and specificity for the mu-opioid receptor.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Endomorphin 2 is a newly discovered peptide that has high affinity and specificity for the mu-opioid receptor. " | ( Morphological evidence of endomorphin as an agonist for the mu-opioid receptor in the rat spinal cord. Guan, JL; Shioda, S; Wang, QP; Zadina, JE, 2003) | 1.76 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Endomorphin 2 (EM2) plays essential roles in regulating nociceptive transmission within the spinal dorsal horn, where EM2-immunopositive (EM2-IP) fibers and terminals are densely encountered. " | ( Origins of endomorphin-2 immunopositive fibers and terminals in the spinal dorsal horn of the rat. Chen, T; Hui, R; Li, H; Li, YQ; Lü, BC; Wang, W; Wu, SX; Zhang, T, 2010) | 1.8 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The cyclization of linear analogs based on endomorphin-2 structure, Tyr/Dmt-d-Lys-Phe-Phe-Asp-NH2 and Tyr/Dmt-d-Cys-Phe-Phe-Cys-NH2 (where Dmt=2',6'-dimethyltyrosine), resulting in obtaining lactam or disulfide derivatives, was studied using liquid chromatography combined with on-line mass spectrometry (LC-MS) and tandem mass spectrometry (LC-MS/MS)." | ( Cyclic pentapeptide analogs based on endomorphin-2 structure: cyclization studies using liquid chromatography combined with on-line mass spectrometry and tandem mass spectrometry. Janecka, A; Kluczyk, A; Perlikowska, R; Piekielna, J, 2014) | 0.4 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Our results demonstrate that cyclization might be a promising strategy to enhance bioavailability of peptides and may serve a role in the development of novel endomorphin analogs with increased therapeutic potential." | ( Synthesis and biological evaluation of cyclic endomorphin-2 analogs. Cravezic, A; do-Rego, JC; Fichna, J; Janecka, A; Perlikowska, R; Toth, G; Wyrebska, A, 2010) | 0.36 |
| " Furthermore, the described methodology may be useful for increasing the bioavailability and delivery of opioid peptides to the CNS." | ( Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration. Chen, C; Fichna, J; Grzywacz, D; Janecka, A; Kamysz, W; Mazur, M; Olczak, J; Perlikowska, R; Piekielna, J; Sałaga, M; Sobczak, M; Toth, G, 2013) | 0.39 |
| " Although, additional structural modifications are needed to achieve compounds exhibiting high/fair bioavailability after oral administration, the examples presented herein demonstrate that the bioactive peptides SP(1-7) and endomorphin-2 can be converted into low molecular weight compounds that are able to mimic the in vivo actions of the heptapeptide SP(1-7)." | ( From the Anti-Nociceptive Substance P Metabolite Substance P (1-7) to Small Peptidomimetics. Hallberg, M; Sandstrom, A, 2018) | 0.48 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " 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 |
| " The dose-response curves revealed the development of acute tolerance (tachyphylaxis) to endomorphin." | ( Antinociceptive effects of intrathecal endomorphin-1 and -2 in rats. Benedek, G; Horvath, G; Szikszay, M; Tömböly, C, 1999) | 0.3 |
| ") that was inactive against DAMGO, did not affect endomorphin-1-induced antinociception but shifted the dose-response curve of endomorphin-2 3-fold to the right." | ( Differential antagonism of endomorphin-1 and endomorphin-2 spinal antinociception by naloxonazine and 3-methoxynaltrexone. Fujimura, T; Hayashi, T; Kastin, AJ; Murayama, K; Sakurada, C; Sakurada, S; Sakurada, T; Takeshita, M; Yonezawa, A; Yuhki, M; Zadina, JE, 2000) | 0.31 |
| "25-1 microg) significantly increased both the locomotor and the rearing activity, resulting in a bell-shaped dose-response curve." | ( Behavioral and neuroendocrine actions of endomorphin-2. Bujdosó, E; Jászberényi, M; Telegdy, G; Tömböly, C; Tóth, G, 2001) | 0.31 |
| " A 2-h pretreatment with endomorphin-1 (30 nmol) produced a 3-fold shift to the right in the dose-response curve for endomorphin-1." | ( Acute antinociceptive tolerance and asymmetric cross-tolerance between endomorphin-1 and endomorphin-2 given intracerebroventricularly in the mouse. Fujimoto, JM; Hung, KC; Mizoguchi, H; Tseng, LF; Wu, HE, 2001) | 0.31 |
| " and co-administration of 3-methylnaltrexone shifted the dose-response curves for endomorphin-2 induced antinociception to the right by 4-fold." | ( Differential antagonism of endomorphin-1 and endomorphin-2 supraspinal antinociception by naloxonazine and 3-methylnaltrexone. Fujimura, T; Hayashi, T; Kastin, AJ; Murayama, K; Sakurada, C; Sakurada, S; Sakurada, T; Sato, T; Takeshita, M; Yonezawa, A; Yuhki, M; Zadina, JE, 2002) | 0.31 |
| "924 nM)] and with a correlation between delta-opioid receptor affinities and functional bioactivity using MVD; (iii) intracerebroventricular administration of [Dmt(1)]- (14) and [Det(1)]EM-2 (10) produced a dose-response antinociception in mice, with the former analogue more active than the latter; and (iv) a marked shift occurred from the trans-orientation at the Tyr(1)-Pro(2) bond to a cis-conformer compared to that observed previously with [Dmt(1)]EM-2 (14) (Okada et al." | ( Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. Ambo, A; Bryant, SD; Fujita, Y; Jinsmaa, Y; Lazarus, LH; Li, T; Miyazaki, A; Okada, Y; Sasaki, Y; Tsuda, Y, 2005) | 0.33 |
| " Endomorphin-1, endomorphin-2 and deltorphin I at the dosage of 1, 10, 100 nmol/embryo could stimulate angiogenesis dose-dependently, respectively." | ( Endogenous opioid peptides, endomorphin-1 and -2 and deltorphin I, stimulate angiogenesis in the CAM assay. Cui, SG; Dai, X; Liu, Q; Song, HJ; Wang, R; Wang, T, 2008) | 0.35 |
| " In several situations, including clinical depression, MIF-1 exhibits an inverted U-shaped dose-response relationship in which increasing doses can result in decreasing effects." | ( From MIF-1 to endomorphin: the Tyr-MIF-1 family of peptides. Kastin, AJ; Pan, W, 2007) | 0.34 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.0844 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| [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) | IC50 (µMol) | 255.0241 | 0.0001 | 0.7298 | 10.0000 | AID242323; AID426389 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 8.0385 | 0.0000 | 0.6068 | 9.2330 | AID1196465; AID149671; AID149817; AID1667818; AID1807959; AID1872038; AID238805; AID268520; AID339692; AID705242; AID770994 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0010 | 0.0001 | 0.8874 | 10.0000 | AID635905 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0046 | 0.0000 | 0.3845 | 8.6000 | AID1196464; AID151610; AID151770; AID151771; AID1667817; AID1807958; AID1872037; AID238756; AID239609; AID268517; AID312059; AID339690; AID339691; AID705243; AID770995 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 6.6702 | 0.0000 | 0.1868 | 3.9500 | AID148592; AID1667819; AID1807960 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0059 | 0.0000 | 0.4197 | 10.0000 | AID1129801; AID148592; AID1600055; AID266691; AID449582; AID698507; AID760561 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 3.4030 | 0.0000 | 0.5978 | 9.9300 | AID1129825; AID148592; AID1600056; AID698508; AID760560 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 1.0000 | 0.0003 | 0.7123 | 7.0700 | AID1173781 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 2.7080 | 0.0000 | 0.2018 | 6.4240 | AID1196466 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 1.1513 | 0.0000 | 0.3624 | 10.0000 | AID148592; AID1600057; AID1872033; AID703060 |
| Mu-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 0.0241 | 0.0008 | 1.6992 | 10.0000 | AID151138 |
| [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) |
|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.5390 | 0.0000 | 0.0647 | 0.9320 | AID277680; AID339695 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0202 | 0.0000 | 0.3263 | 9.4000 | AID1229433; AID1275489; AID1536311; AID1600059; AID1667820; AID1807965; AID1872039; AID1872048; AID277678; AID314189; AID698512 |
| Delta-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 1.0000 | 0.0000 | 0.4332 | 8.3000 | AID277680; AID314190 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | EC50 (µMol) | 1.0000 | 0.0000 | 0.0493 | 0.9320 | AID277680 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1807963 | Inhibition of electric-field induced guinea pig ileum contraction | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1808010 | Chronic antinociceptive tolerance in Kunming mouse pretreated with compound followed by repeated compound addition at 20 nmol, icv once daily for 7 days and measured after 5 mins by radiant heat paw withdrawal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID312061 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding relative to basal level | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID398173 | Displacement of [3H]DAMGO from mu 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. |
| AID1807962 | Selectivity index, ratio of Ki for displacement of [3H]-U69593 from KOR in Wistar rat brain membranes to Ki for displacement of [3H]DAMGO from MOR in Wistar rat brain membranes | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1184644 | Stability in rat brain homogenate assessed as degradation rate constant measured up to 60 mins by RP-HPLC analysis | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID268518 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain relative to morphiceptin | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID770995 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation. |
| AID314194 | Antinociceptive activity in mouse assessed as paw licking latency at 3 ug, icv by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
| AID587665 | Half life in rat brain homogenate by RP-HPLC | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
| AID277678 | Activity at mu 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). |
| AID1536311 | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins | |||
| AID242238 | In vitro inhibitory concentration against Opioid receptor mu 1 was measured using guinea pig ileum assay | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID314192 | Antinociceptive activity in mouse assessed as rearing latency at 10 ug, icv by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
| AID760561 | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) expressed in CHO cells after 90 mins by liquid scintillation counting | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Structural and biological exploration of phe(3)-phe(4)-modified endomorphin-2 peptidomimetics. |
| AID76400 | in vitro inhibition of electrically evoked contractions of GPI (Guinea pig ileum) | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID1872040 | Antinociceptive activity in Swiss albino mouse assessed tail flick response in warm water administered icv | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID268517 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID1808013 | Toxicity in icv dosed Kunming mouse assessed as inhibition of gastrointestinal transit by measuring charcoal distance travel by charcoal meal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID484198 | Displacement of [3H]nalocone from mu opioid receptor in rat brain membranes | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues. |
| AID151771 | Displacement of [3H]endomorphin-2 from Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID1058675 | Agonist activity at mu opioid receptor in guinea pig ileum | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration. |
| AID1536341 | Toxicity in Kunming mouse assessed as inhibition of gastrointestinal transit by measuring reduction in distance traveled by charcoal at 10 to 30 mg/kg, ip dosed 15 mins prior charcoal meal measured after 30 mins | |||
| AID1229437 | Agonist activity at human recombinant delta opioid receptor expressed in CHO cells co-expressing Galphaq66Di5 assessed as stimulation of calcium release up to 1 uM by Fluo-4 AM dye-based fluorescence assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
| AID277690 | Antinociceptive activity in Swiss Albino mouse assessed as effect on rearing by hot plate method at 10 ug | 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). |
| AID239609 | Inhibition of DAMGO (Tyr-[D-Ala]-Gly-[NMe-Phe]-Gly-ol) binding to rat brain mu opioid receptor | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models. |
| AID587667 | Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay relative to baseline | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
| AID1667825 | Antinociceptive activity in kunming mouse models assessed as maximum possible effect at 0.4 nmol, icv measured from 5 to 60 mins by warm water tail-flick assay relative to control | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID1275473 | Displacement of [3H]DAMGO from MOR in Wistar rat brain homogenates by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID1173781 | Displacement of [3H]nor-BNI from KOR in Dunkin Hartley guinea pig membranes by liquid scintillation counting method | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 | Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine. |
| AID1667817 | Displacement of [3H]-DAMGO from Wistar rat mu opioid receptor incubated for 1 hr by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID398177 | Binding affinity to recombinant OPRM1 receptor immobilized on biosensor assessed as dissociation rate constant by BIAcore X system | 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. |
| AID635912 | Antinociceptive activity in icv dosed in Swiss albino mouse assessed as jumping latency by hot plate method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| 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. |
| AID426389 | Agonist activity at delta opioid receptor in mouse vas deference assessed as inhibition of electrically-stimulated contraction | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. |
| AID314193 | Antinociceptive activity in mouse assessed as jumping latency at 10 ug, icv by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
| AID1807973 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID698514 | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter relative to control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID703057 | Displacement of [3H]DPDPE from delta opioid receptor in calf frontal cortex after 1 hr by gamma counter | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2. |
| AID1196472 | Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology at 3.3 uM measured over 30 mins by label free binding assay relative to DPDPE | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID149794 | Binding affinity towards delta receptor in rat brain using [3H]DSLET | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID1808016 | Toxicity in Kunming mouse model assessed as conditioned place preference time at 10 micromol/kg, sc | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID151610 | Binding affinity against rat brain Opioid receptor mu 1 using [3H]DAMGO radioligand | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties. |
| AID295478 | Selectivity for rat mu opioid receptor over rat delta opioid | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2. |
| AID698513 | Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction in presence of delta opioid receptor antagonist naltrindole | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID140434 | in vitro inhibition of electrically evoked contractions of MVD (Mouse vas deferens) relative to [Leu5]-enkephalin | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID408815 | Selectivity ratio of Ki for delta opioid receptor to Ki for mu opioid receptor in rat brain membrane | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. |
| AID408818 | Selectivity ratio of IC50 for guinea pig ileum to IC50 for mouse vas deferens assay | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. |
| AID1184626 | Displacement of [3H]nor-BNI from KOR in guinea pig brain membranes | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID1536319 | Effect on neurite outgrowth in mouse Neuro2a cells at 10 uM after 18 hrs by phase contrast microscopic analysis relative to control | |||
| AID1229432 | Metabolic stability in rat brain homogenates assessed as enzymatic degradation by measuring compound remaining at 0.5 mM after 90 mins by RP-HPLC analysis | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
| AID148592 | Displacement of [3H]dynorphin A from Opioid receptor kappa 1 of rat brain membranes (DAMGO/DADLE quenching of mu/delta receptor binding) | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID1808004 | Tolerance ratio of ED50 for Kunming mouse pretreated with 3 times ED50 of compound for 2 hrs followed by challenge with second dose of compound to ED50 for Kunming mouse pretreated with saline for 2 hrs followed by compound addition | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1807958 | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID705240 | Agonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assay | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2. |
| 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). |
| AID1872033 | Binding affinity to KOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID277689 | Antinociceptive activity in Swiss Albino mouse assessed as effect on paw licking by hot plate method at 10 ug | 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). |
| AID462888 | Displacement of [3H]SP1-7 from NK1 receptor in Sprague-Dawley rat spinal cord membrane | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Discovery of dipeptides with high affinity to the specific binding site for substance P1-7. |
| AID1667824 | Antinociceptive activity in kunming mouse models assessed as inhibition of tail-flick response by tail-flick assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID244144 | Selectivity for Opioid receptor mu 1 to that of Opioid receptor delta 1 | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID242323 | In vitro inhibitory concentration against Opioid receptor delta 1 was measured using mouse vas deferens assay | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID1129801 | Binding affinity to mu opioid receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity. |
| AID1808015 | Toxicity in Kunming mouse model assessed as conditioned place preference time at 20 nmol, icv | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1807961 | Selectivity index, ratio of Ki for displacement of [3H]DPDPE from DOR in Wistar rat brain membranes to Ki for displacement of [3H]DAMGO from MOR in Wistar rat brain membranes | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1807964 | Inhibition of electric-field induced mouse vas deferens contraction | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1629765 | Activation of mu opioid receptor-1 (unknown origin) expressed in CHO cells assessed as beta-arrestin-2 recruitment at 10 uM after 90 mins by beta-galactosidase complementation assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID515107 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane after 3 hrs by liquid scintillation counting | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. |
| AID277684 | Agonist activity at delta opioid receptor by inhibition of electrically evoked muscle contraction in isolated mouse vas deferens | 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). |
| AID760558 | Selectivity ratio of Ki for delta opioid receptor (unknown origin) expressed in CHO cells to Ki for mu opioid receptor (unknown origin) expressed in CHO cells | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Structural and biological exploration of phe(3)-phe(4)-modified endomorphin-2 peptidomimetics. |
| AID1536313 | Agonist activity at kappa-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins | |||
| AID277682 | Agonist activity at mu opioid receptor by inhibition of electrically evoked muscle contraction in guinea pig ileum | 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). |
| AID770991 | Antinociceptive effect in icv dosed CD1 mouse assessed as increase in tail-flick latency period by tail flick test | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation. |
| AID1667820 | Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID266695 | Agonist activity at mu opioid receptor by guinea pig ileum assay | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands. |
| AID306545 | Apparent permeability from apical to basolateral side of human Caco-2 cell membrane | 2007 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7 | Comparison of the in vitro apparent permeability and stability of opioid mimetic compounds with that of the native peptide. |
| AID698511 | Selectivity ratio of IC50 for mu opioid receptor in guinea pig ileum to IC50 for delta opioid receptor in Kunming mouse vas deferens | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID587666 | Agonist activity at opioid receptor in mu rat brain membrane by [35S]GTPgammaS binding assay relative to baseline in presence of opioid-selective antagonist naloxone | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
| AID1196475 | Half life in rat brain homogenate at 10 uM | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID515111 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. |
| AID244330 | Relative potency of EM-2 measured towards Opioid receptor mu 1 assayed with [3H]DAMGO | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| 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. |
| AID426387 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. |
| AID1058673 | Antinociceptive activity in mouse assessed as prolongation time to jump at 3 mg/kg, iv by hot plate test | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration. |
| AID150065 | Binding affinity towards delta receptor in rat brain using [3H]DSLET relative to [Leu5]-enkephalin | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID1229433 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells co-expressing C-terminally modified GGalphaqi5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
| AID1600056 | Displacement of [3H]deltrophin-2 from human recombinant DOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting method | |||
| AID1196467 | Selectivity ratio of Ki for rat cortex delta opioid receptor to Ki for rat cortex mu opioid receptor | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID339693 | Selectivity ratio of Ki for displacement of [3H]DAMGO from mu opioid receptor over Ki for displacement of [3H]Ile5,6deltorphin from delta opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
| AID1229430 | Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membranes after 120 mins by scintillation counting analysis | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
| AID396781 | Antinociceptive activity in Swiss albino CD1 mouse assessed as duration of inhibition of paw licking at 3 ng, icv by hot plate test | 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. |
| AID238805 | Inhibition of [3H]DPDPE binding to delta-Opioid receptor | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. |
| AID195849 | In vitro percent maximal stimulation of [35S]GTP-gamma-S, binding by the compound in rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID698512 | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID288658 | Selectivity for mu opioid receptor over delta opiod receptor in Sprague-Dawley rat brain P2 synaptosome membrane | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. |
| AID705243 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2. |
| AID1872039 | Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID132679 | In vitro inhibitory concentration against electrically induced twitches in mouse vas deferens | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties. |
| AID1536320 | Antagonist activity at mu-opioid receptor in mouse Neuro2a cells assessed as inhibition of NPFF-induced neurite outgrowth by measuring neurite outgrowth at 10 uM after 18 hrs by phase contrast microscopic analysis (Rvb = 24.05 +/- 1.19%) | |||
| AID293121 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked muscle contractions | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 | Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
| AID268520 | Displacement of [3H]DPDPE from delta opioid receptor in Wistar rat brain | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID1872054 | Stability in rat brain homogenate assessed as compound remaining measured after 90 mins relative to control | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1275485 | Agonist activity at human recombinant KOR expressed in CHO cells assessed as calcium mobilization up to 1 uM by Fluo-4 AM based fluorescence analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID314195 | Antinociceptive activity in mouse assessed as rearing latency at 3 ug, icv by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
| AID698510 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID1275488 | Retention time of compound by RP-HPLC analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID314191 | Antinociceptive activity in mouse assessed as paw licking latency at 10 ug, icv by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
| AID635916 | Antinociceptive activity in icv dosed Swiss albino mouse assessed as jumping latency at 3 ug, icv up to 90 mins by hot plate method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| AID288656 | Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosome membrane | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. |
| AID1196471 | Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as change in cell morphology at 3.3 uM measured over 30 mins by label free binding assay relative to DAMGO | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID314184 | Displacement of [3H]DAMGO from mu 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. |
| AID1229440 | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as stimulation of calcium release up to 1 uM by Fluo-4 AM dye-based fluorescence assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
| AID1872048 | Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulation | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID288659 | Displacement of [3H]U-69593 from kappa opioid receptor in Hartley guinea pig cerebellum P2 synaptosome membrane | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. |
| AID1536343 | Antinociceptive activity in icv dosed Kunming mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal up to 60 mins radiant heat tail flick method | |||
| AID268521 | Selectivity for mu opioid receptor over delta opioid receptor | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID239108 | Mean value of binding constant for Opioid receptors assayed with [3H]DAMGO | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID295476 | Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2. |
| AID1807960 | Displacement of [3H]-U69593 from KOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1807965 | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID152383 | Binding affinity towards mu receptor in rat brain using [3H]DAMGO | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID288657 | Displacement of [3H]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosome membrane | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. |
| AID770992 | Analgesic activity in icv dosed CD1 mouse assessed as inhibition of heat-induced jumping behaviour after 5 to 30 mins by hot plate method | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation. |
| AID1129825 | Binding affinity to delta opioid receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity. |
| AID1807972 | Antinociceptive activity in icv dosed Kunming mouse model assessed as increase in paw withdrawal latency by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID268525 | Half life in mouse brain at 10 ul | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID1229429 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes after 120 mins by scintillation counting analysis | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
| AID1173780 | Displacement of [3H][Ile5,6]deltorphin-2 from DOR in Wistar rat brain membranes by liquid scintillation counting method | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 | Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine. |
| AID339691 | Displacement of [3H]endomorphin-2 from mu opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
| AID312065 | Agonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID244333 | In vitro potency of EM-2 measured towards Opioid receptor delta 1 using mouse vas deferens assay | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID396786 | Antinociceptive activity in Swiss albino CD1 mouse assessed as duration of inhibition of rearing at 3 ng, icv by hot plate test | 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. |
| AID241858 | In vitro inhibition of opioid receptor mu using isolated guinea pig ileum | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. |
| AID770994 | Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain membranes by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation. |
| AID587664 | Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
| AID80151 | in vitro inhibition of electrically evoked contractions of GPI (Guinea pig ileum) relative to [Leu5]-enkephalin | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID515106 | Displacement of [3H]U69593 from delta opioid receptor in guinea pig brain membrane after 3 hrs by liquid scintillation counting | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. |
| AID398178 | Stability in rat brain homogenates assessed as degradation half life | 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. |
| AID1807978 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 10 mins with naloxone followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID705241 | Selectivity ratio of Ki for Wistar rat delta opioid receptor to Ki for Wistar rat mu opioid receptor | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2. |
| AID312058 | Stability in rat brain assessed as half life | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID1196466 | Displacement of [3H]U69,593 from guinea pig cortex/cerebella kappa opioid receptor after 2 hrs by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID515110 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. |
| AID1275486 | Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization up to 1 uM by Fluo-4 AM based fluorescence analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID314189 | Antagonist activity at mu 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. |
| AID288660 | Selectivity for Sprague-Dawley rat brain mu opioid receptor over Hartley guinea pig cerebellum kappa opioid receptor | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. |
| AID408814 | Displacement of [3H]DPDPE from delta opioid receptor in rat brain membrane | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. |
| AID312064 | Agonist activity at mu opioid receptor in rat brain assessed as maximal stimulation of [35S]GTP-gamma-S binding | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID270136 | Agonist activity at mu opioid receptor assessed as inhibition of electrically-evoked contraction of guinea pig ileum | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore. |
| AID1807976 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv measured after 20 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID339690 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
| AID149817 | Displacement of [3H]Ile5,6-deltorphin II from opioid receptor delta 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID705242 | Displacement of [3H][Ile5,6]deltorphin 2 from delta opioid receptor in Wistar rat brain membranes | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2. |
| AID312060 | Displacement of [3H]deltorphin 2 from delta opioid receptor in Wistar rat brain after 45 mins | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID241750 | In vitro inhibition of opioid receptor delta using mouse vas deferens | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. |
| AID426390 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. |
| AID1807959 | Displacement of [3H]DPDPE from DOR in Wistar rat brain membranes measured after 3 hrs by scintillation counting method | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID760560 | Displacement of [3H]DPDPE from delta opioid receptor (unknown origin) expressed in CHO cells after 90 mins by liquid scintillation counting | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Structural and biological exploration of phe(3)-phe(4)-modified endomorphin-2 peptidomimetics. |
| AID1667828 | Antinociceptive activity in kunming mouse models assessed as effective dose after icv administration measured from 5 to 60 mins by warm water tail-flick assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| 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. |
| AID398176 | Binding affinity to recombinant OPRM1 receptor immobilized on biosensor assessed as association rate constant by BIAcore X system | 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. |
| AID1807980 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 20 mins with naloxonazine followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1667819 | Displacement of[3H]-U69,593 from Wistar rat kappa opioid receptor incubated for 1.5 hrs by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID1184625 | Displacement of [3H](Ile5,6)deltorphin-2 from DOR in rat brain membranes | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID515109 | Selectivity ratio of Ki for delta opioid receptor in guinea pig brain membrane to Ki for mu opioid receptor in rat brain membrane | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. |
| AID1196468 | Selectivity ratio of Ki for guinea pig cortex/cerebella kappa opioid receptor to Ki for rat cortex mu opioid receptor | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID1808002 | Antinociceptive tolerance in Kunming mouse pretreated with saline for 2 hrs followed by compound addition by radiant heat paw withdrawal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID293123 | Ratio of pA2 for delta opioid receptor in MVD to pA2 for mu opioid receptor in GPI | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 | Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
| AID1196465 | Displacement of [3H]DPDPE from rat cortex delta opioid receptor after 2.5 hrs by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID195718 | In vitro effective dose against [35S]GTP-gamma-S, binding to rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID408816 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. |
| AID698508 | Displacement of [3H]DPDPE from Myc-tagged delta opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID587662 | Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane homogenate by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
| AID268522 | Antinociceptive activity in mouse at 4 ul, icv by hot plate test assessed as area under %MPE - time curve after 15 mins | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID1275475 | Displacement of [3H]nor-BNI from KOR in Dunkin Hartley guinea pig brain homogenates by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID295477 | Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2. |
| AID705239 | Agonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assay relative to control | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2. |
| AID587663 | Selectivity ratio of Ki for delta opioid receptor in rat brain to mu opioid receptor in rat brain | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
| AID484194 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contraction | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues. |
| AID339695 | Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
| AID587661 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane homogenate by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
| AID1667822 | Half life in Kunming mouse brain homogenate at 10'-2 mol/L by RP-HPLC analysis | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID12705 | Half-life in rat brain homogenate | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID635911 | Antinociceptive activity in icv dosed in Swiss albino mouse assessed as rearing latency by hot plate method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| AID1229431 | Displacement of [3H]nor-BNI from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
| AID149744 | Inhibition of Opioid receptor mu 1 of guinea pig ileum | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID339692 | Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
| AID1872051 | Degradation half life in rat brain homogenate | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID398175 | Selectivity ratio of IC50 for delta opioid receptor to IC50 for mu 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. |
| AID1667834 | Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method relative to control | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID277691 | Antinociceptive activity in Swiss Albino mouse assessed as effect on jumping by hot plate method at 10 ug | 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). |
| AID268524 | Antinociceptive activity in mouse at 4ul, icv by hot plate test assessed as area under %MPE - time curve after 45 mins | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID396779 | Antinociceptive activity in Swiss albino CD1 mouse assessed as inhibition of paw licking at 100 ng, icv by hot plate test | 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. |
| AID449582 | Binding affinity to human mu opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor. |
| AID78311 | In vitro inhibitory concentration against electrically induced twitches in guinea pig ileum | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties. |
| AID244332 | In vitro potency of EM-2 was measured towards Opioid receptor mu 1 using guinea pig ileum assay | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID635909 | Half life in Wistar rat brain at 0.5 mM by RP-HPLC analysis | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| AID152390 | Binding affinity towards mu receptor in rat brain using [3H]DAMGO relative to [Leu5]-enkephalin | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID266691 | Binding affinity to mu opioid receptor | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands. |
| AID703060 | Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells after 60 mins by liquid scintillation counter | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2. |
| AID1562920 | Displacement of [3H]JWH-018 from CB1R/CB2R in Wistar rat brain membranes at 10 uM after 60 mins by liquid scintillation analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. |
| AID312059 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain after 45 mins | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID1184628 | Selectivity ratio of IC50 for KOR in guinea pig brain membranes to IC50 for MOR in rat brain membranes | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID314188 | Selectivity for mu opioid receptor over 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. |
| AID243115 | Ratio of IC50s against Opioid receptor delta 1 was measured in mouse vas deferens to that of guinea pig ileum | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID312062 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID1667823 | Half life in Kunming mouse serum at 10'-2 mol/L by RP-HPLC analysis | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID1807974 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv measured after 5 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1184627 | Selectivity ratio of IC50 for DOR in rat brain membranes to IC50 for MOR in rat brain membranes | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID1807970 | Metabolic stability in Kunming mouse serum assessed as half life measured upto 480 mins by RP-HPLC analysis | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1808014 | Toxicity in Kunming mouse assessed as inhibition of gastrointestinal transit at 10 micromol/kg, sc by charcoal meal test (Rvb = 70.3 +/- 3 %) | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID635905 | Displacement of [3H]DAMGO from Wistar rat mu opioid receptor by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| AID760559 | Selectivity ratio of Ki for mu opioid receptor (unknown origin) expressed in CHO cells to Ki for delta opioid receptor (unknown origin) expressed in CHO cells | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Structural and biological exploration of phe(3)-phe(4)-modified endomorphin-2 peptidomimetics. |
| AID268523 | Antinociceptive activity in mouse at 4ul, icv by hot plate test assessed as area under %MPE - time curve after 30 mins | 2006 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4. |
| AID705244 | Half life in Wistar rat brain homogenate | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2. |
| AID312063 | Agonist activity at mu opioid receptor in rat brain assessed as maximal stimulation of [35S]GTP-gamma-S binding relative to basal level | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. |
| AID1275474 | Displacement of [3H][Ile5,6]deltorphin-2 from DOR in Wistar rat brain homogenates by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID698507 | Displacement of [3H]DAMGO from FLAG-tagged mu opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| 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. |
| AID1872055 | Stability in rat brain homogenate assessed as half life | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1807966 | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID242998 | Relative binding to delta and mu Opioid receptors (ratio of Ki) | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. |
| AID635915 | Antinociceptive activity in Swiss albino mouse assessed as jumping latency at 3 ug, icv after 5 to 10 mins by hot plate method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| 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. |
| AID314196 | Antinociceptive activity in mouse assessed as jumping latency at 3 ug, icv by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
| AID635910 | Antinociceptive activity in icv dosed in Swiss albino mouse assessed as paw licking latency by hot plate method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| AID408813 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. |
| AID1600059 | Agonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assay | |||
| AID244331 | Relative potency of EM-2 measured towards Opioid receptor delta 1 assayed with [3H]DPDPE | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID1184624 | Displacement of [3H]DAMGO from MOR in rat brain membranes | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID293119 | Agonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of electrically evoked myenteric plexus longitudinal muscle contractions | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 | Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
| AID149671 | Binding affinity against rat brain opioid receptor delta 1 using [3H]DPDPE radioligand | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties. |
| AID1872049 | Stability in mouse serum assessed as half life | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1667818 | Displacement of [3H]-DPDPE from Wistar rat delta opioid receptor incubated for 3 hrs by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID1498740 | Displacement of [3H]SP1-7 from NK1 receptor in Sprague-Dawley rat spinal cord membranes after 60 mins by scintillation counting method | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | An imidazole based H-Phe-Phe-NH |
| AID238756 | Inhibition of [3H]DAMGO binding to mu-Opioid receptor | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. |
| AID1807983 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 10 micromol/kg, sc by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID132865 | in vitro inhibition of electrically evoked contractions of MVD (Mouse vas deferens) | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
| AID698506 | Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID1807982 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 30 mins with nor-BNI followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID226741 | Relative inhibition of mu opioid receptor of guinea pig ileum and mouse vas deferens | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID635906 | Displacement of [3H][Ile5,6]deltorphin 2 from delta opioid receptor in Wistar rat brain membrane by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| AID239109 | Mean value of binding constant for Opioid receptors assayed with [3H]DPDPE | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. |
| AID1196464 | Displacement of [3H]DAMGO from rat cortex mu opioid receptor after 30 mins by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
| AID231320 | Relative affinity for delta and kappa opioid receptors | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID1807971 | Octanol/buffer distribution coefficient, log D of the compound at pH 7.4 by RP-HPLC analysis | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1536312 | Agonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins | |||
| AID1872037 | Displacement of [3H]DAMGO from Wistar rat brain membrane MOP | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID293118 | Selectivity for rat mu opioid receptor over rat delta opioid receptor | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 | Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
| AID396787 | Antinociceptive activity in Swiss albino CD1 mouse assessed as duration of inhibition of jumping at 3 ng, icv by hot plate test | 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. |
| AID1184629 | Half life in rat brain homogenate by RP-HPLC analysis | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID1600055 | Displacement of [3H]DAMGO from human recombinant MOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting method | |||
| AID339694 | Selectivity ratio of Ki for displacement of [3H]endomorphin-2 from mu opioid receptor over Ki for displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
| AID1275476 | Stability of compound in Wistar rat brain homogenate assessed as compound remaining after 90 mins by RP-HPLC analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID339696 | Half life in rat brain membrane homogenate | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
| AID288661 | 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 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. |
| AID698509 | Selectivity ratio of Ki for Myc-tagged delta opioid receptor to Ki for FLAG-tagged mu opioid receptor | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
| AID1173779 | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes by liquid scintillation counting method | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 | Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine. |
| AID1807969 | Metabolic stability in Kunming mouse brain assessed as half life measured upto 480 mins by RP-HPLC analysis | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID251658 | Inhibition of electrically evoked contraction in mice by tail flick method | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. |
| AID288662 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands. |
| AID151770 | Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID1872038 | Displacement of [3H]-[Ile5,6]-deltorphin-2 from Wistar rat brain membrane DOP | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID635907 | Selectivity ratio of IC50 for delta opioid receptor in Wistar rat brain membrane to IC50 for mu opioid receptor in Wistar rat brain membrane | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
| AID231287 | Ratio of binding affinity against rat brain delta opioid receptor to that of mu opioid receptor | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties. |
| AID408817 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated contraction | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. |
| AID1275477 | Antinociceptive activity in icv dosed BalbC albino mouse assessed as latency of jumping after 10 mins by hot-plate method | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID293117 | Displacement of [3H]deltorphin 2 from delta opioid receptor in rat brain P2 synaptosome | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 | Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
| AID1129802 | Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for mu opioid receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity. |
| AID484193 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues. |
| AID1808003 | Antinociceptive tolerance in Kunming mouse pretreated with 3 times ED50 of compound for 2 hrs followed by challenge with second dose of compound by radiant heat paw withdrawal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1807979 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 4 hrs with beta-FNA followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22 | Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
| AID1275489 | Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
| AID1600057 | Displacement of [3H]U-69593 from human recombinant KOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting method | |||
| AID1600058 | n-Octanol/water partition coefficient, log P of compound at 50 ug at pH 7.4 measured after 2 mins by RP-HPLC analysis | |||
| AID151138 | Inhibition of Mu opioid receptor of mouse vas deferens | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
| AID1667836 | Antinociceptive activity in kunming mouse models assessed as maximum possible effect at 4 nmol, icv measured from 5 to 60 mins by warm water tail-flick assay relative to control | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
| AID293116 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain P2 synaptosome | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 | Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
| AID1346400 | Rat mu receptor (Opioid receptors) | 1997 | Nature, Apr-03, Volume: 386, Issue:6624 | A potent and selective endogenous agonist for the mu-opiate receptor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 58 (13.27) | 18.2507 |
| 2000's | 251 (57.44) | 29.6817 |
| 2010's | 115 (26.32) | 24.3611 |
| 2020's | 13 (2.97) | 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 (18.40) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 26 (5.87%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 417 (94.13%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||