Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5462471 |
| CHEMBL ID | 38874 |
| CHEBI ID | 272 |
| SCHEMBL ID | 725750 |
| MeSH ID | M0111607 |
| PubMed CID | 5485228 |
| MeSH ID | M0111607 |
| Synonym |
|---|
| gtpl1647 |
| enkephalin, ala(2)-mephe(4)-gly-ol(5)- |
| glyol |
| 2-ala-4-mephe-5-gly-enkephalin |
| chembl38874 , |
| [3h]damgo |
| (2s)-2-{2-[(2r)-2-[(2s)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]-n-methylacetamido}-n-(2-hydroxyethyl)-3-phenylpropanamide |
| bdbm21015 |
| [tyrosyl-3,5-3h(n)]-d-ala2-mephe4-glyol5-enkephalin |
| rx 783006 |
| tyr-d-ala-gly-mephe-gly-ol |
| 78123-71-4 |
| damgo |
| (d-ala(2)-mephe(4)-gly-ol(5))enkephalin |
| dagol |
| tyr-ala-gly-(nme)phe-gly-ol |
| damge |
| ala(2)-mephe(4)-gly-ol(5) enkephalin |
| l-phenylalaninamide, l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-nalpha-methyl- |
| dago |
| NCGC00167303-01 |
| chebi:272 , |
| (2s)-2-amino-n-[(2r)-1-[[2-[[(2s)-1-(2-hydroxyethylamino)-1-oxo-3-phenylpropan-2-yl]-methylamino]-2-oxoethyl]amino]-1-oxopropan-2-yl]-3-(4-hydroxyphenyl)propanamide |
| (2s)-2-[[2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]-methylamino]-n-(2-hydroxyethyl)-3-phenylpropanamide |
| tyr-d-ala-gly-n-methyl-phe-gly-ol |
| SCHEMBL725750 |
| l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-nalpha-methyl-l-phenylalaninamide |
| DTXSID30228775 |
| [d-ala2, nme-phe4, gly-ol5]-enkephalin |
| h-tyr-d-ala-gly-n-me-phe-glycinol |
| c26h35n5o6 |
| HB2409 |
| h-tyr-d-ala-gly-n(me)phe-gly-ol |
| (2s)-2-amino-n-[(1r)-2-[[2-[[(1s)-1-benzyl-2-(2-hydroxyethylamino)-2-oxo-ethyl]-methyl-amino]-2-oxo-ethyl]amino]-1-methyl-2-oxo-ethyl]-3-(4-hydroxyphenyl)propanamide |
| AKOS024456435 |
| HPZJMUBDEAMBFI-WTNAPCKOSA-N |
| HY-P0210 |
| CS-0021316 |
| Q5204254 |
| damgo (tfa) |
| tyr-dala-gly-mephe-gly-ol |
| tyr-d-ala-gly-(nme)phe-gly-ol |
| h-tyr-d-ala-gly-mephe-gly-ol |
| tyr-d-ala2-gly-nmephe-gly-ol |
| tyr-d-ala-gly-nme-phe-gly-ol |
| tyr-d-ala-gly-nmephe-gly-ol |
| tyr-d-ala-gly-n(me)phe-gly-ol |
| tyr-d-ala-gly-n(ch3)phe-gly-ol |
| tyr-d-ala-gly-mephe-gly(ol) |
| tyr-d-ala-gly-n-me-phe-gly-ol |
| (s)-2-amino-n-((r)-1-(2-(((s)-1-(2-hydroxyethylamino)-1-oxo-3-phenylpropan-2-yl)(methyl)amino)-2-oxoethylamino)-1-oxopropan-2-yl)-3-(4-hydroxyphenyl)propanamide |
| rx783006;dagol |
| BD173150 |
| BD174973 |
| AS-83278 |
| benzenepropanimidic?acid, .alpha.-amino-4-hydroxy-n-[(1r,2z)-2-hydroxy-2-[[2-[[(1s,2z)-2-hydroxy-2-[(2-hydroxyethyl)imino]-1-(phenylmethyl)ethyl]methylamino]-2-oxoethyl]imino]-1-methylethyl]-, (.alpha.s)- |
| 3: pn: wo2009046859 page: 98 claimed protein |
| l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-n.alpha.-methyl-l-phenylalaninamide |
| 2YM5VT3MNR |
| 158: pn: us20030176421 page: 54-55 claimed protein |
| d-ala2-mephe4-met(0)5-enkephalin-ol |
| enkephalin, ala(2)-mephe(4)-gly(5)- |
| l-phenylalaninamide, l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-nalpha-methyl-, monoacetate (salt) |
| l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-nalpha-methyl-l-phenylalaninamide monoacetate (salt) |
| enkephalin, alanyl(2)-methylphenylalanyl(4)-glycine(5)- |
| 100929-53-1 |
| l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-n-alpha-methyl-l-phenylalaninamide monoacetate (salt) |
| l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-n-.alpha.-methyl-l-phenylalaninamide monoacetate (salt) |
| damgo (acetate) |
| mfcd00133215 |
| [d-ala2, n-me-phe4, gly5-ol]-enkephalin acetate salt, >=97% (hplc) |
| acetic acid;(2s)-2-amino-n-[(1r)-1-[[[(1s)-1-(2-hydroxyethylcarbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl]methylcarbamoyl]ethyl]-3-(4-hydroxyphenyl)propanamide |
| (s)-2-amino-n-((r)-1-(2-(((s)-1-(2-hydroxyethylamino)-1-oxo-3-phenylpropan-2-yl)(methyl)amino)-2-oxoethylamino)-1-oxopropan-2-yl)-3-(4-hydroxyphenyl)propanamide acetate |
| dago acetate salt |
| l-phenylalaninamide, l-tyrosyl-d-alanylglycyl-n-(2-hydroxyethyl)-nalpha-methyl-, monoacetate (salt) (9ci) |
| acetic acid;(2s)-2-amino-n-[(2r)-1-[[2-[[(2s)-1-(2-hydroxyethylamino)-1-oxo-3-phenylpropan-2-yl]-methylamino]-2-oxoethyl]amino]-1-oxopropan-2-yl]-3-(4-hydroxyphenyl)propanamide |
| acetic acid--2-amino-n-[1-hydroxy-1-({2-[{1-hydroxy-1-[(2-hydroxyethyl)imino]-3-phenylpropan-2-yl}(methyl)amino]-2-oxoethyl}imino)propan-2-yl]-3-(4-hydroxyphenyl)propanimidic acid (1/1) |
| DTXSID70905851 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " These favorable pharmacokinetic properties of DALDA and [Dmt1]DALDA, together with their mu-selectivity, potency, and long duration of action, make them ideal candidates as opioid analgesics." | ( In vivo pharmacokinetics of selective mu-opioid peptide agonists. Desiderio, DM; Fasolo, J; Fridland, G; Lovelace, JL; Schiller, PW; Soong, Y; Szeto, HH; Wu, D, 2001) | 0.31 |
| " Pharmacokinetic studies in rats demonstrated that this formulation produced stable, pharmacologically relevant plasma levels of naltrexone for approximately 1 month following either subcutaneous or intramuscular injections." | ( Vivitrex, an injectable, extended-release formulation of naltrexone, provides pharmacokinetic and pharmacodynamic evidence of efficacy for 1 month in rats. Bartus, RT; Basile, AS; Blaustein, M; Dean, RL; Emerich, DF; Hotz, J; Perdomo, B, 2003) | 0.32 |
| " The fentanyl concentrations derived by both methods were compared by linear regression and pharmacokinetic analysis." | ( Comparison of liquid chromatography-mass spectrometry and radioimmunoassay for measurement of fentanyl and determination of pharmacokinetics in equine plasma. Mama, KR; Stanley, SD; Thomasy, SM, ) | 0.13 |
| " The aim of this paper was to use pharmacokinetic analysis and simulations to identify key factors that determine the effective drug concentration-time profile at the target site in the brain." | ( Pharmacokinetic considerations of nanodelivery to the brain: Using modeling and simulations to predict the outcome of liposomal formulations. Fridén, M; Hammarlund-Udenaes, M; Lindqvist, A, 2016) | 0.43 |
| Excerpt | Relevance | Reference |
|---|---|---|
| "05) without affecting exogenously applied acetylcholine dose-response curves." | ( Role of K+ channels in the modulation of cholinergic neural responses in guinea-pig and human airways. Barnes, PJ; Belvisi, MG; Miura, M; Stretton, CD; Yacoub, MH, 1992) | 0.28 |
| " 1) In the presence of a fixed dose of DPDPE (150 nmol), there was a left shift in the dose-response curve of the mu agonist, with the magnitude of the shifts being greater than those anticipated from a simple additive interaction: PL017 (31-fold) > or = DAMGO (20-fold) > morphine (6." | ( Isobolographic and dose-response analyses of the interaction between intrathecal mu and delta agonists: effects of naltrindole and its benzofuran analog (NTB). Malmberg, AB; Yaksh, TL, 1992) | 0.28 |
| " We now report that LiCl pretreatment shifted the antinociceptive dose-response curve produced by the opioid agonists morphine, [D-Ala2, MePhe4, Gly5-ol]enkephalin (DAMGO) and sufentanil in inverse order of their intrinsic efficacy." | ( Opioid efficacy is linked to the LiCl-sensitive, inositol-1,4,5-trisphosphate-restorable pathway. Connelly, CD; Martinez, RP; Raffa, RB, 1992) | 0.28 |
| " agonist dose-response curves by theophylline (i." | ( Involvement of adenosine in antinociception produced by spinal or supraspinal receptor-selective opioid agonists: dissociation from gastrointestinal effects in mice. DeLander, GE; Mosberg, HI; Porreca, F, 1992) | 0.28 |
| " The opioid antagonist naloxone and the alpha-2 adrenergic antagonist idazoxan were given as intrathecal pretreatments at doses chosen to shift the dose-response curves of their corresponding agonist (given alone) 4- to 10-fold to the right; this always resulted in a smaller, but significant (2- to 4-fold) shift in the dose-response curve of the other agonist given alone." | ( Spinal interactions between opioid and noradrenergic agonists in mice: multiplicativity involves delta and alpha-2 receptors. Hylden, JK; Kitto, K; Lei, S; Roerig, SC; Wilcox, GL, 1992) | 0.28 |
| " The mid-points of the dose-response curves for (1)-naloxone and (d)-naloxone were 10 micrograms/kg and 100 micrograms/kg, respectively." | ( Significance of an opiate mechanism in the adjustment of cerebrocortical oxygen consumption and blood flow during hypercapnic stress. Dora, E; Hines, K; Kunos, G; McLaughlin, AC, 1992) | 0.28 |
| " catheters, dose-response curves were carried out using the hot plate (HP) test for a number of receptor-preferring opioids." | ( Characteristics of dose-dependent antagonism by beta-funaltrexamine of the antinociceptive effects of intrathecal mu agonists. Mjanger, E; Yaksh, TL, 1991) | 0.28 |
| "8-fold rightward shift in the dose-response curve." | ( Lack of antinociceptive cross-tolerance between [D-Pen2, D-Pen5]enkephalin and [D-Ala2]deltorphin II in mice: evidence for delta receptor subtypes. Mattia, A; Mosberg, HI; Porreca, F; Vanderah, T, 1991) | 0.28 |
| " Regression analyses failed to reflect significant shifts in the dose-response functions for either agonist on either measure." | ( Gender effects and central opioid analgesia. Bodnar, RJ; Kepler, KL; Kest, B; Pasternak, GW; Paul, D; Standifer, KM, 1991) | 0.28 |
| " Upon pretreatment with morphine over greater than or equal to 12 h, a fourfold shift of the PGE1-morphine dose-response curve was observed, whether or not IBMX was added." | ( Regulation of cyclic AMP by the mu-opioid receptor in human neuroblastoma SH-SY5Y cells. Duan, DS; Eiger, S; Lameh, J; Sadée, W; Yu, VC, 1990) | 0.28 |
| " In dose-response studies, beta-FNA antagonized all the actions with similar potencies (ID50 values of 12." | ( Comparison of naloxonazine and beta-funaltrexamine antagonism of mu 1 and mu 2 opioid actions. Pasternak, GW; Paul, D; Pick, CG, 1991) | 0.28 |
| "The effect of intravenous infusion of agonists of mu-(DAGO) and delta-(DADL, DAAE) opiate receptors on mean arterial pressure and heart rate was studied in experiments on rats with dosed blood loss of up to 30% of calculated blood volume." | ( [The effect of opiate receptor agonists on the blood circulation in rats with hemorrhagic shock]. Grossler, Iu; Sheĭkh, DV; Slepushkin, VD, ) | 0.13 |
| " On day 6, the magnitude of tolerance was assessed by establishing IT dose-response lines for the effect of the chronic drug given as bolus injections (probe)." | ( Tolerance to delta- but not mu-opioid receptors in the spinal cord attenuates inhibition of the tail-flick response induced by beta-endorphin administered intracerebroventricularly in mice. Suh, HH; Tseng, LF, 1990) | 0.28 |
| " Proglumide both shifted the dose-response curve for morphine analgesia to the left and prolonged morphine's duration of action." | ( Proglumide selectively potentiates supraspinal mu 1 opioid analgesia in mice. Bodnar, RJ; Pasternak, GW; Paul, D, 1990) | 0.28 |
| " The FHR response to DADLE was similar to DAGO in both dose-response and time-action characteristics." | ( Central opioid modulation of fetal cardiovascular function: role of mu- and delta-receptors. Cai, LQ; Szeto, HH; Zhu, YS, 1990) | 0.28 |
| ") injected 1 min before each agonist produced a significant parallel shift to the right of the dose-response curves for morphine and DAMGO, but only partly antagonized the effects of DADLE and DSLET." | ( Role of peripheral mu, delta and kappa opioid receptors in opioid-induced inhibition of gastrointestinal transit in rats. La Regina, A; Petrillo, P; Sbacchi, M; Tavani, A, 1990) | 0.28 |
| " Dose-response curves at 1 hr revealed similar potencies of oxymorphone and the derivatives, with the exception of OxyPNPH which was significantly less potent." | ( Irreversible opiate agonists and antagonists. IV. Analgesic actions of 14-hydroxydihydromorphinone hydrazones. Bodnar, RJ; Burks, TF; Clark, JE; Hahn, EF; Pasternak, GW; Williams, CL, 1988) | 0.27 |
| " dose-response curves for the effect of the chronic drug given as a bolus." | ( Potency of infused spinal antinociceptive agents is inversely related to magnitude of tolerance after continuous infusion. Stevens, CW; Yaksh, TL, 1989) | 0.28 |
| " Naloxonazine shifted the supraspinal DAGO dose-response curve 4-fold to the right without changing the curve for spinal DAGO." | ( Different mu receptor subtypes mediate spinal and supraspinal analgesia in mice. Bodnar, RJ; Gistrak, MA; Pasternak, GW; Paul, D, 1989) | 0.28 |
| " The slopes of the dose-response lines were parallel, but the delta compound was about 250 times less potent than DAMGO." | ( Sympathoadrenal, cardiovascular and blood gas responses to highly selective mu and delta opioid peptides. Kiritsy-Roy, JA; Marson, L; Van Loon, GR, 1989) | 0.28 |
| " Antinociceptive dose-response curves were constructed for mu ([D-Ala2,NMePhe4,Gly-ol]enkephalin, DAGO; morphine) and delta ([D-Pen2,D-Pen5]enkephalin, DPDPE)-agonists in the absence, and in the presence of the mu non-surmountable antagonist, beta-funaltrexamine (beta-FNA) or the delta-antagonist ICI 174,864 (N,N-diallyl-Tyr-Aib-Aib-Phe-Leu-OH, where Aib is alpha-amino-isobutyric acid)." | ( Opioid delta-receptor involvement in supraspinal and spinal antinociception in mice. Heyman, JS; Mosberg, HI; Mulvaney, SA; Porreca, F, 1987) | 0.27 |
| " The dose-response curves of the preferential mu- ligands morphine and [D-Ala2, MePhe4, Gly-ol5] enkephalin (DAGO) were shifted by naloxone at low doses but not by ICI 174,864." | ( The role of mu- and delta- opioid receptors on the intestinal propulsion in rats. La Regina, A; Petrillo, P; Sbacchi, M; Tavani, A, 1986) | 0.27 |
| " The dose-response curves were shifted to the right in a non-parallel fashion with increasing calcium concentration (0." | ( Comparison of the effects of calcium concentration on mu and kappa agonist actions in the guinea pig ileum. Hill, RG; Hughes, J; Johnson, MA, 1986) | 0.27 |
| " Similar blockade was observed for EKC and U 50488 at doses of 10 and/or 20 ng/kg, but DAGO was unable to affect the AS-induced gastric inhibition at any dosage tested (20-200 ng/kg icv)." | ( CNS blockade of acoustic stress-induced gastric motor inhibition by kappa-opiate agonists in dogs. Alvinerie, M; Bueno, L; Gue, M; Honde, C; Junien, JL; Pascaud, X, 1988) | 0.27 |
| " Incubation of increasing concentrations of ICI 174,864 (10,30,100 and 300 nM) produced a dose-related and parallel rightward displacement of the DPDPE dose-response curve in the MVD." | ( Studies in vitro with ICI 174,864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO). Burks, TF; Hirning, LD; Hruby, VJ; Hurst, R; Mosberg, HI; Porreca, F, 1985) | 0.27 |
| " pairs of time-response curves, pairs of dose-response lines were constructed at various times; these lines showed decreasing displacement with time, indicative of the disappearance of naloxone." | ( Estimation of the affinity of naloxone at supraspinal and spinal opioid receptors in vivo: studies with receptor selective agonists. Heyman, JS; Koslo, RJ; Mosberg, HI; Porreca, F; Tallarida, RJ, 1986) | 0.27 |
| "The effects of the delta-selective antagonist ICI 174864 and naltrexone on the dose-response curves to the mu-selective agonist RX 783006 and D-ala-D-leucine enkephalin (DADL) have been investigated in the rat isolated vas deferens preparation (RVD) set up in Krebs solution containing half the normal Ca++ concentration." | ( Delta receptors in the rat vas deferens. Carter, A; Smith, CF, 1986) | 0.27 |
| " The pellets were removed and 24 h later, mice were sacrificed and binding studies were conducted, or mice were tested in analgesia (tail-flick) dose-response studies." | ( Supersensitivity to opioid analgesics following chronic opioid antagonist treatment: relationship to receptor selectivity. Chan, K; Davis, T; Duttaroy, A; Shah, S; Yoburn, BC, ) | 0.13 |
| " Pretreatment also shifted to the right the dose-response function for DALA intra-accumbens." | ( Mesoaccumbens dopamine-opiate interactions in the control over behaviour by a conditioned reinforcer. Everitt, BJ; Phillips, GD; Robbins, TW, 1994) | 0.29 |
| " The most potent analogue, D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2, caused a parallel rightward shift of the NMB dose-response curve, the Schild plot slope was not significantly different from unity, and the affinity was 230 nM." | ( Discovery of a novel class of neuromedin B receptor antagonists, substituted somatostatin analogues. Battey, JF; Coy, DH; Jensen, RT; Mantey, SA; Moreau, JP; Mrozinski, JE; Orbuch, M; Taylor, JE, 1993) | 0.29 |
| " In addition, opioid dose-response curves with preemptive administration were compared with early and late postadministrations." | ( Electrophysiologic analysis of preemptive effects of spinal opioids on N-methyl-D-aspartate receptor-mediated events. Chapman, V; Dickenson, AH; Haley, JE, 1994) | 0.29 |
| " Naloxone shifted to the right the dose-response curves for each opioid peptide significantly enhancing the ED50 values." | ( Modulation of non-adrenergic non-cholinergic inhibitory transmission in rat duodenum: role of opiates and 5-hydroxytryptamine. Adamo, EB; Di Giovanni, G; Marini, R; Mulè, F; Postorino, A; Serio, R, 1993) | 0.29 |
| " Dose-response curves were generated for both delta 9-THC (i." | ( Interactions between delta 9-tetrahydrocannabinol and kappa opioids in mice. Martin, BR; Smith, PB; Welch, SP, 1994) | 0.29 |
| "01-micrograms dosage was associated with hyperactivity." | ( Behavioral effects of the mu-opioid peptide agonists DAMGO, DALDA, and PL017 on locomotor activities. Meyer, ME, 1993) | 0.29 |
| "03 microgram of DAMGO resulting in a steeper dose-response relationship." | ( Evidence for delta opioid receptor subtypes in rat spinal cord: studies with intrathecal naltriben, cyclic[D-Pen2, D-Pen5] enkephalin and [D-Ala2, Glu4]deltorphin. Hammond, DL; Stewart, PE, 1993) | 0.29 |
| " The time course and dose-response relationships between mu receptor phosphorylation and agonist-induced desensitization display interesting parallels." | ( Differential mu opiate receptor phosphorylation and desensitization induced by agonists and phorbol esters. Mackin, S; Uhl, GR; Wang, JB; Weight, FF; Yu, Y; Zhang, L, 1996) | 0.29 |
| " Initial dose-response curves revealed that dopamine was approximately equipotent at producing motor activity after microinjection into the core and shell, AMPA was more effective in the core, whereas DAMGO was more potent in the shell." | ( Involvement of the ventral tegmental area in locomotion elicited from the nucleus accumbens or ventral pallidum. Churchill, L; Hooks, MS; Johnson, K; Kalivas, PW; Klitenick, MA, 1996) | 0.29 |
| " However, [D-Pen2,D-Pen5]enkephalin (DPDPE), a delta 1-opioid receptor agonist, and [D-Ala2,Cys4]deltorphin, a delta 2-opioid receptor agonist, at doses which exhibit no intrinsic effects (10(-8) and 10(-7) M), shifted the dose-response curve for mu-opioid receptor-evoked adenosine release to the left in a dose-dependent manner." | ( Synergy between mu/delta-opioid receptors mediates adenosine release from spinal cord synaptosomes. Cahill, CM; Sawynok, J; White, TD, 1996) | 0.29 |
| " Fentanyl pumps and placebo pellets were removed on the third day following implantation and 4 h later mu-opioid receptor saturation binding studies in whole brain ([3H][D-Ala2,MePhe4,Gly-ol5]enkephalin: DAMGO) or fentanyl analgesic dose-response studies (tailflick assay) were conducted." | ( Magnitude of tolerance to fentanyl is independent of mu-opioid receptor density. Chan, KW; Duttory, A; Yoburn, BC, 1997) | 0.3 |
| " However, inhibition reached the maximal level only at 50 mM sodium, and typical sigmoidal dose-response curves were obtained only in the presence of 118 mM sodium." | ( Regulation of mu-opioid receptor in neural cells by extracellular sodium. Medzihradsky, F; Yabaluri, N, 1997) | 0.3 |
| " injections of morphine or fentanyl, produced antinociceptive tolerance as shown by a significant rightward displacement of the agonist dose-response curves compared to controls." | ( Competitive and non-competitive NMDA antagonists block the development of antinociceptive tolerance to morphine, but not to selective mu or delta opioid agonists in mice. Bilsky, EJ; Hruby, VJ; Inturrisi, CE; Porreca, F; Sadée, W, 1996) | 0.29 |
| "055 nmol from the dose-response curve." | ( Central regulation of urine production by a selective mu-opioid agonist, [D-Ala2, N-Me-Phe4, Gly5-ol]-enkephalin, in rats. Matsuda, T; Mori, M; Tsushima, H, 1997) | 0.3 |
| " Naloxone (1 microM) or norbinaltorphimine (10 nM) shifted the dose-response curve of (-)-U50,488H to the right by 100-fold." | ( Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. Chen, C; Li, JG; Liu-Chen, LY; Luo, LY; Zhu, J, 1997) | 0.3 |
| " Prolonged exposure to agonists induced desensitization of the receptor as estimated by a reduction in the maximal stimulation of GTP[gamma-35S] binding by DAMGO and rightward shifts in the dose-response curves." | ( Down-regulation of mu-opioid receptor by full but not partial agonists is independent of G protein coupling. Medzihradsky, F; Yabaluri, N, 1997) | 0.3 |
| "0 mg/kg clocinnamox displaced the morphine dose-response curve 4-fold to the right of the control curve and 10 mg/kg clocinnamox eliminated morphine's antinociceptive effects at doses up to 1000 mg/kg for at least seven days." | ( Clocinnamox dose-dependently antagonizes morphine-analgesia and [3H]DAMGO binding in rats. Paronis, CA; Woods, JH, 1997) | 0.3 |
| " Dose-response curves for 1DMe in the presence of naltrindole or naltrexone, delta- and mu-opioid selective antagonists respectively, indicate that 1DMe preferentially reversed mu-receptor-mediated but increased delta-receptor-mediated analgesia." | ( Differential modulation of mu- and delta-opioid antinociception by neuropeptide FF receptors in young mice. Desprat, C; Zajac, JM, 1997) | 0.3 |
| ") pretreatment with calcium and thapsigargin, which increase intracellular calcium, reduced [D-Ala2,N-MePhe4,Gly-ol5]-enkephalin (DAMGO)-induced antinociception by shifting its dose-response curve to the right." | ( Role of intracellular calcium in modification of mu and delta opioid receptor-mediated antinociception by diabetes in mice. Kamei, J; Nagase, H; Ohsawa, M, 1998) | 0.3 |
| " Finally, shifts in the morphine dose-response lines after 24-h pretreatment with the four dihydrocodeinone compounds suggest that the nitrocinnamoylamino derivatives may produce a greater magnitude long-term antagonism of morphine-induced antinociception than the chlorocinnamoylamino analogs." | ( Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity. Archer, S; Bidlack, JM; Hill, KP; Jiang, Q; McLaughlin, JP; Sebastian, A, 1999) | 0.3 |
| " At doses of cocaine on the descending limb of the cocaine dose-response curve, the mu-selective agonist DAMGO produced a dose-related decrease in cocaine self-administration when delivered by microinfusion into the VTA." | ( The mu opioid agonist DAMGO alters the intravenous self-administration of cocaine in rats: mechanisms in the ventral tegmental area. Adamson, KL; Chow, BL; Coen, KM; Corrigall, WA, 1999) | 0.3 |
| " 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 combinations of moxonidine-morphine and moxonidine-deltorphin II resulted in significant leftward shifts in the dose-response curves compared to those of each agonist administered separately." | ( Moxonidine, a selective imidazoline/alpha(2) adrenergic receptor agonist, synergizes with morphine and deltorphin II to inhibit substance P-induced behavior in mice. Fairbanks, CA; Kitto, KF; Posthumus, IJ; Stone, LS; Wilcox, GL, 2000) | 0.31 |
| " TAPA dose-response curve for antinociception." | ( Selective antagonism by naloxonazine of antinociception by Tyr-D-Arg-Phe-beta-Ala, a novel dermorphin analogue with high affinity at mu-opioid receptors. Hayashi, T; Kisara, K; Kutsuwa, M; Sakurada, C; Sakurada, S; Sakurada, T; Sato, T; Takeda, S; Tan-No, K; Yuki, M, 2000) | 0.31 |
| ") 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 |
| " The MOR internalization is dose-dependent, with a similar dose-response to that observed for opioid-induced increases in potassium conductance." | ( Postsynaptic signaling via the [mu]-opioid receptor: responses of dorsal horn neurons to exogenous opioids and noxious stimulation. Abbadie, C; Basbaum, AI; Marek, K; Trafton, JA, 2000) | 0.31 |
| " Time- and dose-response curves were obtained in beta-endorphin-deficient and matched wild-type C57BL/6 congenic control mice using the tail-immersion/withdrawal assay." | ( Disparate spinal and supraspinal opioid antinociceptive responses in beta-endorphin-deficient mutant mice. Bales, JR; Belknap, JK; Grisel, JE; Hayward, MD; Low, MJ; Mogil, JS; Rubinstein, M, 2000) | 0.31 |
| " The Ca(2+) response occurred in all-or-none fashion and the half-maximal dosage of U50488H (812." | ( Cyclic AMP regulates the calcium transients released from IP(3)-sensitive stores by activation of rat kappa-opioid receptors expressed in CHO cells. Allen, CN; Grandy, DK; Ikeda, M; Nelson, CS; Shinagawa, H; Shinoe, T; Sugiyama, T; Yoshioka, T, 2001) | 0.31 |
| " NTB (30 nM) shifted the dose-response curve of DAMGO to the right and attenuated the maximal effect." | ( Pharmacological effects of naltriben as a ligand for opioid mu and kappa receptors in rat cerebral cortex. Cho, KP; Kim, KW; Shin, BS; Son, Y, 2001) | 0.31 |
| " The time course and dose-response studies demonstrated that mu receptor phosphorylation was a rapid event, exhibited a positive dose-dependent response, and was similar to that observed in the cloned mu receptor in CHO cells." | ( Agonist-induced mu opioid receptor phosphorylation and functional desensitization in rat thalamus. Deng, HB; Guang, W; Wang, H; Wang, JB; Yu, Y, 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 |
| " Furthermore, LY294002 at 33 nmol significantly shifted the dose-response curves for DAMGO-, DPDPE- and [D-Ala(2)]deltorphin II-induced antinociception to the right." | ( Implications of phosphoinositide 3-kinase in the mu- and delta-opioid receptor-mediated supraspinal antinociception in the mouse. Narita, M; Nemoto, M; Ohnishi, O; Suzuki, T; Yajima, Y, 2002) | 0.31 |
| " Among the opioid-responsive nociceptors, a gene dose-response relationship exists such that maximal opioid inhibition occurs when the MOR mRNA concentration of a cell is >15 pm." | ( Quantitative single-cell differences in mu-opioid receptor mRNA distinguish myelinated and unmyelinated nociceptors. Beacham, DW; McCleskey, EW; Silbert, SC, 2003) | 0.32 |
| " Using three human cancer cell lines: MIA PaCa-2 pancreatic adenocarcinoma, HT-29 colon adenocarcinoma, and CAL-27 squamous cell carcinoma of the head and neck, and OGF and the opioid antagonist naltrexone (NTX) at a dosage (10(-6)M) selected because it is known to repress or increase, respectively, cell replication, the effects on apoptosis (TUNEL, Annexin V) and necrosis (trypan blue) were investigated on days 2, 5, and 7 of exposure." | ( Opioids and the apoptotic pathway in human cancer cells. McLaughlin, PJ; Zagon, IS, 2003) | 0.32 |
| " In this study, potential neuronal sites and mechanisms responsible for the disturbances were investigated, dose-response relationships were established, and it was determined whether general anesthesia plays a role." | ( Mu-opioid receptor agonist effects on medullary respiratory neurons in the cat: evidence for involvement in certain types of ventilatory disturbances. Lalley, PM, 2003) | 0.32 |
| " Furthermore, the differences between intermittent and continuous dosing protocols were evaluated." | ( Opioid agonist and antagonist treatment differentially regulates immunoreactive mu-opioid receptors and dynamin-2 in vivo. Patel, K; Purohit, V; Yoburn, BC; Zhang, Q, 2004) | 0.32 |
| " A separate group of animals was used to investigate the dose-response effect on this motor dysfunction." | ( Mu and delta, but not kappa, opioid agonists induce spastic paraparesis after a short period of spinal cord ischaemia in rats. Davison, KJ; Fuchigami, T; Kakinohana, M; Marsala, M; Nakamura, S; Sugahara, K, 2006) | 0.33 |
| " None of the drugs affected the residual volume, micturition threshold pressure or bladder contraction pressure at any dosage examined." | ( Effects of opioid subtypes on detrusor overactivity in rats with cerebral infarction. Ishiura, Y; Komatsu, K; Nagasaka, Y; Nakamura, Y; Namiki, M; Yokoyama, O, 2007) | 0.34 |
| " Subclinical MOR activation (10 nM DAMGO) produced a leftward shift in (D-Ala2)-Deltorphin II dose-response curve in non-ligated rats (IC50 16." | ( Depression of C fibre-evoked spinal field potentials by the spinal delta opioid receptor is enhanced in the spinal nerve ligation model of neuropathic pain: involvement of the mu-subtype. Aguilera, L; Aira, Z; Azkue, JJ; Bilbao, J; Buesa, I; Mozas, M; Salgueiro, M; Urrutia, A; Zimmermann, M, 2008) | 0.35 |
| " The purpose of the present study was to characterize the dose-response and time-course of mu receptor occupancy following systemic cocaine administration and to determine if release of endogenous opioids by cocaine is mediated by activation of D1 or D2 dopamine receptors." | ( Cocaine-induced mu opioid receptor occupancy within the striatum is mediated by dopamine D2 receptors. Soderman, AR; Unterwald, EM, 2009) | 0.35 |
| " In a dose-response experiment, the low dose (0." | ( Preference for a high fat diet, but not hyperphagia following activation of mu opioid receptors is blocked in AgRP knockout mice. Argyropoulos, G; Barnes, MJ; Bray, GA, 2010) | 0.36 |
| " An intravenous loading dose of DAMGO followed by a 2 h constant rate infusion was administered to rats, and after a washout period of 1 h, GSH-PEG liposomal DAMGO was administered using a similar dosing regimen." | ( Enhanced brain delivery of the opioid peptide DAMGO in glutathione pegylated liposomes: a microdialysis study. Björkman, S; Gaillard, PJ; Hammarlund-Udenaes, M; Lindqvist, A; Rip, J, 2013) | 0.39 |
| " Isobolographic analyses of dose-response curves determined whether interactions were synergistic or additive." | ( The delta-opioid receptor is sufficient, but not necessary, for spinal opioid-adrenergic analgesic synergy. Chabot-Doré, AJ; Millecamps, M; Stone, LS, 2013) | 0.39 |
| "First, a dose-response curve for analgesic efficacy was generated for each opioid agonist." | ( Evaluation of the effects of specific opioid receptor agonists in a rodent model of spinal cord injury. Aceves, M; Hook, MA; Mathai, BB, 2016) | 0.43 |
| Class | Description |
|---|---|
| peptide | Amide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another with formal loss of water. The term is usually applied to structures formed from alpha-amino acids, but it includes those derived from any amino carboxylic acid. X = OH, OR, NH2, NHR, etc. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0030 | 0.0005 | 2.7739 | 25.1700 | AID141775 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0030 | 0.0005 | 2.8919 | 25.1700 | AID141775 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0030 | 0.0005 | 2.7478 | 25.1700 | AID141775 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0030 | 0.0005 | 2.7802 | 25.1700 | AID141775 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0030 | 0.0005 | 3.3142 | 49.5000 | AID141775 |
| Substance-P receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.0000 | 0.0001 | 0.1993 | 0.3981 | AID145798 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 100.0000 | 0.0002 | 0.9316 | 10.0000 | AID437483 |
| Gastrin/cholecystokinin type B receptor | Homo sapiens (human) | Ki | 0.0110 | 0.0001 | 0.0366 | 0.3450 | AID411824 |
| Delta-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 1.2415 | 0.0001 | 0.7298 | 10.0000 | AID1497530; AID1497533 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 3.2577 | 0.0000 | 0.6068 | 9.2330 | AID149804; AID514360; AID770994 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0132 | 0.0001 | 0.8874 | 10.0000 | AID141775; AID151457; AID242329; AID452777 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0026 | 0.0000 | 0.3845 | 8.6000 | AID141655; AID151616; AID151758; AID1689583; AID1877933; AID239174; AID312059; AID452777; AID497530; AID514359; AID770995 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0040 | 0.0001 | 0.8133 | 10.0000 | AID1186505; AID1277622; AID1285647; AID1336344; AID1355425; AID1425956; AID148354; AID1512057; AID1512058; AID1630481; AID340259; AID346442; AID480390; AID514364; AID751658; AID751864; AID752227 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0612 | 0.0000 | 0.4197 | 10.0000 | AID1138771; AID1162884; AID1185265; AID1197351; AID1237676; AID1268024; AID1268025; AID1268040; AID1355418; AID1434273; AID150841; AID150992; AID152071; AID1581727; AID1630477; AID1630710; AID1749821; AID1755974; AID1820694; AID1855412; AID1861726; AID239075; AID296543; AID346442; AID411820; AID437485; AID450016; AID603169; AID603170; AID603171; AID621887; AID647794; AID707254; AID747129; AID749692; AID751658; AID751864; AID765827 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0014 | 0.0002 | 0.7521 | 8.0140 | AID452776 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 1.7040 | 0.0000 | 0.5978 | 9.9300 | AID1197353; AID1237675; AID148220; AID148252; AID149891; AID150093; AID239157; AID452776; AID621888; AID647795; AID749691; AID765826 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 5.0000 | 0.0000 | 0.2018 | 6.4240 | AID514361 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 3.4116 | 0.0000 | 0.3624 | 10.0000 | AID1237677; AID147987; AID148023; AID148252; AID148714; AID239074; AID621889 |
| Nociceptin receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.0337 | 0.5000 | AID621019 |
| Mu-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 0.0048 | 0.0008 | 1.6992 | 10.0000 | AID1497529; AID1755977 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0008 | 0.0000 | 0.1228 | 1.3000 | AID1165886 |
| Nociceptin receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0011 | 0.0011 | 0.1765 | 0.6920 | AID268677 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0283 | 0.0002 | 0.6603 | 10.0000 | AID1497532 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0009 | 0.0000 | 0.2786 | 9.0000 | AID1630710; AID224571; AID268677 |
| [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) |
|---|---|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Km | 43.0000 | 0.0140 | 3.7172 | 10.0000 | AID678942 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | pEC50 | 0.0074 | 0.0074 | 0.0074 | 0.0074 | AID391171 |
| Mu-type opioid receptor | Homo sapiens (human) | ED50 | 0.0400 | 0.0340 | 0.0390 | 0.0420 | AID296734; AID440053; AID443807; AID749684 |
| Delta-type opioid receptor | Homo sapiens (human) | ED50 | 1.8500 | 0.0260 | 1.3337 | 1.9800 | AID149616 |
| Delta-type opioid receptor | Homo sapiens (human) | Emax | 0.1240 | 0.1240 | 0.1510 | 0.1780 | AID149617; AID56289 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | ED50 | 0.5090 | 0.5090 | 0.5690 | 0.6290 | AID148548 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Emax | 0.1350 | 0.0580 | 0.1274 | 0.1430 | AID148549; AID95207 |
| Kappa-type opioid receptor | Homo sapiens (human) | ED50 | 8.9400 | 0.0007 | 1.4569 | 8.9400 | AID443804 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | ED50 | 0.5920 | 0.3170 | 1.1153 | 2.1420 | AID152215 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Emax | 0.1230 | 0.1230 | 0.1483 | 0.1770 | AID138848; AID152217 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | pEC50 | 0.0074 | 0.0074 | 0.0074 | 0.0074 | AID391171 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID391172 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay relative to control | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
| AID603171 | Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | Generation of novel radiolabeled opiates through site-selective iodination. |
| AID1820166 | Displacement of [3H]-PrRP-20 from human PrRP receptor expressed in CHO cells by TopCount scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
| AID1528315 | Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP formation incubated for 8 min followed by forskolin stimulation by ELISA | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators. |
| AID1358134 | Agonist activity at human MOR expressed in African green monkey COS1 cell membranes assessed as stimulation of [35S]GTPgS binding at 10 uM by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| AID268678 | Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. |
| AID1186505 | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists. |
| AID251162 | Efficacy against isolated guinea pig ileum contraction induced by electrical stimulation | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor. |
| AID751658 | Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells after 60 mins | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
| AID765838 | Selectivity ratio of EC50 for human KOR to EC50 for human DOR | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID730861 | Agonist activity at FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis relative to DAMGO | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potent μ-opioid agonists. |
| AID1629756 | Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | 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. |
| AID440053 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphans. |
| AID264438 | Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells | 2006 | Journal of medicinal chemistry, May-18, Volume: 49, Issue:10 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
| AID95206 | [35S]GTP-gamma-S, induced maximal stimulation ( E max )against Kappa opioid receptor in guinea pig caudate membranes blocked with 6 nM nor-BNI | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
| AID765836 | Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID749684 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID1689596 | Agonist activity at human kappa opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID776680 | Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Novel 6β-acylaminomorphinans with analgesic activity. |
| AID422084 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
| AID1237675 | Displacement of [3H]-naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structural Requirements for CNS Active Opioid Glycopeptides. |
| AID149109 | Apparent binding affinity of compound was determined by antagonism towards Opioid receptor kappa 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate; na = not applicable | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID233860 | Selectivity between kappa opioid receptor and delta opioid receptor. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID127627 | Effective dose for the inhibition of acetylcholine induced mouse abdominal contriction was determined in vivo | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols. |
| AID443807 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
| AID751723 | Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells at 10 uM after 60 mins relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
| AID1700431 | Agonist activity at DOR in MOR knock out C57BL6 mouse spinal cord membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 60 mins by scintillation counting assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID1355425 | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as inhibition forskolin-induced cAMP accumulation after 15 mins by EIA | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist. |
| AID149891 | Binding affinity against Opioid receptor delta 1 | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine. |
| AID148354 | Binding activity against human Opioid receptor mu 1 using [3H]DAMGO as a radioligand | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics. |
| 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. |
| AID268680 | Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. |
| AID1820695 | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | |||
| AID621025 | Partial agonist activity at human MOP receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting relative to DAMGO | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID1689583 | Displacement of [3H]-DAMGO from rat mu opioid receptor expressed in CHO cells incubated for 30 mins by liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID592534 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
| AID151758 | Binding affinity against Opioid receptor mu 1 in P2 membrane preparation of rat brain by [3H]DAGO displacement. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Function of negative charge in the "address domain" of deltorphins. |
| AID1164347 | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
| AID1138774 | Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II. |
| AID1755977 | Agonist activity at mouse HA-tagged mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based | 2021 | Journal of natural products, 01-22, Volume: 84, Issue:1 | Isolation and Pharmacological Characterization of Six Opioidergic |
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| AID1165889 | Agonist activity at human MOR expressed in CHO cells by [35S]GTPgammaS binding assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies. |
| AID1506427 | Agonist activity at mouse KOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy relative to U50488H | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception. |
| AID1162884 | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID1386864 | Agonist activity at human mu opioid receptor expressed in human USOS-beta-arrestin-hMOR-PathHunter cells incubated for 90 mins by beta-arrestin-2 enzyme fragment complementation assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias. |
| 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. |
| AID1685502 | Agonist activity at human KOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID149124 | Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID452777 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
| AID148162 | Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor kappa 1 transfected into CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
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| AID268677 | Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. |
| AID385259 | Activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine. |
| AID232698 | Selectivity ratio of Ki of [3H]-DSLET to Ki of [3H]DAGO; relative inhibition at opioid receptor subtype delta 1 versus mu 1 | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID1689594 | Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID621021 | Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID680027 | TP_TRANSPORTER: inhibition of Deltorphin II uptake (Deltorphin II: 50 uM, DAMGO: 200 uM) in Xenopus laevis oocytes | 2000 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 294, Issue:1 | Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. |
| AID1138771 | Displacement of [3H]DAMGO from human mu opioid receptor transfected in CHO cell membranes after 60 mins | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II. |
| AID149804 | Binding affinity against Opioid receptor delta 1 in P2 membrane preparation of rat brain by [3H]DADLE displacement. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Function of negative charge in the "address domain" of deltorphins. |
| AID296062 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding after 60 mins | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. |
| AID386234 | Antagonist activity at CB1 receptor expressed in HEK293 cells assessed as blockade of secreted alkaline phosphatase activity at 1 uM after 6 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | Hemopressin is an inverse agonist of CB1 cannabinoid receptors. |
| AID765829 | Activation of mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to untreated control | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID138707 | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
| AID497534 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
| AID1543758 | Displacement of [3H]-DAMGO from MOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | (2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist. |
| AID1162887 | Inhibition of human kappa opioid receptor expressed in HEK293T cells assessed as inhibition of cAMP production after 30 mins | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID443804 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
| AID411821 | Binding affinity to mu opioid receptor expressed in CHO cells assessed per mg of protein | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. |
| AID138511 | Agonist activity was evaluated using mouse vas deferens assay in presence of delta-selective antagonist naltrindole (NTI); NR:Not reversed | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6 | Ring constrained analogues of the orvinols: the furanomorphides. |
| AID340259 | Inhibition of human mu opioid receptor | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. |
| AID1630716 | Selectivity ratio of Ki for displacement of [3H]U69593 from rat KOR expressed in CHO cells to Ki for displacement of [3H]DAMGO from MOR in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID1237685 | Selectivity ratio of Ki for human delta opioid receptor to Ki for human mu opioid receptor | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structural Requirements for CNS Active Opioid Glycopeptides. |
| 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. |
| AID475046 | Binding affinity to YC-tagged human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization. |
| AID1303079 | Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4 | Discovery of Potent and Selective Agonists of δ Opioid Receptor by Revisiting the "Message-Address" Concept. |
| AID621027 | Partial agonist activity at human KOP receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting relative to U69593 | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| 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. |
| AID1497532 | Agonist activity at mu-opioid receptor in guinea pig ileum assessed as inhibition of electrically induced contractions | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Chemical space screening around Phe |
| AID1630482 | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method relative to control | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID1700417 | Agonist activity at MOR/DOR in wild-type C57BL6 mouse spinal cord membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 60 mins by scintillation counting assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID239455 | Inhibition of [3H]nociceptin binding to human Opioid receptor like 1; ND denotes not determined | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| AID1685506 | Activity at human MOR expressed in CHOK1 cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment measured after 90 mins by PathHunter assay | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID1138783 | Displacement of [3H]Cl-DPDPE from human delta opioid receptor transfected in CHO cell membranes after 60 mins | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II. |
| AID149970 | Agonistic activity against Guinea pig ileum using nor-BNI as Opioid receptor kappa 1 antagonist; no reversal | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol. |
| AID149616 | Ability to stimulate binding to delta-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes, blocked with 20 nM naltrindole (NTI) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. |
| AID1630481 | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID95210 | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
| AID603170 | Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | Generation of novel radiolabeled opiates through site-selective iodination. |
| AID1855414 | Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 45 mins by cAMP HTRF assay | |||
| AID1581726 | Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes incubated for 60 mins | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. |
| AID1820170 | Displacement of [3H]-Diprenorphine from human DOP receptor expressed in HEK293 cells by scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
| AID670120 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting relative to control | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. |
| 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. |
| AID450022 | Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID452776 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
| AID138356 | Inhibitory activity before protection from beta-CNS-induced inactivation in MVD | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID1820710 | Half life of compound | |||
| AID450028 | Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID1855415 | Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 45 mins by cAMP HTRF assay relative to control | |||
| AID1685508 | Bias factor, ratio of biased agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin2 EFC recruitment to biased agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as inhibi | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID1714468 | Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID270238 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine. |
| AID1809486 | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. |
| AID149343 | Binding affinity to opioid receptor delta was determined in rat brain using [3H]DSTBULET as radioligand | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| 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. |
| AID246679 | Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1; ND denotes not determined | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| 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. |
| AID329904 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID1285647 | Displacement of [3H]DAMGO from human recombinant Mu-type opioid receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
| AID411820 | Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. |
| AID1497535 | Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Chemical space screening around Phe |
| AID1165886 | Displacement of [3H]DAMGO from mouse whole brain MOR | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies. |
| AID391171 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
| AID56281 | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
| AID1299237 | Agonist activity at MOR in Dunkin-Hartley guinea pig ileum assessed as inhibition of EFS-induced contractions incubated for 60 mins | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Evaluation of N-substituent structural variations in opioid receptor profile of LP1. |
| AID327873 | Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay | 2007 | The Journal of biological chemistry, Sep-14, Volume: 282, Issue:37 | Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors. |
| AID1820171 | Displacement of [3H]-Diprenorphine from human KOP receptor expressed in HEK293 cells by scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
| AID1700428 | Agonist activity at EA-fragment beta-arrestin-tagged human MOR/DOR expressed in human U2OS cell membranes assessed as stimulation beta-arrestin recruitment after 60 mins by Pathhunter chemiluminescence assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID554169 | Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to control | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Development of potent μ and δ opioid agonists with high lipophilicity. |
| AID592441 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting relative to control | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Aminothiazolomorphinans with mixed κ and μ opioid activity. |
| AID719302 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC. |
| AID621888 | Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID1162885 | Displacement of [3H]DADLE from delta opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID1497534 | Agonist activity at rat mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Chemical space screening around Phe |
| AID1689597 | Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID751864 | Binding affinity to human mu-type opioid receptor by radioligand displacement assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
| AID149294 | Binding affinity to opioid receptor mu was determined in rat brain using [3H]DAGO as radioligand | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| AID678942 | TP_TRANSPORTER: uptake in membrane vesicle from MDR1-expressing SW1573/S1 cell | 2001 | Peptides, Dec, Volume: 22, Issue:12 | MDR1 P-glycoprotein transports endogenous opioid peptides. |
| AID145798 | Affinity for rat Tachykinin receptor 1 determined in displacement screening by using radioligand 3,4-[3H]-(L-Pro e2) SP. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides. |
| AID1669026 | Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | |||
| AID132837 | Inhibitory effect was measured on mouse vas deferens | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| AID1630720 | Agonist activity at MOR in Dunkin-Hartley guinea pig ileum assessed as inhibition of electrically-evoked contractions | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID288866 | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay relative to control | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
| AID443808 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to 1 uM DAMGO | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
| AID149354 | It is the ratio of Ki value for delta receptor to that of opioid receptor mu | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| AID148626 | In vitro inhibitory activity against opioid receptor in Guinea pig ileum | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols. |
| AID1861724 | Binding affinity to sigma 2 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID1512056 | Ratio of IC50 for Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells at pH 7.4 to IC50 for Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells at pH 6.5 by Glo-sensor assay | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists. |
| AID1755974 | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO-K1 cells by radioligand binding assay | 2021 | Journal of natural products, 01-22, Volume: 84, Issue:1 | Isolation and Pharmacological Characterization of Six Opioidergic |
| AID1714485 | Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay relative to control | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID1129810 | Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation at 1 uM after 30 mins | 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. |
| AID554168 | Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Development of potent μ and δ opioid agonists with high lipophilicity. |
| AID1129819 | Intrinsic efficacy at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay relative to untreated control | 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. |
| AID1700420 | Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting method | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID232679 | Selectivity ratio, inhibition of electrically evoked contraction (IC50) of mouse vas deferens (MVD) versus guinea pig ileum (GPI) | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID151592 | Inhibition of [3H]DAGO binding to mu 1 opioid receptor in rat brain membranes | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID480390 | Displacement of [3H]naloxone from mu opioid receptor expressed in CHO cell membrane | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica. |
| AID1425956 | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists. |
| AID149996 | Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID1700424 | Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding at 10 uM after 60 mins by beta-galactosidase based scintillation counting method relative to DELT II | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID450021 | Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID1197353 | Displacement of [3H]DADLE from human recombinant opioid delta receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID268679 | Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. |
| AID765837 | Agonist activity at mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID1820168 | Displacement of [125I]-43RFa from human QRFP receptor expressed in CHO cells by TopCount scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
| AID347314 | Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists. |
| AID707254 | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 2 hrs by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus. |
| 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. |
| AID761674 | Displacement of [131I]-[D-Ala2,4'-I-Phe8]alpha-Neoendorphin from opioid receptor in CD-1 mouse brain after 90 mins by competitive binding assay | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Sandmeyer reaction repurposed for the site-selective, non-oxidizing radioiodination of fully-deprotected peptides: studies on the endogenous opioid peptide α-neoendorphin. |
| AID739881 | Agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting relative to control | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors. |
| AID149615 | Apparent binding affinity of compound was determined by antagonism towards opioid receptor delta 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate; na = not applicable | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID224571 | Binding affinity against mu opioid receptor | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine. |
| AID231502 | Ratio of binding affinity of mu and delta opioid receptor | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID141775 | Binding affinity against rat mu-opioid receptor expressed in CHO cells by competitive inhibition of 1 nM [3H]DAMGO | 1998 | Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15 | Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors. |
| AID670121 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [33S]GTPgammaS binding after 60 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. |
| AID765839 | Selectivity ratio of EC50 for human KOR to EC50 for human MOR | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID1861723 | Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID239075 | Inhibition of [3H]diprenorphine binding to human Opioid receptor mu 1 | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| AID149656 | Binding affinity against Opioid receptor delta 1 by displacement of radioligand [3H]DSLET in rat brain membrane | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID739880 | Antagonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors. |
| AID1685507 | Activity at human MOR expressed in CHOK1 cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment measured after 90 mins by PathHunter assay relative to control | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID286312 | Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors. |
| AID327872 | Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM | 2007 | The Journal of biological chemistry, Sep-14, Volume: 282, Issue:37 | Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors. |
| AID410728 | Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID239074 | Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| AID452782 | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
| AID1714470 | Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID149719 | Agonistic activity towards Opioid receptor mu 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID95211 | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor. |
| AID149724 | Emax value towards Opioid receptor mu 1 determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID1755980 | Agonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay | 2021 | Journal of natural products, 01-22, Volume: 84, Issue:1 | Isolation and Pharmacological Characterization of Six Opioidergic |
| AID415726 | Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies. |
| AID148549 | Ability to stimulate binding to kappa-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes, blocked with 6 nM nor-binaltorphimine (nor-BNI) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. |
| AID1685509 | Activity at human MOR expressed in U2OS cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment by Tango assay | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID1861727 | Binding affinity to DOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID147987 | Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID151599 | Binding affinity against Opioid receptor mu 1 by displacement of radioligand [3H]-DAGO in rat brain membrane | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| 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. |
| AID1268024 | Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexy | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24 | Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor. |
| AID56288 | [35S]GTP-gamma-S, induced maximal stimulation ( E max ) Delta opioid receptor in guinea pig caudate membranes blocked with 20 nM NTI | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
| AID151432 | Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | 2000 | Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24 | Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids. |
| AID1820172 | Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells by scintillation counting analysis | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
| AID621887 | Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID747129 | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. |
| AID261097 | Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. |
| AID1689598 | Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID1497529 | Displacement of [125I]-DAMGO from mouse Flag-tagged mu-opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Chemical space screening around Phe |
| AID443805 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to 500 nM (-)-U50488 | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
| AID730862 | Agonist activity at FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potent μ-opioid agonists. |
| AID320361 | Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
| AID138843 | [35S]GTP-gamma-S, induced maximal stimulation ( E max ) against Mu opioid receptor in guinea pig caudate membranes blocked with 6000 nM CTAP; NS indicates No simulation | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
| AID148023 | In vitro potency was measured against human Opioid receptor kappa 1 | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics. |
| AID1268025 | Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24 | Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor. |
| 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. |
| AID1129817 | Agonist activity at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay | 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. |
| AID1506425 | Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy relative to DAMGO | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception. |
| AID776682 | Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Novel 6β-acylaminomorphinans with analgesic activity. |
| AID1497533 | Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Chemical space screening around Phe |
| AID149659 | Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID1714472 | Selectivity ratio of EC50 for agonist activity at human kappa opiod receptor expressed in CHO-K1 cells to EC50 for agonist activity at human mu opiod receptor expressed in CHO-K1 cells | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID450016 | Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID690646 | Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting relative to control | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixed μ/δ opioid receptor agonistic properties. |
| AID246504 | Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor mu 1 | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| AID286311 | Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors. |
| 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. |
| AID1861725 | Selectivity index, ratio of Ki for sigma 1 receptor (unknown origin) to Ki for sigma 2 receptor (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID621019 | Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID1820673 | Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry | |||
| AID1685504 | Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID1630718 | Selectivity ratio of Ki for displacement of [3H]DPDPE from human DOR expressed in CHO cells to Ki for displacement of [3H]DAMGO from MOR in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID1630712 | Displacement of [3H]DPDPE from human DOR expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID592440 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Aminothiazolomorphinans with mixed κ and μ opioid activity. |
| AID514367 | Agonist activity at delta opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation at 1 pM to 10 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID621022 | Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID1434273 | Displacement of [3H]DAMGO from human MOR expressed in CHO cells | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands. |
| AID329907 | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to (-)-U50,488 | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID1877933 | Displacement of [3H]-DAMGO from Sprague-Dawley rat brain membrane mu opioid receptor incubated for 45 mins by liquid scintillation counting analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation. |
| AID334454 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum membrane | 1992 | Journal of natural products, Mar, Volume: 55, Issue:3 | Akuammine and dihydroakuammine, two indolomonoterpene alkaloids displaying affinity for opioid receptors. |
| AID149767 | Apparent binding affinity of compound was determined by antagonism towards opioid receptor delta 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate; na = not applicable | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID148345 | Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID229273 | Ratio of IC50 measured in MVD to that of GPI. | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| AID1700416 | Agonist activity at EA-fragment beta-arrestin-tagged human MOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting method | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID259401 | Functional activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors. |
| AID1855412 | Displacement of [3H]-DAMGO from human MOR expressed in CHO-K1 cell membranes incubated for 90 mins measured by MicroBeta scintillation counter method | |||
| AID1630711 | Displacement of [3H]U69593 from rat KOR expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID138338 | Agonist activity was evaluated using mouse vas deferens assay. | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6 | Ring constrained analogues of the orvinols: the furanomorphides. |
| AID296543 | Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in in CHO cells | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids. |
| AID152071 | Binding affinity for mu opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9 | New scaffolds in the development of mu opioid-receptor ligands. |
| 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). |
| AID1820706 | Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay | |||
| AID690645 | Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixed μ/δ opioid receptor agonistic properties. |
| AID1714467 | Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID452783 | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding relative to untreated basal control | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. |
| AID1820694 | Displacement of [3H]-Diprenorphine from human mu opiod receptor expressed in CHO cells incubated for 1 hr by competition binding assay | |||
| AID125747 | Analgesic potency in mice after icv injection and 10 min before exposing to hot plate | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID765834 | Activation of human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to untreated control | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID411824 | Displacement of [3H]DAMGO from CCK2R-MOPR coexpressed in CHO cells | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. |
| 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. |
| AID296734 | Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorph |
| AID56289 | [35S]GTP-gamma-S, induced maximal stimulation ( E max ) Delta opioid receptor in guinea pig caudate membranes blocked with 20 nM NTI | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor. |
| AID346442 | Displacement of radiolabeled DAMGO from human mu-type opioid receptor agonist site | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. |
| 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. |
| AID246131 | Inhibition of isolated guinea pig ileum contraction induced by electrical stimulation | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor. |
| AID151601 | Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID1197354 | Displacement of [3H]U69,593 from human recombinant opioid kappa receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID437483 | Binding affinity to adenosine receptor A1 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist. |
| AID1714490 | Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production up to 10 uM measured after 30 mins by HitHunter luminescence based assay relative to control | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID138522 | Ke value for naloxone as antagonist (compound) was measured by using Mouse vas deferens (MVD) assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID1506424 | Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception. |
| AID1700419 | Agonist activity at EA-fragment beta-arrestin-tagged human MOR expressed in human U2OS cell membranes assessed as stimulation beta-arrestin recruitment after 60 mins by Pathhunter chemiluminescence assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID138847 | [35S]GTP-gamma-S, induced maximal stimulation ( E max )against Mu opioid receptor in guinea pig caudate membranes in unblocked condition | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
| AID148252 | In vitro potency was measured against human Opioid receptor delta 1 | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics. |
| AID1861726 | Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID79042 | Opioid agonistic activity against Guinea pig ileum | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol. |
| AID151285 | Dissociation constant of [3H]DAMGO binding to Opioid receptor mu 1 from rat brain membrane | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity. |
| AID765831 | Activation of human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to U69593 | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID1655383 | Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin. |
| AID747126 | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. |
| AID514364 | Agonist activity at mu opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID422085 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay relative to basal level | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16 | Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
| AID392479 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. |
| AID296061 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. |
| AID670122 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [33S]GTPgammaS binding after 60 mins by scintillation counting relative to control | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. |
| AID150093 | Binding affinity for delta opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9 | New scaffolds in the development of mu opioid-receptor ligands. |
| AID514359 | Displacement of [3H]DAMGO from Sprague-Dawley rat mu opioid receptor by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID1164346 | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to untreated control | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
| AID259402 | Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors. |
| AID150992 | In vitro potency was measured against human Opioid receptor mu 1 | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics. |
| AID141655 | Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library. |
| AID1689599 | Agonist activity at human kappa opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID1237677 | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structural Requirements for CNS Active Opioid Glycopeptides. |
| AID1268040 | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24 | Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor. |
| AID288856 | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
| AID1820169 | Displacement of [3H]-Diprenorphine from human MOP receptor expressed in HEK293 cells by scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
| AID392481 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. |
| AID150841 | Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID78873 | Concentration of compound to inhibit 50% (IC50) electrically evoked contractions was tested in Guinea pig ileum(GPI) assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID621020 | Selectivity ratio of Ki for human MOP receptor to Ki for human NOP receptor | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID229266 | Ratio of IC50 in Mouse vas deferens and Guinea pig ileum assay | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID1809485 | Agonist activity at human MOR expressed in HEK-293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay relative to DAMGO | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. |
| AID776681 | Agonist activity at mouse cloned kappa opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Novel 6β-acylaminomorphinans with analgesic activity. |
| AID1194143 | Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by cytosensor micrometer | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands. |
| AID1630477 | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID765840 | Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID148070 | Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID329906 | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID232233 | Selectivity given as ratio of mu receptor to delta receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID765828 | Activation of mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to U69593 | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID410730 | Activity at human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID149865 | Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus:longitudinal muscle preparation) by antagonist action at mu 1 opioid receptors | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID621889 | Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
| AID242329 | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-]. |
| AID177312 | In vivo efficacy was measured using thermal escape assay | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics. |
| AID151757 | Compound was evaluated for the binding affinity of Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from rat brain membrane | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity. |
| AID765827 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Probes for narcotic receptor mediated phenomena. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation. |
| AID1604697 | Agonist activity at human MOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
| AID392480 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. |
| AID1633370 | Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
| AID592535 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. |
| AID1237676 | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structural Requirements for CNS Active Opioid Glycopeptides. |
| AID1820678 | Agonist activity at mu opioid receptor (unknown origin) assessed as maximal cAMP level incubated for 40 mins by spectrophotometry relative to DAMGO | |||
| AID1386861 | Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by scintillation counting method | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias. |
| AID1809484 | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. |
| AID411826 | Activity at CCK2R-MOPR coexpressed in CHO cells co-transfected with delta-6-Galphaqi4-myr assessed as intracellular calcium release by FLIPR | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. |
| AID1512058 | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 6.5 measured after 15 mins by Glo-Sensor assay | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists. |
| AID1336344 | Displacement of [3H]DAMGO from human recombinant mu-opioid receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
| AID450511 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain measured total binding per mg of protein at 5 uM | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. |
| AID603169 | Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | Generation of novel radiolabeled opiates through site-selective iodination. |
| AID647795 | Displacement of [3H]-DADLE from human delta opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selective μ-antagonist activity. |
| 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). |
| AID719301 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting relative to untreated-control | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC. |
| AID497530 | Displacement of [3H]DPDPE from rat mu opioid receptor | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
| AID138345 | Concentration of compound to inhibit 50% (IC50) electrically evoked contractions was tested in Mouse vas deferens (MVD) assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID78859 | Agonistic activity in electrically stimulated guinea pig ileum preparation (GPI) | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6 | Ring constrained analogues of the orvinols: the furanomorphides. |
| AID151468 | Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes. | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12 | Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
| AID749691 | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID296060 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding relative to basal level after 60 mins | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. |
| AID1581725 | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes incubated for 60 mins | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. |
| AID749692 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID149647 | Ability to inhibit the binding of [3H]DSLET to Opioid receptor delta 1 in rat brain membranes | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID310355 | Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC. |
| AID239157 | Inhibition of [3H]naltrindole binding to human Opioid receptor delta 1 | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| AID1689595 | Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID151457 | The compound was tested for binding affinity towards rat Opioid receptor mu 1 by displacing [3H]DAMGO. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides. |
| 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. |
| AID220597 | Inhibition of adenylyl cyclase activity in membranes of the human SH-SY5Y neuroblastoma cell line. | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives. |
| AID138848 | [35S]GTP-gamma-S, induced maximal stimulation ( E max )against Mu opioid receptor in guinea pig caudate membranes in unblocked condition | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor. |
| AID148714 | Binding affinity for kappa opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9 | New scaffolds in the development of mu opioid-receptor ligands. |
| AID148548 | Ability to stimulate binding to kappa-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes, blocked with 6 nM nor-binaltorphimine (nor-BNI) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. |
| AID497535 | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding relative to control | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
| AID152215 | Ability to stimulate binding to mu-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes under unblocked condition | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. |
| AID1685503 | Agonist activity at human KOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay relative to DAMGO | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID747128 | Displacement of [3H]DADLE from delta opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. |
| AID1528331 | Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP formation incubated for 8 min followed by forskolin stimulation by ELISA (Rvb = 0 %) | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators. |
| AID233862 | Selectivity between mu opioid receptor and delta opioid receptor. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID1197351 | Displacement of [3H]DAMGO from human recombinant opioid mu receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID1700426 | Agonist activity at EA-fragment beta-arrestin-tagged human MOR/DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting method | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID1611182 | Agonist activity at human mu opioid receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP production by FRET assay | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity. |
| AID1456288 | Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study. |
| AID247134 | Agonist activity as maximal effect in [35S]-GTP-gamma binding assay compared to 10 uM DAMGO | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| AID152231 | Ability to stimulate binding to mu-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes, blocked with 6000 nM CTAP; NS=no stimulation | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. |
| AID1685511 | Bias factor, ratio of biased agonist activity at human mu opiod receptor expressed in U2OS cells assessed as stimulation of beta-arrestin2 EFC recruitment to biased agonist activity at human mu opiod receptor expressed in U2OS cells assessed as inhibition | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID670119 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. |
| AID1685510 | Activity at human MOR expressed in U2OS cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment by Tango assay relative to control | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID151447 | Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12 | Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
| AID1185265 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cells by scintillation counting | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Synthesis of tripeptides containing D-Trp substituted at the indole ring, assessment of opioid receptor binding and in vivo central antinociception. |
| 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. |
| AID239174 | Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-]. |
| AID79199 | Agonistic activity in electrically stimulated guinea pig ileum preparation (GPI) in presence of mu-selective antagonist CTAP | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6 | Ring constrained analogues of the orvinols: the furanomorphides. |
| AID385258 | Activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine. |
| AID1861728 | Binding affinity to KOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID232691 | Selectivity ratio of Ki (Delta opioid receptor) to that of Ki (mu opioid receptor) | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine. |
| AID1888741 | Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward δ and κ opioid receptors. |
| AID514360 | Displacement of [3H]DPDPE from Sprague-Dawley rat delta opioid receptor by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID1194141 | Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by microplate reader analysis | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands. |
| 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. |
| AID1714469 | Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID329911 | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as induction of yellow fluorescent protein internalization at 1 uM after 24 hrs | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID232232 | Selectivity given as ratio of kappa receptor to delta receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID1685505 | Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay relative to DAMGO | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID201472 | Potency for inhibition of forskolin-stimulated cyclic AMP accumulation in SH-SY5Y cells | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12 | Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
| AID1685500 | Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID1162886 | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID1700425 | Agonist activity at EA-fragment beta-arrestin-tagged human MOR expressed in human U2OS cell membranes assessed as stimulation beta-arrestin recruitment at 10 uM after 60 mins by Pathhunter chemiluminescence assay relative to DELT II | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID417157 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID1820167 | Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
| AID1685501 | Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay relative to DAMGO | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | G-Protein biased opioid agonists: 3-hydroxy- |
| AID132841 | Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus;longitudinal muscle)[agonist action at mu 1 opioid receptors) and inhibition of electrically evoked contraction of mouse vas deferens (agonist action at delta 1 opioid rec | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID365600 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID1700421 | Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation beta-arrestin recruitment after 60 mins by Pathhunter chemiluminescence assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID148382 | Percent stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor delta 1 expressed in CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID411825 | Binding affinity to CCK2R-MOPR coexpressed in CHO cells assessed per mg of protein by [3H]DAMGO displacement assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. |
| AID1358122 | Displacement of [3H]diprenorphine from human MOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| AID152217 | Ability to stimulate binding to mu-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes under unblocked condition | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. |
| AID247140 | Agonist activity as maximal effect in [35S]-GTP-gamma binding assay compared to 60 nM N/OFQ; ND denotes not determined | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor. |
| AID592439 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Aminothiazolomorphinans with mixed κ and μ opioid activity. |
| AID1237684 | Selectivity ratio of Ki for human kappa opioid receptor to Ki for human mu opioid receptor | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structural Requirements for CNS Active Opioid Glycopeptides. |
| AID1355424 | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as inhibition forskolin-induced cAMP accumulation at 0.00001 to 100 uM after 15 mins by EIA relative to control | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist. |
| AID79036 | Inhibitory effect was measured on guinea pig ileum for maximal contraction | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| AID147899 | Apparent binding affinity of compound was determined by antagonism towards Opioid receptor mu 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate; na = not applicable | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID410729 | Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to basal GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID1456286 | Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method relative to DAMGO | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study. |
| AID514365 | Agonist activity at delta opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID514361 | Displacement of [3H]U69593 from Sprague-Dawley rat kappa opioid receptor in guinea pig cerebella by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID1355418 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membranes after 2 hrs by liquid scintillation spectrometry | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist. |
| AID417156 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID151616 | Binding affinity towards Opioid receptor mu 1 | 2000 | Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24 | Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids. |
| AID1386867 | Selectivity index, change in deltalog(Tau/KA) for agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding to deltalog(Tau/KA) for agonist activity at human mu opioid receptor expressed | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias. |
| AID329908 | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2-GFP plasma membrane translocation at 1 uM after 10 mins | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID296733 | Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay relative to DAMGO | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorph |
| AID1581727 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes incubated for 60 mins | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. |
| AID1497530 | Displacement of [125I]-Deltorphin 2 from mouse Flag-tagged delta-opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Chemical space screening around Phe |
| AID475044 | Induction of receptor internalization in YFP-tagged mu opioid receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization. |
| AID1386868 | Bias factor, change in deltalog(Tau/KA) for agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding to deltalog(Tau/KA) for agonist activity at human mu opioid receptor expressed in hu | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias. |
| AID1506426 | Agonist activity at mouse KOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception. |
| AID138844 | [35S]GTP-gamma-S, induced maximal stimulation ( E max ) against Mu opioid receptor in guinea pig caudate membranes blocked with 6000 nM CTAP; NS indicates No simulation | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor. |
| AID290265 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as DAMGO-stimulated [35S]GTP-gamma-S binding | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | High-affinity carbamate analogues of morphinan at opioid receptors. |
| AID1655287 | Displacement of [3H]-DAMGO from MOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | |||
| AID739882 | Agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors. |
| AID1700430 | Agonist activity at MOR in DOR knock out C57BL6 mouse spinal cord membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 60 mins by scintillation counting assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template. |
| AID1358133 | Agonist activity at human MOR expressed in African green monkey COS1 cell membranes assessed as stimulation of [35S]GTPgS binding at 1 uM by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| AID148544 | Agonistic activity towards Opioid receptor kappa 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate; na = not applicable | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID1820707 | Agonist activity at mu opioid receptor (unknown origin) assessed as maximal beta arrestin-2 recruitment incubated for 3 days by PathHunter assay relative to DAMGO | |||
| AID765842 | Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID1164342 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Novel cyclic biphalin analogue with improved antinociceptive properties. |
| AID56295 | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor. |
| AID415725 | Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation [35S]GTPgammaS binding relative to basal level | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies. |
| AID95207 | [35S]GTP-gamma-S, induced maximal stimulation ( E max )against Kappa opioid receptor in guinea pig caudate membranes blocked with 6 nM nor-BNI | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor. |
| AID752227 | Binding affinity to mu opioid receptor (unknown origin) by radioligand displacement assay | 2013 | Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10 | Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
| AID1358121 | Displacement of [3H]diprenorphine from human MOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| AID79361 | The relative potency of compound was measured by comparing with [Leu]enkephalin in Guinea pig ileum(GPI) assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID151009 | Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor mu 1 transfected into CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID437485 | Binding affinity to mu opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist. |
| AID1749821 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis | |||
| AID514366 | Agonist activity at mu opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation at 1 pM to 10 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID148542 | Dose ratio IC50 after beta-CAN (10e-7 M) 15 min pretreatment on guinea pig ileum in presence of DAMGO divided by IC50 before beta-CNA/DAMGO treatment against opioid receptor kappa in guinea pig ileum | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols. |
| 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. |
| AID228347 | Ratio of Ki values for mu and delta opioid receptors. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Function of negative charge in the "address domain" of deltorphins. |
| AID1809487 | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay relative to DAMGO | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse 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. |
| AID765841 | Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID765826 | Displacement of [3H]DADLE from human delta opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Probes for narcotic receptor mediated phenomena. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation. |
| AID749683 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding at 1000 nM after 3 hrs by liquid scintillation counting analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID264437 | Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells | 2006 | Journal of medicinal chemistry, May-18, Volume: 49, Issue:10 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
| AID647794 | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selective μ-antagonist activity. |
| AID1512057 | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 7.4 measured after 15 mins by Glo-Sensor assay | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists. |
| AID264435 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | 2006 | Journal of medicinal chemistry, May-18, Volume: 49, Issue:10 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
| AID79202 | Ke value for naloxon as antagonist (compound) was measured by using Guinea pig ileum assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID141499 | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor. |
| AID149617 | Ability to stimulate binding to delta-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes, blocked with 20 nM naltrindole (NTI) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. |
| AID1714473 | Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay relative to DAMGO | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 | Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability. |
| AID79356 | Relative potency to that of [DAla2,Leu5]enkaphalinamide. | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| AID1591427 | Agonist activity at human mu opioid receptor expressed in CHO cells by cAMP assay | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity. |
| AID149957 | The relative potency of compound was measured against Opioid receptor delta 1 to that of [Leu]enkephalin in [3H]DSLET binding assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID290264 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | High-affinity carbamate analogues of morphinan at opioid receptors. |
| AID148206 | Opioid agonistic activity against Guinea pig ileum using CTAP as Opioid receptor mu 1 antagonist | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol. |
| AID264436 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | 2006 | Journal of medicinal chemistry, May-18, Volume: 49, Issue:10 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
| AID450520 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. |
| AID137098 | Relative potency to that of [D-Ala2, Leu5]-enkaphalinamide in mouse vas deferens | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
| AID152050 | The relative potency of compound was measured against Opioid receptor mu 1 to that of [Leu]enkephalin in [3H]DAGO binding assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID765832 | Activation of human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to DPDPE | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening. |
| AID148220 | Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID138530 | The relative potency of compound was measured by comparing with [Leu]enkephalin in Mouse vas deferens (MVD) assay. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity. |
| AID138355 | Inhibitory activity after protection from beta-CNS-induced inactivation in MVD | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
| AID1277622 | Agonist activity at human MOR expressed in CHO cells assessed as induction of membrane potential change measured every 3 secs for 30 secs by fluorescent membrane potential assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation. |
| AID1798042 | Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay from Article 10.1021/jm061465o: \\Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.\\ | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors. |
| AID1798026 | Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay from Article 10.1021/jm070332f: \\A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Recept | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. |
| AID1798046 | Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay from Article 10.1021/jm050921q: \\Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.\\ | 2006 | Journal of medicinal chemistry, May-18, Volume: 49, Issue:10 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. |
| AID1346411 | Rat kappa receptor (Opioid receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21 | Cloning and pharmacological characterization of a rat kappa opioid receptor. |
| AID1346364 | Human mu receptor (Opioid receptors) | 1981 | European journal of pharmacology, Apr-09, Volume: 70, Issue:4 | Analogues of beta-LPH61-64 possessing selective agonist activity at mu-opiate receptors. |
| AID1346364 | Human mu receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
| AID1346329 | Human kappa receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
| AID1346400 | Rat mu receptor (Opioid receptors) | 1994 | Molecular pharmacology, Feb, Volume: 45, Issue:2 | Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 322 (11.57) | 18.7374 |
| 1990's | 1129 (40.55) | 18.2507 |
| 2000's | 824 (29.60) | 29.6817 |
| 2010's | 434 (15.59) | 24.3611 |
| 2020's | 75 (2.69) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (10.33) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 1 (0.04%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Reviews | 19 (0.70%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 2 (0.07%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 151 (100.00%) | 84.16% |
| Other | 2,705 (99.19%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||