Page last updated: 2024-08-07 16:37:11
Delta-type opioid receptor
A delta-type opioid receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41143]
Synonyms
D-OR-1;
DOR-1
Research
Bioassay Publications (333)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 11 (3.30) | 18.7374 |
| 1990's | 46 (13.81) | 18.2507 |
| 2000's | 137 (41.14) | 29.6817 |
| 2010's | 113 (33.93) | 24.3611 |
| 2020's | 26 (7.81) | 2.80 |
Compounds (198)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bremazocine | Homo sapiens (human) | IC50 | 0.0010 | 3 | 4 |
| amiodarone | Homo sapiens (human) | IC50 | 8.0140 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 2.8250 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 12.9790 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 4.5750 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 20.8940 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 7.3650 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | IC50 | 26.8940 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | Ki | 9.4810 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 4.9780 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 1.7550 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 1.4420 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 0.5080 | 1 | 0 |
| fentanyl | Homo sapiens (human) | IC50 | 0.3092 | 2 | 2 |
| fentanyl | Homo sapiens (human) | Ki | 0.8025 | 2 | 2 |
| fluphenazine | Homo sapiens (human) | IC50 | 24.0360 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 8.4730 | 1 | 0 |
| fluspirilene | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| ketoconazole | Homo sapiens (human) | IC50 | 12.7970 | 1 | 0 |
| ketoconazole | Homo sapiens (human) | Ki | 4.5110 | 1 | 0 |
| loperamide | Homo sapiens (human) | IC50 | 0.8960 | 1 | 0 |
| loperamide | Homo sapiens (human) | Ki | 0.3160 | 1 | 0 |
| 4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide | Homo sapiens (human) | IC50 | 1.6200 | 1 | 1 |
| meperidine | Homo sapiens (human) | IC50 | 16.8333 | 3 | 3 |
| methadone | Homo sapiens (human) | IC50 | 1.0900 | 1 | 1 |
| miconazole | Homo sapiens (human) | IC50 | 3.3870 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 1.1940 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| pyroxamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| raloxifene | Homo sapiens (human) | IC50 | 6.6440 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 2.3420 | 1 | 0 |
| vorinostat | Homo sapiens (human) | IC50 | 7.2000 | 1 | 1 |
| ultram | Homo sapiens (human) | Ki | 0.0094 | 1 | 1 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pimozide | Homo sapiens (human) | IC50 | 3.7600 | 1 | 1 |
| cyclazocine | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| penfluridol | Homo sapiens (human) | Ki | 1.7140 | 1 | 1 |
| tramadol | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| paclitaxel | Homo sapiens (human) | IC50 | 4.2020 | 1 | 0 |
| paclitaxel | Homo sapiens (human) | Ki | 1.4810 | 1 | 0 |
| spiradoline | Homo sapiens (human) | Ki | 7.1500 | 2 | 4 |
| enadoline | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| carfentanil | Homo sapiens (human) | Ki | 0.0033 | 1 | 1 |
| nelfinavir | Homo sapiens (human) | IC50 | 66.1490 | 1 | 0 |
| nelfinavir | Homo sapiens (human) | Ki | 23.3190 | 1 | 0 |
| loperamide hydrochloride | Homo sapiens (human) | IC50 | 0.1230 | 1 | 1 |
| enkephalin, d-penicillamine (2,5)- | Homo sapiens (human) | IC50 | 0.0011 | 3 | 3 |
| enkephalin, d-penicillamine (2,5)- | Homo sapiens (human) | Ki | 0.0759 | 8 | 9 |
| vanoxerine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| u 69593 | Homo sapiens (human) | IC50 | 3.6437 | 4 | 6 |
| u 69593 | Homo sapiens (human) | Ki | 6.7140 | 11 | 14 |
| gr 127935 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| tifluadom | Homo sapiens (human) | Ki | 0.0321 | 2 | 5 |
| bw 373u86 | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| bw 373u86 | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| pramipexole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| enkephalin-leu, arg(6)- | Homo sapiens (human) | Ki | 0.0091 | 1 | 1 |
| tyrosyl-arginyl-phenylalanyl-lysinamide | Homo sapiens (human) | Ki | 19.2000 | 1 | 1 |
| met-enkephalinamide | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | IC50 | 0.0086 | 7 | 7 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | Ki | 0.0014 | 5 | 5 |
| 4-methoxymethylfentanyl | Homo sapiens (human) | Ki | 0.0230 | 1 | 1 |
| 2-(3,4-dichlorophenyl)-n-methyl-n-(1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl)acetamide | Homo sapiens (human) | IC50 | 1.0000 | 1 | 2 |
| salvinorin a | Homo sapiens (human) | Ki | 8.1360 | 8 | 10 |
| 3,5-bis(trifluoromethyl)benzyl n-acetyltryptophan | Homo sapiens (human) | Ki | 0.1340 | 1 | 1 |
| ly 106737 | Homo sapiens (human) | Ki | 0.0330 | 4 | 4 |
| 5-hydroxy-3',4',6,7-tetramethoxyflavone | Homo sapiens (human) | Ki | 3.1000 | 1 | 1 |
| enkephalin, pen(2,5)-4-chloro-phe(4)- | Homo sapiens (human) | IC50 | 0.0015 | 2 | 2 |
| salvigenin | Homo sapiens (human) | Ki | 26.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| trapoxin a | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
| saquinavir | Homo sapiens (human) | IC50 | 28.1680 | 1 | 0 |
| saquinavir | Homo sapiens (human) | Ki | 9.9300 | 1 | 0 |
| enkephalin, methionine | Homo sapiens (human) | IC50 | 0.0064 | 1 | 1 |
| enkephalin, methionine | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| diprenorphine | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| trichostatin a | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 2.7180 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 0.9580 | 1 | 0 |
| enkephalin, leucine | Homo sapiens (human) | Ki | 0.0062 | 7 | 9 |
| cannabidiol | Homo sapiens (human) | Ki | 6.4000 | 1 | 1 |
| tyrosyl-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-phenylalanyl-phenylalanine | Homo sapiens (human) | Ki | 0.0036 | 2 | 4 |
| tamoxifen | Homo sapiens (human) | IC50 | 13.3390 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 4.7020 | 1 | 0 |
| mitragynine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| mitragynine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| u-50488 | Homo sapiens (human) | Ki | 6.5800 | 5 | 8 |
| paynantheine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| paynantheine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| metazocine | Homo sapiens (human) | Ki | 0.1400 | 1 | 1 |
| dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0098 | 1 | 1 |
| ici 199441 | Homo sapiens (human) | Ki | 0.0240 | 2 | 2 |
| dynorphin (1-11) | Homo sapiens (human) | IC50 | 0.2840 | 1 | 1 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | IC50 | 32.0000 | 2 | 2 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0880 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 4.7950 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 1.6900 | 1 | 0 |
| amentoflavone | Homo sapiens (human) | Ki | 0.0362 | 2 | 2 |
| flunarizine hydrochloride | Homo sapiens (human) | IC50 | 3.6300 | 1 | 1 |
| codeine | Homo sapiens (human) | IC50 | 9.3000 | 1 | 1 |
| codeine | Homo sapiens (human) | Ki | 52.2070 | 1 | 1 |
| hydromorphone | Homo sapiens (human) | Ki | 0.0380 | 1 | 1 |
| nalmefene | Homo sapiens (human) | Ki | 0.0130 | 4 | 4 |
| nalorphine | Homo sapiens (human) | Ki | 0.1200 | 1 | 1 |
| naloxone | Homo sapiens (human) | IC50 | 0.1896 | 14 | 13 |
| naloxone | Homo sapiens (human) | Ki | 0.1315 | 22 | 23 |
| oxymorphone | Homo sapiens (human) | Ki | 0.1075 | 2 | 2 |
| morphine | Homo sapiens (human) | IC50 | 0.1199 | 5 | 5 |
| morphine | Homo sapiens (human) | Ki | 0.2700 | 28 | 35 |
| 7-benzylidenenaltrexone | Homo sapiens (human) | Ki | 0.0056 | 4 | 4 |
| alpha-neoendorphin | Homo sapiens (human) | Ki | 0.0017 | 1 | 1 |
| beta-funaltrexamine | Homo sapiens (human) | Ki | 0.0278 | 2 | 2 |
| endomorphin 1 | Homo sapiens (human) | Ki | 2.8685 | 6 | 8 |
| endomorphin 2 | Homo sapiens (human) | Ki | 3.4030 | 5 | 7 |
| j 113397 | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| j 113397 | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
| l 745870 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nalbuphine | Homo sapiens (human) | IC50 | 1.1195 | 2 | 1 |
| nalbuphine | Homo sapiens (human) | Ki | 0.4950 | 3 | 2 |
| n-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide | Homo sapiens (human) | Ki | 8.6471 | 2 | 2 |
| 5,7-dihydroxy-4',6-dimethoxyflavone | Homo sapiens (human) | Ki | 8.4000 | 1 | 1 |
| oxiconazole | Homo sapiens (human) | IC50 | 5.3081 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 1.8712 | 1 | 0 |
| levorphanol | Homo sapiens (human) | IC50 | 0.0040 | 2 | 2 |
| levorphanol | Homo sapiens (human) | Ki | 0.0042 | 7 | 8 |
| cyclorphan | Homo sapiens (human) | Ki | 0.0019 | 9 | 10 |
| naltrexone | Homo sapiens (human) | IC50 | 0.0319 | 10 | 14 |
| naltrexone | Homo sapiens (human) | Ki | 0.0290 | 39 | 44 |
| butorphanol | Homo sapiens (human) | Ki | 0.0120 | 3 | 3 |
| methylnaltrexone | Homo sapiens (human) | Ki | 1.9776 | 2 | 2 |
| n-methylnaltrindole | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | IC50 | 0.0014 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | Ki | 1.7040 | 12 | 12 |
| naloxone hydrochloride | Homo sapiens (human) | IC50 | 0.0049 | 2 | 2 |
| norbinaltorphimine | Homo sapiens (human) | IC50 | 0.0240 | 2 | 2 |
| norbinaltorphimine | Homo sapiens (human) | Ki | 0.0165 | 23 | 28 |
| dermorphin | Homo sapiens (human) | IC50 | 0.2492 | 4 | 4 |
| dermorphin | Homo sapiens (human) | Ki | 0.9290 | 1 | 1 |
| naltrexone hydrochloride | Homo sapiens (human) | IC50 | 0.0006 | 2 | 2 |
| 6 beta-hydroxynaltrexone | Homo sapiens (human) | IC50 | 0.0199 | 4 | 12 |
| 6 beta-hydroxynaltrexone | Homo sapiens (human) | Ki | 0.0530 | 1 | 1 |
| enkephalinamide-leu, ala(2)- | Homo sapiens (human) | Ki | 0.0042 | 2 | 3 |
| 14-methoxymetopon | Homo sapiens (human) | Ki | 0.0166 | 2 | 2 |
| biphalin | Homo sapiens (human) | IC50 | 0.0022 | 4 | 4 |
| biphalin | Homo sapiens (human) | Ki | 0.0027 | 11 | 11 |
| alvimopan anhydrous | Homo sapiens (human) | Ki | 0.0085 | 2 | 2 |
| sinococuline | Homo sapiens (human) | IC50 | 37.0000 | 1 | 1 |
| tyrosyl alanyl-glycyl-phenylalaninamide | Homo sapiens (human) | IC50 | 0.7419 | 4 | 4 |
| tyrosyl alanyl-glycyl-phenylalaninamide | Homo sapiens (human) | Ki | 0.2505 | 5 | 6 |
| oxymorphindole | Homo sapiens (human) | Ki | 0.0011 | 2 | 2 |
| naltrindole | Homo sapiens (human) | IC50 | 0.0006 | 3 | 3 |
| naltrindole | Homo sapiens (human) | Ki | 0.0013 | 27 | 31 |
| 7-benzylidenenaltrexone | Homo sapiens (human) | Ki | 0.0028 | 2 | 2 |
| trk 820 | Homo sapiens (human) | Ki | 0.0365 | 1 | 1 |
| gw 1929 | Homo sapiens (human) | IC50 | 3.2090 | 1 | 0 |
| gw 1929 | Homo sapiens (human) | Ki | 1.1310 | 1 | 0 |
| clocinnamox | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| clocinnamox | Homo sapiens (human) | Ki | 0.0025 | 6 | 6 |
| gr 103545 | Homo sapiens (human) | Ki | 0.4220 | 1 | 1 |
| enkephalin, leucine-2-alanine | Homo sapiens (human) | Ki | 0.0059 | 2 | 3 |
| nalfurafine hydrochloride | Homo sapiens (human) | Ki | 0.6930 | 1 | 1 |
| naloxonazine | Homo sapiens (human) | IC50 | 0.1360 | 1 | 0 |
| naloxonazine | Homo sapiens (human) | Ki | 0.0480 | 1 | 0 |
| sodium selenate | Homo sapiens (human) | Ki | 0.0056 | 15 | 16 |
| ggti 298 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| o-demethyltramadol | Homo sapiens (human) | Ki | 6.4500 | 2 | 2 |
| ro 64-6198 | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
| ggti 2147 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| ly 255582 | Homo sapiens (human) | Ki | 0.0268 | 6 | 8 |
| deltorphin ii, ala(2)- | Homo sapiens (human) | Ki | 0.0013 | 1 | 1 |
| sb-612111 | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
| deltorphin i, ala(2)- | Homo sapiens (human) | IC50 | 0.0009 | 2 | 2 |
| deltorphin i, ala(2)- | Homo sapiens (human) | Ki | 0.0017 | 1 | 1 |
| 8-carboxamidocyclazocine | Homo sapiens (human) | Ki | 0.0067 | 5 | 6 |
| akuammicine | Homo sapiens (human) | Ki | 24.1594 | 1 | 2 |
| 6-deoxy-6-fluoronaltrexone | Homo sapiens (human) | IC50 | 0.0079 | 1 | 1 |
| dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0085 | 1 | 1 |
| dynorphin a (1-11)-amide | Homo sapiens (human) | IC50 | 0.0177 | 2 | 4 |
| dynorphin a (1-11)-amide | Homo sapiens (human) | Ki | 0.0031 | 3 | 3 |
| h-dmt-tic-gly-nh-bzl | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| mesyl salvinorin b | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| adl 5859 | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| 9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester | Homo sapiens (human) | Ki | 1.1700 | 3 | 3 |
| salvinorin b | Homo sapiens (human) | Ki | 10.0000 | 3 | 3 |
| way 207024 | Homo sapiens (human) | Ki | 0.5500 | 1 | 1 |
| 14-o-methyloxymorphone | Homo sapiens (human) | Ki | 0.0088 | 1 | 1 |
| mitragynine, (3beta,16e,20beta)-isomer | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| mitragynine, (3beta,16e,20beta)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| mitragynine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| mitragynine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| grandisine d | Homo sapiens (human) | IC50 | 1.6500 | 1 | 1 |
| morphine sulfate | Homo sapiens (human) | IC50 | 0.1330 | 2 | 2 |
| nociceptin | Homo sapiens (human) | Ki | 3.3077 | 6 | 6 |
| dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0059 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 1-(1-(1-methylcyclooctyl)-4-piperidinyl)-2-((3r)-3-piperidinyl)-1h-benzimidazole | Homo sapiens (human) | Ki | 0.6670 | 1 | 1 |
| salvinorin b ethoxymethyl ether | Homo sapiens (human) | Ki | 1.0170 | 1 | 1 |
| dynorphins | Homo sapiens (human) | Ki | 0.0115 | 5 | 9 |
| ly2456302 | Homo sapiens (human) | Ki | 0.1440 | 2 | 2 |
| ici 174865 | Homo sapiens (human) | IC50 | 0.0830 | 1 | 1 |
| ici 174865 | Homo sapiens (human) | Ki | 0.0191 | 1 | 1 |
| 7-hydroxymitragynine | Homo sapiens (human) | Ki | 0.2360 | 1 | 1 |
| mitragynine pseudoindoxyl | Homo sapiens (human) | IC50 | 0.0015 | 2 | 2 |
| mitragynine pseudoindoxyl | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| 7-spiroindanyloxymorphone | Homo sapiens (human) | Ki | 0.0404 | 4 | 4 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| cj 15,208 | Homo sapiens (human) | IC50 | 2.6000 | 1 | 1 |
| cj 15,208 | Homo sapiens (human) | Ki | 51.0000 | 2 | 2 |
| 4-[[(4-ethylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| LSM-2536 | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| a-1155463 | Homo sapiens (human) | Ki | 2.1249 | 2 | 0 |
| 3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 22-thiocyanatosalvinorin a | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| loperamide | Homo sapiens (human) | EC50 | 0.1560 | 1 | 1 |
| pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| propranolol | Homo sapiens (human) | EC50 | 5.0119 | 1 | 1 |
| suramin | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| adenosine diphosphate | Homo sapiens (human) | EC50 | 11.0000 | 1 | 1 |
| alpha,beta-methyleneadenosine 5'-triphosphate | Homo sapiens (human) | EC50 | 8.0000 | 1 | 1 |
| enkephalin, d-penicillamine (2,5)- | Homo sapiens (human) | EC50 | 0.0104 | 9 | 10 |
| enkephalin, d-penicillamine (2,5)- | Homo sapiens (human) | Kd | 0.0005 | 3 | 3 |
| u 69593 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| u 69593 | Homo sapiens (human) | Kd | 1.9800 | 2 | 2 |
| bw 373u86 | Homo sapiens (human) | EC50 | 0.0003 | 2 | 2 |
| met-enkephalinamide | Homo sapiens (human) | EC50 | 0.3000 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | EC50 | 0.0667 | 16 | 16 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | Kd | 0.6290 | 1 | 1 |
| salvinorin a | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| asimadoline | Homo sapiens (human) | EC50 | 8.0000 | 1 | 1 |
| adenosine 5'-o-(3-thiotriphosphate) | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
| enkephalin, methionine | Homo sapiens (human) | EC50 | 0.0164 | 3 | 3 |
| enkephalin, leucine | Homo sapiens (human) | EC50 | 0.0246 | 7 | 8 |
| 4-methyl-N-[1-[2-(1-pyrrolidinyl)ethyl]-2-benzimidazolyl]benzamide | Homo sapiens (human) | EC50 | 7.8000 | 1 | 1 |
| nalmefene | Homo sapiens (human) | Kd | 0.0009 | 1 | 1 |
| naloxone | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
| oxycodone | Homo sapiens (human) | EC50 | 4.0000 | 1 | 1 |
| morphine | Homo sapiens (human) | EC50 | 0.3714 | 7 | 7 |
| 2-methylthio-atp | Homo sapiens (human) | EC50 | 0.6000 | 1 | 1 |
| endomorphin 1 | Homo sapiens (human) | EC50 | 0.9320 | 1 | 1 |
| endomorphin 2 | Homo sapiens (human) | EC50 | 1.0000 | 2 | 2 |
| dihydromorphine | Homo sapiens (human) | Kd | 0.8300 | 1 | 1 |
| naltrexone | Homo sapiens (human) | EC50 | 0.0091 | 4 | 4 |
| naltrexone | Homo sapiens (human) | Kd | 0.0016 | 1 | 1 |
| methylnaltrexone | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | EC50 | 3.4690 | 3 | 3 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | Kd | 0.7404 | 5 | 5 |
| norbinaltorphimine | Homo sapiens (human) | EC50 | 0.3800 | 1 | 1 |
| biphalin | Homo sapiens (human) | EC50 | 0.0012 | 12 | 19 |
| tyrosyl alanyl-glycyl-phenylalaninamide | Homo sapiens (human) | EC50 | 0.1903 | 2 | 4 |
| naltrindole | Homo sapiens (human) | EC50 | 0.0001 | 1 | 1 |
| naltrindole | Homo sapiens (human) | Kd | 0.0112 | 1 | 1 |
| cyprodime | Homo sapiens (human) | EC50 | 1.1050 | 1 | 1 |
| trk 820 | Homo sapiens (human) | EC50 | 0.0741 | 1 | 1 |
| enkephalin, leucine-2-alanine | Homo sapiens (human) | EC50 | 0.4781 | 3 | 3 |
| enkephalin, leucine-2-alanine | Homo sapiens (human) | Kd | 0.6250 | 1 | 1 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Homo sapiens (human) | Kd | 0.0155 | 1 | 1 |
| sincalide | Homo sapiens (human) | Kd | 0.0013 | 1 | 1 |
| tan 67 | Homo sapiens (human) | EC50 | 0.0009 | 3 | 3 |
| deltorphin ii, ala(2)- | Homo sapiens (human) | EC50 | 0.0095 | 2 | 2 |
| deltorphin i, ala(2)- | Homo sapiens (human) | EC50 | 0.0016 | 3 | 3 |
| eluxadoline | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| adl 5859 | Homo sapiens (human) | EC50 | 0.0200 | 1 | 1 |
| 9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| 14-o-methyloxymorphone | Homo sapiens (human) | EC50 | 0.0373 | 1 | 1 |
| dynorphin (1-17) | Homo sapiens (human) | EC50 | 0.0186 | 1 | 1 |
| cym51010 | Homo sapiens (human) | EC50 | 3.0553 | 3 | 3 |
| 1-(1-(1-methylcyclooctyl)-4-piperidinyl)-2-((3r)-3-piperidinyl)-1h-benzimidazole | Homo sapiens (human) | EC50 | 4.6960 | 1 | 1 |
| dynorphins | Homo sapiens (human) | EC50 | 0.0186 | 2 | 2 |
| ici 174865 | Homo sapiens (human) | EC50 | 0.1160 | 1 | 1 |
| mitragynine pseudoindoxyl | Homo sapiens (human) | EC50 | 0.0017 | 2 | 2 |
| trv130 | Homo sapiens (human) | EC50 | 6.4000 | 2 | 2 |
Drugs with Other Measurements
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New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward δ and κ opioid receptors.Bioorganic & medicinal chemistry, , 01-01, Volume: 53, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Identification of an Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
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An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Discovery of Potent and Selective Agonists of δ Opioid Receptor by Revisiting the "Message-Address" Concept.ACS medicinal chemistry letters, , Apr-14, Volume: 7, Issue:4, 2016
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
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A selective delta opioid receptor antagonist based on a stilbene core.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 25, Issue:23, 2015
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
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.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Further studies of tyrosine surrogates in opioid receptor peptide ligands.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
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.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
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Probes for narcotic receptor mediated phenomena. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation.European journal of medicinal chemistry, , Volume: 67, 2013
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.European journal of medicinal chemistry, , Volume: 50, 2012
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
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Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
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.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
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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.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
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New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Novel delta opioid receptor agonists with oxazatricyclodecane structure.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
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Syntheses of novel high affinity ligands for opioid receptors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.Bioorganic & medicinal chemistry letters, , May-15, Volume: 19, Issue:10, 2009
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Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
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N,N-dialkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, potent, selective delta opioid agonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
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.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
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Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
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Semisynthetic neoclerodanes as kappa opioid receptor probes.Bioorganic & medicinal chemistry, , May-01, Volume: 20, Issue:9, 2012
Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.Journal of natural products, , Apr-25, Volume: 74, Issue:4, 2011
Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Herkinorin analogues with differential beta-arrestin-2 interactions.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Synthesis of salvinorin A analogues as opioid receptor probes.Journal of natural products, , Volume: 69, Issue:6, 2006
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1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.ACS medicinal chemistry letters, , Oct-14, Volume: 1, Issue:7, 2010
Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.Journal of medicinal chemistry, , Nov-12, Volume: 58, Issue:21, 2015
Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.Bioorganic & medicinal chemistry letters, , May-15, Volume: 19, Issue:10, 2009
Further studies of tyrosine surrogates in opioid receptor peptide ligands.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Isolation and Pharmacological Characterization of Six Opioidergic Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands.RSC medicinal chemistry, , Nov-17, Volume: 12, Issue:11, 2021
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
[no title available]Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Applications of amide isosteres in medicinal chemistry.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 29, Issue:18, 2019
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Structure-activity relationships of dynorphin a analogues modified in the address sequence.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Peptides as receptor selectivity modulators of opiate pharmacophores.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
Extended TIP(P) analogues as precursors for labeled delta-opioid receptor ligands.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.Journal of medicinal chemistry, , Aug-07, Volume: 35, Issue:16, 1992
Selective reversible and irreversible ligands for the kappa opioid receptor.Journal of medicinal chemistry, , Jun-12, Volume: 35, Issue:12, 1992
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 18, Issue:12, 2008
Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.Bioorganic & medicinal chemistry, , Jul-15, Volume: 23, Issue:14, 2015
Antagonists of the kappa opioid receptor.Bioorganic & medicinal chemistry letters, , May-01, Volume: 24, Issue:9, 2014
Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.Bioorganic & medicinal chemistry, , Sep-15, Volume: 17, Issue:18, 2009
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
[no title available]Journal of natural products, , 03-26, Volume: 84, Issue:3, 2021
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
[no title available]Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors.Journal of natural products, , Jun-26, Volume: 78, Issue:6, 2015
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Habbemines A and B, pyrrolidine alkaloids with human delta-opioid receptor binding affinity from the leaves of Elaeocarpus habbemensis.Journal of natural products, , Volume: 70, Issue:5, 2007
Indolizidine alkaloids with delta-opioid receptor binding affinity from the leaves of Elaeocarpus fuscoides.Journal of natural products, , Volume: 70, Issue:5, 2007
Alkaloids with human delta-opioid receptor binding affinity from the Australian rainforest tree Peripentadenia mearsii.Journal of natural products, , Volume: 70, Issue:12, 2007
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis.Journal of natural products, , Volume: 69, Issue:9, 2006
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Structure-activity relationships of dynorphin a analogues modified in the address sequence.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.Journal of medicinal chemistry, , Oct-11, Volume: 44, Issue:21, 2001
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.Bioorganic & medicinal chemistry letters, , Mar-20, Volume: 10, Issue:6, 2000
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[no title available],
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The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
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Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
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Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.Journal of medicinal chemistry, , May-01, Volume: 35, Issue:9, 1992
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Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
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Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.Journal of medicinal chemistry, , Volume: 30, Issue:9, 1987
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Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
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A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).Journal of medicinal chemistry, , Jul-12, Volume: 55, Issue:13, 2012
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Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.Bioorganic & medicinal chemistry, , Nov-01, Volume: 20, Issue:21, 2012
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
[no title available]European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.Bioorganic & medicinal chemistry, , Apr-01, Volume: 22, Issue:7, 2014
Structural and biological exploration of phe(3)-phe(4)-modified endomorphin-2 peptidomimetics.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
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Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
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Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
Syntheses of novel high affinity ligands for opioid receptors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
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[no title available],
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
High-affinity carbamate analogues of morphinan at opioid receptors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Aminothiazolomorphinans with mixed κ and μ opioid activity.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 15, Issue:12, 2007
High-affinity carbamate analogues of morphinan at opioid receptors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.ACS medicinal chemistry letters, , Dec-12, Volume: 10, Issue:12, 2019
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Tetrahydroquinoline derivatives as opioid receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.ACS medicinal chemistry letters, , Oct-14, Volume: 1, Issue:7, 2010
14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.Bioorganic & medicinal chemistry, , Sep-15, Volume: 17, Issue:18, 2009
Syntheses of novel high affinity ligands for opioid receptors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.Journal of natural products, , Volume: 70, Issue:8, 2007
Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 17, Issue:19, 2007
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.Journal of medicinal chemistry, , Oct-05, Volume: 49, Issue:20, 2006
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.Journal of medicinal chemistry, , Aug-24, Volume: 49, Issue:17, 2006
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 15, Issue:8, 2005
N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.Journal of medicinal chemistry, , Dec-09, Volume: 37, Issue:25, 1994
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Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
Peptides as receptor selectivity modulators of opiate pharmacophores.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
[no title available],
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Rational Design, Chemical Syntheses, and Biological Evaluations of Peripherally Selective Mu Opioid Receptor Ligands as Potential Opioid Induced Constipation Treatment.Journal of medicinal chemistry, , 03-24, Volume: 65, Issue:6, 2022
Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of μ-opioid receptor antagonists.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 27, Issue:13, 2017
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.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Structural Requirements for CNS Active Opioid Glycopeptides.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
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.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Probes for narcotic receptor mediated phenomena. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation.European journal of medicinal chemistry, , Volume: 67, 2013
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.European journal of medicinal chemistry, , Volume: 50, 2012
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
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.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
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.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
New scaffolds in the development of mu opioid-receptor ligands.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
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Structure-activity relationships of dynorphin a analogues modified in the address sequence.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Herkinorin analogues with differential beta-arrestin-2 interactions.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Synthesis of salvinorin A analogues as opioid receptor probes.Journal of natural products, , Volume: 69, Issue:6, 2006
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
Herkinorin analogues with differential beta-arrestin-2 interactions.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists.Journal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.Journal of medicinal chemistry, , Oct-11, Volume: 44, Issue:21, 2001
4-(p-Bromophenyl)-4-(dimethylamino)-1-phenethylcyclohexanol, an extremely potent respresentative of a new analgesic series.Journal of medicinal chemistry, , Volume: 22, Issue:10, 1979
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent aJournal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
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.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 18, Issue:12, 2008
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
Structure-Activity Relationships of [des-ArgJournal of medicinal chemistry, , 11-23, Volume: 59, Issue:22, 2016
Effect of anchoring 4-anilidopiperidines to opioid peptides.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.Journal of medicinal chemistry, , Apr-11, Volume: 40, Issue:8, 1997
Modification of the enkephalin "message" with an artificial polycationic C-terminus.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
[no title available]ACS medicinal chemistry letters, , Jul-13, Volume: 8, Issue:7, 2017
Development of κ opioid receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
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).Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled opioid receptor activity | molecular function | Combining with an opioid (any narcotic derived from or resembling opium), and transmitting the signal across the membrane by activating an associated G-protein. [GOC:ai, GOC:bf, PMID:20494127] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| receptor serine/threonine kinase binding | molecular function | Binding to a receptor that possesses protein serine/threonine kinase activity. [GOC:mah] |
| G protein-coupled enkephalin receptor activity | molecular function | Combining with an enkephalin, and transmitting the signal across the membrane by activating an associated G-protein. A enkephalin is a pentapeptide (Tyr-Gly-Gly-Phe-Met or Tyr-Gly-Gly-Phe-Leu) involved in regulating nociception in the body. [GOC:bf, Wikipedia:Enkephalin] |
| neuropeptide binding | molecular function | Interacting selectively and non-covalently and stoichiometrically with neuropeptides, peptides with direct synaptic effects (peptide neurotransmitters) or indirect modulatory effects on the nervous system (peptide neuromodulators). [http://www.wormbook.org/chapters/www_neuropeptides/neuropeptides.html] |
Located In
This protein is located in 8 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| synaptic vesicle membrane | cellular component | The lipid bilayer surrounding a synaptic vesicle. [GOC:mah] |
| dendrite membrane | cellular component | The portion of the plasma membrane surrounding a dendrite. [GOC:mah] |
| presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
| axon terminus | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl] |
| spine apparatus | cellular component | A specialization of the endomembrane system found in some classes of dendritic spines consisting of two or more closely apposed lamellae with interspersed electron dense material. The endomembrane component is continuous with the smooth endoplasmic reticulum. [NIF_Subcellular:sao725931194, PMID:20400711, PMID:8987748] |
| postsynaptic density membrane | cellular component | The membrane component of the postsynaptic density. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
| neuronal dense core vesicle | cellular component | A dense core vesicle (granule) that is part of a neuron. These vesicles typically contain neuropeptides. They can be found in all parts of neurons, including the soma, dendrites, axonal swellings (varicosities) and synaptic terminals. [GOC:dos, ISBN:978-0-07-181001-2, Wikipedia:Neuropeptide&oldid=713905176] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Involved In
This protein is involved in 19 target(s):
| Target | Category | Definition |
|---|
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| adult locomotory behavior | biological process | Locomotory behavior in a fully developed and mature organism. [GOC:ai] |
| negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| negative regulation of protein-containing complex assembly | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of protein complex assembly. [GOC:mah] |
| positive regulation of CREB transcription factor activity | biological process | Any process that activates or increases the frequency, rate or extent of activity of the transcription factor CREB. [GOC:dph, GOC:ecd, GOC:tb] |
| positive regulation of peptidyl-serine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-serine. [GOC:mah] |
| response to nicotine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nicotine stimulus. [GOC:bf, GOC:ef, ISBN:0198506732, ISBN:0582227089] |
| G protein-coupled opioid receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by an opioid binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:bf, PMID:20494127] |
| eating behavior | biological process | The specific behavior of an organism relating to the intake of food, any substance (usually solid) that can be metabolized by an organism to give energy and build tissue. [GOC:jl, GOC:pr, PMID:19361967] |
| regulation of mitochondrial membrane potential | biological process | Any process that modulates the establishment or extent of the mitochondrial membrane potential, the electric potential existing across the mitochondrial membrane arising from charges in the membrane itself and from the charges present in the media on either side of the membrane. [GOC:ai] |
| regulation of calcium ion transport | biological process | Any process that modulates the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| cellular response to growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a growth factor stimulus. [GOC:mah] |
| cellular response to hypoxia | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| cellular response to toxic substance | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a toxic stimulus. [GOC:pr] |
| neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |