Page last updated: 2024-08-07 16:34:13
Mu-type opioid receptor
A mu-type opioid receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35372]
Synonyms
M-OR-1;
MOR-1;
Mu opiate receptor;
Mu opioid receptor;
MOP;
hMOP
Research
Bioassay Publications (346)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 6 (1.73) | 18.7374 |
| 1990's | 19 (5.49) | 18.2507 |
| 2000's | 134 (38.73) | 29.6817 |
| 2010's | 149 (43.06) | 24.3611 |
| 2020's | 38 (10.98) | 2.80 |
Compounds (224)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bremazocine | Homo sapiens (human) | IC50 | 0.0008 | 2 | 3 |
| 1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| amiodarone | Homo sapiens (human) | IC50 | 19.0370 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 7.7280 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 1.4920 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.6060 | 1 | 0 |
| bithionol | Homo sapiens (human) | IC50 | 5.5070 | 1 | 0 |
| bithionol | Homo sapiens (human) | Ki | 2.2360 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 14.3970 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 5.8440 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 1.8020 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 0.7310 | 1 | 0 |
| disulfiram | Homo sapiens (human) | IC50 | 3.5110 | 1 | 0 |
| disulfiram | Homo sapiens (human) | Ki | 1.4250 | 1 | 0 |
| domperidone | Homo sapiens (human) | IC50 | 4.2180 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 1.7120 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 5.6930 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 2.3110 | 1 | 0 |
| fentanyl | Homo sapiens (human) | IC50 | 0.0058 | 3 | 3 |
| fentanyl | Homo sapiens (human) | Ki | 0.0030 | 6 | 6 |
| fluphenazine | Homo sapiens (human) | IC50 | 20.7450 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 8.4210 | 1 | 0 |
| fluspirilene | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| gr 89696 | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| haloperidol | Homo sapiens (human) | IC50 | 2.4430 | 1 | 0 |
| haloperidol | Homo sapiens (human) | Ki | 4.4873 | 3 | 2 |
| ifenprodil | Homo sapiens (human) | IC50 | 1.0000 | 1 | 2 |
| loperamide | Homo sapiens (human) | IC50 | 0.0014 | 1 | 0 |
| loperamide | Homo sapiens (human) | Ki | 0.0005 | 3 | 2 |
| meperidine | Homo sapiens (human) | IC50 | 13.6050 | 3 | 3 |
| methadone | Homo sapiens (human) | IC50 | 0.0041 | 1 | 1 |
| methadone | Homo sapiens (human) | Ki | 0.0130 | 1 | 1 |
| miconazole | Homo sapiens (human) | IC50 | 6.0590 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 2.4600 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| raloxifene | Homo sapiens (human) | IC50 | 1.1760 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 0.4770 | 1 | 0 |
| ultram | Homo sapiens (human) | IC50 | 7.6000 | 2 | 2 |
| ultram | Homo sapiens (human) | Ki | 1.8000 | 2 | 2 |
| tuaminoheptane | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
| meperidine hydrochloride | Homo sapiens (human) | Ki | 0.9200 | 2 | 2 |
| reserpine | Homo sapiens (human) | IC50 | 4.1520 | 1 | 0 |
| reserpine | Homo sapiens (human) | Ki | 1.6860 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | IC50 | 26.7690 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | Ki | 10.8670 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 3.1130 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | Ki | 1.2640 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| cyproterone acetate | Homo sapiens (human) | IC50 | 2.1830 | 1 | 0 |
| cyproterone acetate | Homo sapiens (human) | Ki | 0.8860 | 1 | 0 |
| normethadone | Homo sapiens (human) | Ki | 0.0359 | 1 | 1 |
| gentian violet | Homo sapiens (human) | IC50 | 2.1450 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.8710 | 1 | 0 |
| etonitazene | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| diphenoxylate | Homo sapiens (human) | Ki | 0.0124 | 1 | 1 |
| pimozide | Homo sapiens (human) | IC50 | 0.3720 | 1 | 1 |
| cyclazocine | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| danazol | Homo sapiens (human) | IC50 | 14.0790 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 5.7150 | 1 | 0 |
| normeperidine | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| penfluridol | Homo sapiens (human) | Ki | 0.8670 | 1 | 1 |
| tramadol | Homo sapiens (human) | Ki | 2.4000 | 1 | 1 |
| mifepristone | Homo sapiens (human) | IC50 | 2.4570 | 1 | 0 |
| mifepristone | Homo sapiens (human) | Ki | 0.9970 | 1 | 0 |
| spiradoline | Homo sapiens (human) | IC50 | 0.2340 | 1 | 0 |
| spiradoline | Homo sapiens (human) | Ki | 0.0950 | 1 | 0 |
| enadoline | Homo sapiens (human) | Ki | 0.0220 | 1 | 1 |
| carfentanil | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| nelfinavir | Homo sapiens (human) | IC50 | 14.4320 | 1 | 0 |
| nelfinavir | Homo sapiens (human) | Ki | 5.8590 | 1 | 0 |
| loperamide hydrochloride | Homo sapiens (human) | IC50 | 0.0015 | 1 | 1 |
| enkephalin, d-penicillamine (2,5)- | Homo sapiens (human) | IC50 | 0.0016 | 1 | 1 |
| enkephalin, d-penicillamine (2,5)- | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| vanoxerine | Homo sapiens (human) | IC50 | 3.5300 | 1 | 1 |
| u 69593 | Homo sapiens (human) | IC50 | 0.1940 | 3 | 4 |
| u 69593 | Homo sapiens (human) | Ki | 2.7538 | 8 | 8 |
| gr 127935 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pd 128907 | Homo sapiens (human) | Ki | 77.9000 | 1 | 1 |
| bw 373u86 | Homo sapiens (human) | IC50 | 0.0021 | 1 | 1 |
| bw 373u86 | Homo sapiens (human) | Ki | 0.2600 | 1 | 1 |
| morphiceptin | Homo sapiens (human) | IC50 | 0.3200 | 1 | 1 |
| morphiceptin | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
| enkephalin-leu, arg(6)- | Homo sapiens (human) | Ki | 0.0406 | 1 | 1 |
| tyrosyl-arginyl-phenylalanyl-lysinamide | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| met-enkephalinamide | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | IC50 | 1.8083 | 3 | 3 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | Ki | 0.8260 | 2 | 2 |
| 4-methoxymethylfentanyl | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| salvinorin a | Homo sapiens (human) | Ki | 5.4156 | 7 | 9 |
| ly 99335, (3r-cis)-isomer | Homo sapiens (human) | Ki | 0.0800 | 1 | 1 |
| ly 106737 | Homo sapiens (human) | IC50 | 0.0016 | 4 | 4 |
| ly 106737 | Homo sapiens (human) | Ki | 0.0018 | 5 | 5 |
| alpha-ergocryptine | Homo sapiens (human) | IC50 | 2.4270 | 1 | 0 |
| alpha-ergocryptine | Homo sapiens (human) | Ki | 0.9850 | 1 | 0 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 7.2650 | 1 | 1 |
| ritonavir | Homo sapiens (human) | IC50 | 65.5420 | 1 | 0 |
| ritonavir | Homo sapiens (human) | Ki | 26.6060 | 1 | 0 |
| saquinavir | Homo sapiens (human) | IC50 | 9.6250 | 1 | 0 |
| saquinavir | Homo sapiens (human) | Ki | 3.9070 | 1 | 0 |
| pentazocine | Homo sapiens (human) | Ki | 0.0039 | 1 | 1 |
| enkephalin, methionine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 1 |
| enkephalin, methionine | Homo sapiens (human) | Ki | 0.0190 | 1 | 1 |
| diprenorphine | Homo sapiens (human) | Ki | 0.0002 | 5 | 5 |
| dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.8500 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.3450 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 5.7780 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 2.3450 | 1 | 0 |
| enkephalin, leucine | Homo sapiens (human) | IC50 | 9.5000 | 1 | 1 |
| enkephalin, leucine | Homo sapiens (human) | Ki | 1.2148 | 3 | 4 |
| cannabidiol | Homo sapiens (human) | Ki | 1.3000 | 1 | 1 |
| tyrosyl-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-phenylalanyl-phenylalanine | Homo sapiens (human) | Ki | 4.5000 | 1 | 1 |
| flunarizine | Homo sapiens (human) | IC50 | 5.2360 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 2.1250 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 2.2720 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.9220 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 17.5940 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 7.1420 | 1 | 0 |
| hirsutine, (16e,20beta)-isomer | Homo sapiens (human) | Ki | 1.0140 | 2 | 2 |
| mitragynine | Homo sapiens (human) | Ki | 0.1850 | 3 | 3 |
| u-50488 | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| paynantheine | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
| paynantheine | Homo sapiens (human) | Ki | 0.4100 | 2 | 2 |
| metazocine | Homo sapiens (human) | Ki | 0.0038 | 1 | 1 |
| ketazocine | Homo sapiens (human) | IC50 | 0.1300 | 1 | 1 |
| dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0238 | 1 | 1 |
| ici 199441 | Homo sapiens (human) | Ki | 0.0530 | 2 | 2 |
| ru 42173 | Homo sapiens (human) | Ki | 130.0000 | 1 | 1 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | IC50 | 24.0000 | 2 | 2 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 0.3060 | 1 | 1 |
| flunarizine hydrochloride | Homo sapiens (human) | IC50 | 2.4100 | 1 | 1 |
| codeine | Homo sapiens (human) | IC50 | 0.1050 | 1 | 1 |
| codeine | Homo sapiens (human) | Ki | 3.5135 | 2 | 2 |
| hydrocodone | Homo sapiens (human) | Ki | 0.0095 | 1 | 1 |
| hydromorphone | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| nalmefene | Homo sapiens (human) | Ki | 0.0006 | 4 | 4 |
| nalorphine | Homo sapiens (human) | Ki | 0.0003 | 2 | 2 |
| naloxone | Homo sapiens (human) | IC50 | 0.0397 | 14 | 14 |
| naloxone | Homo sapiens (human) | Ki | 0.0242 | 25 | 24 |
| oxycodone | Homo sapiens (human) | Ki | 0.0120 | 3 | 3 |
| oxymorphone | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
| morphine | Homo sapiens (human) | IC50 | 0.1220 | 9 | 9 |
| morphine | Homo sapiens (human) | Ki | 0.0041 | 32 | 32 |
| 7-benzylidenenaltrexone | Homo sapiens (human) | Ki | 0.0116 | 3 | 3 |
| alpha-neoendorphin | Homo sapiens (human) | Ki | 0.0073 | 1 | 1 |
| beta-funaltrexamine | Homo sapiens (human) | Ki | 0.0004 | 2 | 2 |
| endomorphin 1 | Homo sapiens (human) | IC50 | 0.0275 | 3 | 3 |
| endomorphin 1 | Homo sapiens (human) | Ki | 0.0158 | 9 | 11 |
| endomorphin 2 | Homo sapiens (human) | Ki | 0.0059 | 7 | 9 |
| j 113397 | Homo sapiens (human) | IC50 | 2.8000 | 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 | 0.0578 | 4 | 3 |
| nalbuphine | Homo sapiens (human) | Ki | 0.0041 | 3 | 2 |
| n-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide | Homo sapiens (human) | IC50 | 1.5070 | 1 | 1 |
| n-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide | Homo sapiens (human) | Ki | 0.1024 | 2 | 2 |
| pd 128907 | Homo sapiens (human) | Ki | 36.6000 | 1 | 1 |
| sb 223412 | Homo sapiens (human) | Ki | 1.8600 | 1 | 1 |
| thebaine | Homo sapiens (human) | Ki | 7.4000 | 1 | 1 |
| sulindac sulfide | Homo sapiens (human) | IC50 | 33.6680 | 1 | 0 |
| sulindac sulfide | Homo sapiens (human) | Ki | 13.6670 | 1 | 0 |
| levorphanol | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| levorphanol | Homo sapiens (human) | Ki | 0.0002 | 6 | 6 |
| levallorphan | Homo sapiens (human) | Ki | 0.0012 | 3 | 3 |
| cyclorphan | Homo sapiens (human) | IC50 | 0.0017 | 6 | 6 |
| cyclorphan | Homo sapiens (human) | Ki | 0.0001 | 8 | 8 |
| naltrexone | Homo sapiens (human) | IC50 | 0.0060 | 15 | 16 |
| naltrexone | Homo sapiens (human) | Ki | 0.0009 | 38 | 39 |
| morphine-6-glucuronide | Homo sapiens (human) | Ki | 0.0380 | 2 | 2 |
| butorphanol | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
| butorphanol | Homo sapiens (human) | Ki | 0.0002 | 3 | 3 |
| methylnaltrexone | Homo sapiens (human) | Ki | 0.0067 | 2 | 2 |
| salutaridine | Homo sapiens (human) | Ki | 34.6000 | 1 | 1 |
| morphinone | Homo sapiens (human) | Ki | 0.1460 | 1 | 1 |
| 6-codeinone | Homo sapiens (human) | Ki | 0.4590 | 1 | 1 |
| oripavine | Homo sapiens (human) | Ki | 0.2860 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | IC50 | 0.0040 | 17 | 17 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | Ki | 0.0612 | 38 | 39 |
| naloxone hydrochloride | Homo sapiens (human) | IC50 | 0.0049 | 2 | 2 |
| norbinaltorphimine | Homo sapiens (human) | IC50 | 0.2120 | 2 | 2 |
| norbinaltorphimine | Homo sapiens (human) | Ki | 0.0325 | 15 | 15 |
| dermorphin | Homo sapiens (human) | IC50 | 0.0018 | 4 | 4 |
| dermorphin | Homo sapiens (human) | Ki | 0.0072 | 3 | 3 |
| naltrexone hydrochloride | Homo sapiens (human) | IC50 | 0.0006 | 2 | 2 |
| 6 beta-hydroxynaltrexone | Homo sapiens (human) | IC50 | 0.0083 | 2 | 5 |
| 6 beta-hydroxynaltrexone | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| 14-methoxymetopon | Homo sapiens (human) | Ki | 0.0001 | 2 | 2 |
| biphalin | Homo sapiens (human) | IC50 | 0.0014 | 2 | 2 |
| biphalin | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| alvimopan anhydrous | Homo sapiens (human) | IC50 | 0.0026 | 2 | 3 |
| alvimopan anhydrous | Homo sapiens (human) | Ki | 0.0004 | 2 | 2 |
| oxymorphindole | Homo sapiens (human) | Ki | 0.2340 | 2 | 2 |
| naltrindole | Homo sapiens (human) | Ki | 0.0234 | 13 | 13 |
| cyprodime | Homo sapiens (human) | Ki | 0.0106 | 1 | 1 |
| 7-benzylidenenaltrexone | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
| trk 820 | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| clocinnamox | Homo sapiens (human) | IC50 | 0.0005 | 1 | 1 |
| clocinnamox | Homo sapiens (human) | Ki | 0.0030 | 4 | 4 |
| gr 103545 | Homo sapiens (human) | Ki | 0.0347 | 1 | 1 |
| nalfurafine hydrochloride | Homo sapiens (human) | Ki | 0.0060 | 1 | 1 |
| naloxonazine | Homo sapiens (human) | IC50 | 0.0072 | 1 | 0 |
| naloxonazine | Homo sapiens (human) | Ki | 0.0025 | 3 | 2 |
| sodium selenate | Homo sapiens (human) | IC50 | 0.0200 | 6 | 6 |
| sodium selenate | Homo sapiens (human) | Ki | 0.0002 | 15 | 15 |
| n-demethylloperamide | Homo sapiens (human) | Ki | 0.0006 | 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 |
| tapentadol | Homo sapiens (human) | Ki | 0.1600 | 1 | 1 |
| o-demethyltramadol | Homo sapiens (human) | IC50 | 0.0470 | 2 | 2 |
| o-demethyltramadol | Homo sapiens (human) | Ki | 0.0109 | 3 | 3 |
| ro 64-6198 | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
| sr 14150 | Homo sapiens (human) | Ki | 0.0299 | 3 | 3 |
| ly 255582 | Homo sapiens (human) | Ki | 0.0001 | 4 | 4 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| sb-612111 | Homo sapiens (human) | Ki | 0.2290 | 2 | 2 |
| deltorphin i, ala(2)- | Homo sapiens (human) | IC50 | 0.2250 | 1 | 1 |
| 8-carboxamidocyclazocine | Homo sapiens (human) | IC50 | 0.0133 | 2 | 2 |
| 8-carboxamidocyclazocine | Homo sapiens (human) | Ki | 0.0003 | 3 | 3 |
| corynoxine b | Homo sapiens (human) | Ki | 0.1098 | 1 | 1 |
| snap 6201 | Homo sapiens (human) | Ki | 4.0000 | 2 | 2 |
| akuammicine | Homo sapiens (human) | Ki | 3.2361 | 1 | 2 |
| 6-deoxy-6-fluoronaltrexone | Homo sapiens (human) | IC50 | 0.0079 | 1 | 1 |
| corynoxine | Homo sapiens (human) | Ki | 0.0164 | 1 | 1 |
| dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0354 | 1 | 1 |
| dynorphin a (1-11)-amide | Homo sapiens (human) | Ki | 0.0063 | 3 | 3 |
| h-dmt-tic-gly-nh-bzl | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| amd 070 | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| mesyl salvinorin b | Homo sapiens (human) | Ki | 6.8200 | 2 | 2 |
| 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 | 0.0120 | 3 | 3 |
| salvinorin b | Homo sapiens (human) | Ki | 10.0000 | 3 | 3 |
| way 207024 | Homo sapiens (human) | Ki | 0.5500 | 1 | 1 |
| cebranopadol | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| 14-o-methyloxymorphone | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| mitragynine, (3beta,16e,20beta)-isomer | Homo sapiens (human) | IC50 | 4.2000 | 1 | 1 |
| mitragynine, (3beta,16e,20beta)-isomer | Homo sapiens (human) | Ki | 0.2230 | 3 | 3 |
| mitragynine | Homo sapiens (human) | IC50 | 5.7000 | 1 | 1 |
| mitragynine | Homo sapiens (human) | Ki | 0.7280 | 2 | 2 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| morphine sulfate | Homo sapiens (human) | IC50 | 0.0125 | 2 | 2 |
| nociceptin | Homo sapiens (human) | Ki | 1.1474 | 5 | 5 |
| dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0094 | 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 | 0.0011 | 1 | 1 |
| salvinorin b ethoxymethyl ether | Homo sapiens (human) | Ki | 0.0410 | 1 | 1 |
| dynorphins | Homo sapiens (human) | Ki | 0.0080 | 1 | 1 |
| ly2456302 | Homo sapiens (human) | Ki | 0.0196 | 2 | 2 |
| e-52862 | Homo sapiens (human) | Ki | 10.0000 | 3 | 3 |
| 7-hydroxymitragynine | Homo sapiens (human) | IC50 | 0.7250 | 1 | 1 |
| 7-hydroxymitragynine | Homo sapiens (human) | Ki | 0.0072 | 1 | 1 |
| mitragynine pseudoindoxyl | Homo sapiens (human) | IC50 | 0.0136 | 3 | 3 |
| mitragynine pseudoindoxyl | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| 7-spiroindanyloxymorphone | Homo sapiens (human) | Ki | 0.0842 | 2 | 2 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| cj 15,208 | Homo sapiens (human) | IC50 | 0.1425 | 2 | 2 |
| cj 15,208 | Homo sapiens (human) | Ki | 0.1285 | 2 | 2 |
| pf-04455242 | Homo sapiens (human) | Ki | 0.0370 | 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 | 2 | 2 |
| trv130 | Homo sapiens (human) | Ki | 0.0037 | 2 | 2 |
| 3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Homo sapiens (human) | Ki | 0.5420 | 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) |
|---|
| fentanyl | Homo sapiens (human) | EC50 | 0.0262 | 4 | 5 |
| haloperidol | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| meperidine | Homo sapiens (human) | EC50 | 9.4000 | 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 |
| ultram | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
| adenosine diphosphate | Homo sapiens (human) | EC50 | 11.0000 | 1 | 1 |
| tramadol | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| sufentanil | Homo sapiens (human) | EC50 | 0.0014 | 2 | 2 |
| carfentanil | Homo sapiens (human) | EC50 | 0.0000 | 1 | 1 |
| alpha,beta-methyleneadenosine 5'-triphosphate | Homo sapiens (human) | EC50 | 8.0000 | 1 | 1 |
| u 69593 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| morphiceptin | Homo sapiens (human) | EC50 | 0.7413 | 1 | 1 |
| met-enkephalinamide | Homo sapiens (human) | EC50 | 0.6300 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | EC50 | 0.0001 | 1 | 1 |
| salvinorin a | Homo sapiens (human) | EC50 | 7.6200 | 3 | 3 |
| 2-phenyl-1,2-benzisothiazol-3-(2h)-one | Homo sapiens (human) | EC50 | 30.0000 | 1 | 0 |
| asimadoline | Homo sapiens (human) | EC50 | 60.0000 | 1 | 1 |
| adenosine 5'-o-(3-thiotriphosphate) | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
| enkephalin, methionine | Homo sapiens (human) | EC50 | 0.6200 | 1 | 1 |
| enkephalin, leucine | Homo sapiens (human) | EC50 | 0.5895 | 5 | 6 |
| 4-methyl-N-[1-[2-(1-pyrrolidinyl)ethyl]-2-benzimidazolyl]benzamide | Homo sapiens (human) | EC50 | 39.0000 | 1 | 1 |
| 4-chloro-N-(4-chloro-2-methylphenyl)-5-dithiazolimine | Homo sapiens (human) | EC50 | 0.1150 | 1 | 0 |
| 3-chloro-N-[3-(4-morpholinyl)propyl]-6-nitro-1-benzothiophene-2-carboxamide | Homo sapiens (human) | EC50 | 0.4880 | 1 | 0 |
| dezocine | Homo sapiens (human) | EC50 | 0.0380 | 1 | 1 |
| mitragynine | Homo sapiens (human) | EC50 | 0.2454 | 4 | 5 |
| u-50488 | Homo sapiens (human) | EC50 | 4.8400 | 1 | 1 |
| metazocine | Homo sapiens (human) | EC50 | 0.0400 | 1 | 1 |
| ketazocine | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| codeine | Homo sapiens (human) | EC50 | 6.1000 | 1 | 1 |
| hydromorphone | Homo sapiens (human) | EC50 | 0.0026 | 1 | 1 |
| nalmefene | Homo sapiens (human) | Kd | 0.0003 | 1 | 1 |
| naloxone | Homo sapiens (human) | Kd | 0.0005 | 3 | 3 |
| oxycodone | Homo sapiens (human) | EC50 | 0.1378 | 4 | 4 |
| oxymorphone | Homo sapiens (human) | EC50 | 0.0078 | 1 | 1 |
| morphine | Homo sapiens (human) | EC50 | 0.1302 | 26 | 27 |
| 2-methylthio-atp | Homo sapiens (human) | EC50 | 0.6000 | 1 | 1 |
| endomorphin 1 | Homo sapiens (human) | EC50 | 0.0208 | 6 | 6 |
| endomorphin 2 | Homo sapiens (human) | EC50 | 0.0202 | 11 | 12 |
| nalbuphine | Homo sapiens (human) | EC50 | 0.0300 | 2 | 2 |
| thebaine | Homo sapiens (human) | EC50 | 5.6000 | 1 | 1 |
| dihydromorphine | Homo sapiens (human) | Kd | 0.8300 | 1 | 1 |
| cyclorphan | Homo sapiens (human) | EC50 | 0.0008 | 7 | 7 |
| naltrexone | Homo sapiens (human) | EC50 | 0.0057 | 3 | 3 |
| naltrexone | Homo sapiens (human) | Kd | 0.0001 | 1 | 1 |
| methylnaltrexone | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| salutaridine | Homo sapiens (human) | EC50 | 32.5000 | 1 | 1 |
| morphinone | Homo sapiens (human) | EC50 | 0.0280 | 1 | 1 |
| 6-codeinone | Homo sapiens (human) | EC50 | 0.2940 | 1 | 1 |
| oripavine | Homo sapiens (human) | EC50 | 0.2770 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | EC50 | 0.0562 | 56 | 58 |
| norbinaltorphimine | Homo sapiens (human) | EC50 | 0.1200 | 1 | 1 |
| dermorphin | Homo sapiens (human) | EC50 | 0.0735 | 3 | 3 |
| 6 beta-hydroxynaltrexone | Homo sapiens (human) | EC50 | 0.0012 | 1 | 1 |
| 14-methoxymetopon | Homo sapiens (human) | EC50 | 0.0033 | 1 | 1 |
| biphalin | Homo sapiens (human) | EC50 | 0.0010 | 1 | 1 |
| naltrindole | Homo sapiens (human) | EC50 | 0.0043 | 1 | 1 |
| cyprodime | Homo sapiens (human) | EC50 | 0.0203 | 1 | 1 |
| trk 820 | Homo sapiens (human) | EC50 | 0.0007 | 1 | 1 |
| enkephalin, leucine-2-alanine | Homo sapiens (human) | EC50 | 0.9364 | 3 | 3 |
| enkephalin, leucine-2-alanine | Homo sapiens (human) | Kd | 0.6250 | 1 | 1 |
| nalfurafine hydrochloride | Homo sapiens (human) | EC50 | 0.0017 | 1 | 1 |
| sodium selenate | Homo sapiens (human) | EC50 | 0.0016 | 7 | 7 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Homo sapiens (human) | Kd | 0.0032 | 1 | 1 |
| tapentadol | Homo sapiens (human) | EC50 | 0.6700 | 1 | 1 |
| o-demethyltramadol | Homo sapiens (human) | EC50 | 0.1800 | 2 | 2 |
| sr 14150 | Homo sapiens (human) | EC50 | 0.0990 | 1 | 1 |
| deltorphin ii, ala(2)- | Homo sapiens (human) | EC50 | 1.9390 | 1 | 1 |
| deltorphin i, ala(2)- | Homo sapiens (human) | EC50 | 1.1300 | 1 | 1 |
| 8-carboxamidocyclazocine | Homo sapiens (human) | EC50 | 0.0032 | 2 | 2 |
| eluxadoline | Homo sapiens (human) | EC50 | 0.0010 | 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 | 0.9880 | 5 | 5 |
| cebranopadol | Homo sapiens (human) | EC50 | 0.0012 | 1 | 1 |
| 14-o-methyloxymorphone | Homo sapiens (human) | EC50 | 0.0026 | 2 | 2 |
| mitragynine, (3beta,16e,20beta)-isomer | Homo sapiens (human) | EC50 | 0.0392 | 1 | 1 |
| dynorphin (1-17) | Homo sapiens (human) | EC50 | 0.2138 | 1 | 1 |
| cym51010 | Homo sapiens (human) | EC50 | 2.3560 | 4 | 4 |
| 1-(1-(1-methylcyclooctyl)-4-piperidinyl)-2-((3r)-3-piperidinyl)-1h-benzimidazole | Homo sapiens (human) | EC50 | 0.0340 | 1 | 1 |
| dynorphins | Homo sapiens (human) | EC50 | 0.2138 | 2 | 2 |
| e-52862 | Homo sapiens (human) | EC50 | 10.0000 | 3 | 3 |
| 7-hydroxymitragynine | Homo sapiens (human) | EC50 | 0.0720 | 3 | 4 |
| mitragynine pseudoindoxyl | Homo sapiens (human) | EC50 | 0.0017 | 2 | 2 |
| trv130 | Homo sapiens (human) | EC50 | 0.0144 | 5 | 6 |
Drugs with Other Measurements
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
Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.Journal of medicinal chemistry, , Volume: 33, Issue:2, 1990
[no title available]European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery.Journal of medicinal chemistry, , 10-27, Volume: 65, Issue:20, 2022
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists.ACS medicinal chemistry letters, , Sep-12, Volume: 10, Issue:9, 2019
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.ACS medicinal chemistry letters, , Nov-14, Volume: 10, Issue:11, 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
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: a new series of hybrid molecules with significant binding affinity for mu-opioid receptors and I2-imidazoline binding sites.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
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
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
[no title available],
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
[no title available],
Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
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
Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics.Journal of medicinal chemistry, , Volume: 23, Issue:9, 1980
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
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
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity.ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Derivatives of tramadol for increased duration of effect.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Emerging molecular approaches to pain therapy.Journal of medicinal chemistry, , May-06, Volume: 42, Issue:9, 1999
Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
Synthesis and biological evaluation of meperidine analogues at monoamine transporters.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.ACS medicinal chemistry letters, , Nov-14, Volume: 10, Issue:11, 2019
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
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
Further studies of tyrosine surrogates in opioid receptor peptide ligands.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
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
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. 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
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
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
Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 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
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
3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
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
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, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
Synthesis and binding affinity of neuropeptide Y at opiate receptors.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Novel delta opioid receptor agonists with oxazatricyclodecane structure.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: the development of diaryl amino piperidines as potent delta opioid receptor agonists with in vivo anti-nociceptive activity in rodent models.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
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
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
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.Journal of medicinal chemistry, , Aug-29, Volume: 40, Issue:18, 1997
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
Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues.Journal of medicinal chemistry, , Dec-26, Volume: 57, Issue:24, 2014
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
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
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: semisynthesis of salvinicins A and B and other chemical transformations of salvinorin A.Journal of natural products, , Volume: 69, Issue:1, 2006
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Effect of the 3- and 4-methyl groups on the opioid receptor properties of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines.Journal of medicinal chemistry, , Apr-10, Volume: 57, Issue:7, 2014
1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.ACS medicinal chemistry letters, , Oct-14, Volume: 1, Issue:7, 2010
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
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
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
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
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
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
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
Further studies of tyrosine surrogates in opioid receptor peptide ligands.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
Synthesis and evaluation of three structurally related ¹⁸F-labeled orvinols of different intrinsic activities: 6-O-[¹⁸F]fluoroethyl-diprenorphine ([¹⁸F]FDPN), 6-O-[¹⁸F]fluoroethyl-buprenorphine ([¹⁸F]FBPN), and 6-O-[¹⁸F]fluoroethyl-phenethyl-orvinol ([¹⁸FJournal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.Journal of medicinal chemistry, , Apr-20, Volume: 43, Issue:8, 2000
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
Structure-activity relationships of dynorphin a analogues modified in the address sequence.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Synthesis and binding affinity of neuropeptide Y at opiate receptors.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
[no title available]Journal of natural products, , 04-23, Volume: 84, Issue:4, 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
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
[no title available]Journal of natural products, , 04-23, Volume: 84, Issue:4, 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
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
Herkinorin analogues with differential beta-arrestin-2 interactions.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]Journal of natural products, , 04-23, Volume: 84, Issue:4, 2021
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
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.The Journal of biological chemistry, , Sep-14, Volume: 282, Issue:37, 2007
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
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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 CRSC medicinal chemistry, , Feb-23, Volume: 13, Issue:2, 2022
[no title available]Journal of natural products, , 03-26, Volume: 84, Issue:3, 2021
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 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
[no title available]Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Opioid Receptor Modulators with a Cinnamyl Group.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 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
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 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
Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 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. 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
Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
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
Probes for narcotic receptor mediated phenomena. 41. Unusual inverse μ-agonists and potent μ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.Journal of medicinal chemistry, , Feb-24, Volume: 54, Issue:4, 2011
Generation of novel radiolabeled opiates through site-selective iodination.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 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
Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
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
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-phenylethylmorphJournal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
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
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
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
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
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
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
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
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.Journal of medicinal chemistry, , Volume: 29, Issue:4, 1986
3-Hydroxy-17-aralkylmorphinans as potential opiate receptor-site-directed alkylating agents.Journal of medicinal chemistry, , Volume: 20, Issue:8, 1977
[no title available],
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
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
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]Journal of natural products, , 04-23, Volume: 84, Issue:4, 2021
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
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
Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist.ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
G-Protein biased opioid agonists: 3-hydroxy-RSC medicinal chemistry, , Aug-01, Volume: 11, Issue:8, 2020
Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 29, Issue:23, 2019
Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 29, Issue:15, 2019
Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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
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
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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
CNS drug design: balancing physicochemical properties for optimal brain exposure.Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
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.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
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
Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
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. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation.European journal of medicinal chemistry, , Volume: 67, 2013
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
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
Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
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
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
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity.ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.Journal of medicinal chemistry, , Feb-24, Volume: 54, Issue:4, 2011
Generation of novel radiolabeled opiates through site-selective iodination.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 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
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.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 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
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
Conformational cross-talk between alpha2A-adrenergic and mu-opioid receptors controls cell signaling.Nature chemical biology, , Volume: 4, Issue:2, 2008
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-phenylethylmorphJournal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.The Journal of biological chemistry, , Sep-14, Volume: 282, Issue:37, 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
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
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
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
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, 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
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
Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics.Journal of medicinal chemistry, , Volume: 23, Issue:9, 1980
Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 24, Issue:10, 2016
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.Journal of medicinal chemistry, , Mar-04, Volume: 37, Issue:5, 1994
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
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
Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery.Journal of medicinal chemistry, , 10-27, Volume: 65, Issue:20, 2022
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.Bioorganic & medicinal chemistry, , 05-01, Volume: 28, Issue:9, 2020
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
Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.Bioorganic & medicinal chemistry, , Nov-01, Volume: 20, Issue:21, 2012
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
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 19, Issue:18, 2009
Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.Bioorganic & medicinal chemistry, , Apr-15, Volume: 16, Issue:8, 2008
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 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
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.Bioorganic & medicinal chemistry, , 05-01, Volume: 28, Issue:9, 2020
[no title available]European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
[no title available]Bioorganic & medicinal chemistry, , 02-15, Volume: 27, Issue:4, 2019
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 of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
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
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
Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 19, Issue:18, 2009
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
New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
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
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay.Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
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
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
[no title available],
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.European journal of medicinal chemistry, , Volume: 46, Issue:4, 2011
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
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
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
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
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
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
Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.ACS medicinal chemistry letters, , Dec-12, Volume: 10, Issue:12, 2019
Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.Bioorganic & medicinal chemistry, , Apr-15, Volume: 23, Issue:8, 2015
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
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
A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.MedChemComm, , May-01, Volume: 4, Issue:5, 2013
Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opioBioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Tetrahydroquinoline derivatives as opioid receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Probes for narcotic receptor mediated phenomena. 41. Unusual inverse μ-agonists and potent μ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.Journal of medicinal chemistry, , Feb-24, Volume: 54, Issue:4, 2011
Generation of novel radiolabeled opiates through site-selective iodination.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 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
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
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 of novel high affinity ligands for opioid receptors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 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
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
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
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 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
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
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 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
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
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
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
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
Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluatiJournal of medicinal chemistry, , Jul-24, Volume: 35, Issue:15, 1992
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
[no title available],
CNS drug design: balancing physicochemical properties for optimal brain exposure.Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
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
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
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 72, 2022
[no title available]European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
[no title available]Journal of natural products, , 04-23, Volume: 84, Issue:4, 2021
Isolation and Pharmacological Characterization of Six Opioidergic Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 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
G-Protein biased opioid agonists: 3-hydroxy-RSC medicinal chemistry, , Aug-01, Volume: 11, Issue:8, 2020
Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
[no title available]Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
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
Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 29, Issue:15, 2019
β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists.ACS medicinal chemistry letters, , Sep-12, Volume: 10, Issue:9, 2019
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 29, Issue:23, 2019
Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 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
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
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
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
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.Bioorganic & medicinal chemistry, , Apr-15, Volume: 23, Issue:8, 2015
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.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Synthesis of tripeptides containing D-Trp substituted at the indole ring, assessment of opioid receptor binding and in vivo central antinociception.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 24, Issue:20, 2014
Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
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
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
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. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation.European journal of medicinal chemistry, , Volume: 67, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potent μ-opioid agonists.Journal of medicinal chemistry, , Apr-11, Volume: 56, Issue:7, 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
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.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
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.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
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.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 22, Issue:24, 2012
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
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
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
Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.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
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixed μ/δ opioid receptor agonistic properties.Journal of medicinal chemistry, , Nov-24, Volume: 54, Issue:22, 2011
Aminothiazolomorphinans with mixed κ and μ opioid activity.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Generation of novel radiolabeled opiates through site-selective iodination.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Evaluation of N-substitution in 6,7-benzomorphan compounds.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
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
Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.Journal of natural products, , May-28, Volume: 73, Issue:5, 2010
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 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
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
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.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Syntheses of novel high affinity ligands for opioid receptors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
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
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.Bioorganic & medicinal chemistry, , May-15, Volume: 16, Issue:10, 2008
Herkinorin analogues with differential beta-arrestin-2 interactions.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
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.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
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-phenylethylmorphJournal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 15, Issue:12, 2007
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
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.The Journal of biological chemistry, , Sep-14, Volume: 282, Issue:37, 2007
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.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
High-affinity carbamate analogues of morphinan at opioid receptors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
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.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
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
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
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
New scaffolds in the development of mu opioid-receptor ligands.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
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
Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 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
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic).Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.Journal of natural products, , Volume: 70, Issue:8, 2007
N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
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
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
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 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
Structure-activity relationships of dynorphin a analogues modified in the address sequence.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
[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
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.Bioorganic & medicinal chemistry letters, , Oct-16, Volume: 10, Issue:20, 2000
Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.Journal of medicinal chemistry, , Apr-20, Volume: 43, Issue:8, 2000
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
[no title available]ACS medicinal chemistry letters, , Nov-09, Volume: 8, Issue:11, 2017
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
Synthesis, biological evaluation, and automated docking of constrained analogues of the opioid peptide H-Dmt-D-Ala-Phe-Gly-NH₂ using the 4- or 5-methyl substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one scaffold.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
An efficient synthesis of 3-OBn-6β,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
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
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
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
Multitarget opioid ligands in pain relief: New players in an old game.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile.ACS medicinal chemistry letters, , Aug-10, Volume: 8, Issue:8, 2017
Synthesis and biological activity of the first cyclic biphalin analogues.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 9, Issue:18, 1999
Opioid Receptor Modulators with a Cinnamyl Group.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
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
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
5'-halogenated analogs of oxymorphindole.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 17, Issue:21, 2007
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
Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 30, Issue:12, 2020
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
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
Synthesis and opioid receptor activity of indolopropellanes.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Syntheses of novel high affinity ligands for opioid receptors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
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
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.Journal of medicinal chemistry, , Dec-16, Volume: 47, Issue:26, 2004
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
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
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
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
4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.Journal of medicinal chemistry, , Mar-04, Volume: 37, Issue:5, 1994
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
Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 59, 2022
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 24, Issue:21, 2014
14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 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
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
(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.European journal of medicinal chemistry, , Apr-15, Volume: 168, 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
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.Journal of medicinal chemistry, , Volume: 29, Issue:4, 1986
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.Journal of medicinal chemistry, , 02-09, Volume: 60, Issue:3, 2017
Discovery of highly selective κ-opioid receptor agonists: 10α-Hydroxy TRK-820 derivatives.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 27, Issue:16, 2017
Multitarget opioid ligands in pain relief: New players in an old game.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
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 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
Aminothiazolomorphinans with mixed κ and μ opioid activity.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
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
Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 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
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 15, Issue:12, 2007
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
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
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
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 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
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
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity.ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Derivatives of tramadol for increased duration of effect.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profilJournal of medicinal chemistry, , Sep-11, Volume: 57, Issue:17, 2014
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
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
N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
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.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.Bioorganic & medicinal chemistry, , May-15, Volume: 16, Issue:10, 2008
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.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
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.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
Structure-Activity Relationships of [des-ArgJournal of medicinal chemistry, , 11-23, Volume: 59, Issue:22, 2016
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
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
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 24, Issue:20, 2014
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
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]Journal of natural products, , 04-23, Volume: 84, Issue:4, 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
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]Journal of natural products, , 04-23, Volume: 84, Issue:4, 2021
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
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
Structure-Activity Relationships of [des-ArgJournal of medicinal chemistry, , 11-23, Volume: 59, Issue:22, 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
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
[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
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
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 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
Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2.Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Progress in the development of more effective and safer analgesics for pain management.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2.Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Orally active opioid compounds from a non-poppy source.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
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
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
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
Antagonists of the kappa opioid receptor.Bioorganic & medicinal chemistry letters, , May-01, Volume: 24, Issue:9, 2014
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
[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 8 target(s):
| Target | Category | Definition |
|---|
| G-protein alpha-subunit binding | molecular function | Binding to a G-protein alpha subunit. The alpha subunit binds a guanine nucleotide. [GOC:hjd] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| beta-endorphin receptor activity | molecular function | Combining with beta-endorphin, and transmitting the signal across the membrane by activating an associated G-protein. Beta-endorphin is a peptide, 31 amino acids long, resulting from processing of the precursor proopiomelanocortin (POMC). [GOC:ai, GOC:bf, Wikipedia:Beta-endorphin] |
| voltage-gated calcium channel activity | molecular function | Enables the transmembrane transfer of a calcium ion by a voltage-gated channel. A voltage-gated channel is a channel whose open state is dependent on the voltage across the membrane in which it is embedded. [GOC:mtg_transport, GOC:tb, ISBN:0815340729] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| morphine receptor activity | molecular function | Combining with morphine (17-methyl-7,8-didehydro-4,5alpha-epoxymorphinan-3,6alpha-diol), and transmitting the signal across the membrane by activating an associated G-protein. [GOC:bf] |
| G-protein beta-subunit binding | molecular function | Binding to a G-protein beta subunit. [GOC:mah] |
| 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 |
|---|
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
| 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] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| perikaryon | cellular component | The portion of the cell soma (neuronal cell body) that excludes the nucleus. [GOC:jl] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
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 16 target(s):
| Target | Category | Definition |
|---|
| 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 acetylcholine receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| 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] |
| sensory perception | biological process | The series of events required for an organism to receive a sensory stimulus, convert it to a molecular signal, and recognize and characterize the signal. This is a neurological process. [GOC:ai, GOC:dph] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| sensory perception of pain | biological process | The series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators] |
| 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] |
| behavioral response to ethanol | biological process | Any process that results in a change in the behavior of an organism as a result of an ethanol stimulus. [GOC:jid] |
| positive regulation of neurogenesis | biological process | Any process that activates or increases the frequency, rate or extent of neurogenesis, the generation of cells within the nervous system. [GOC:ai] |
| negative regulation of Wnt protein secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the controlled release of a Wnt protein from a cell. [GOC:bf, PMID:19223472] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
| calcium ion transmembrane transport | biological process | A process in which a calcium ion is transported from one side of a membrane to the other by means of some agent such as a transporter or pore. [GOC:mah] |
| cellular response to morphine | 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 morphine stimulus. Morphine is an opioid alkaloid, isolated from opium, with a complex ring structure. [GOC:mah] |
| regulation of cellular response to stress | biological process | Any process that modulates the frequency, rate or extent of a cellular response to stress. Cellular response to stress is 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 the organism is under stress. The stress is usually, but not necessarily, exogenous (e.g. temperature, humidity, ionizing radiation). [GOC:dhl] |
| regulation of NMDA receptor activity | biological process | Any process that modulates the frequency, rate or extent of N-methyl-D-aspartate selective glutamate receptor activity. [GOC:BHF] |
| 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] |