Page last updated: 2024-08-07 16:31:31
Mu-type opioid receptor
A mu-type opioid receptor that is encoded in the genome of rat. [OMA:P33535, PRO:DNx]
Synonyms
M-OR-1;
MOR-1;
Opioid receptor B
Research
Bioassay Publications (171)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 20 (11.70) | 18.7374 |
| 1990's | 40 (23.39) | 18.2507 |
| 2000's | 65 (38.01) | 29.6817 |
| 2010's | 38 (22.22) | 24.3611 |
| 2020's | 8 (4.68) | 2.80 |
Compounds (157)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| melatonin | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 1 | 1 |
| acetazolamide | Rattus norvegicus (Norway rat) | Ki | 0.0748 | 4 | 4 |
| aurintricarboxylic acid | Rattus norvegicus (Norway rat) | IC50 | 3.3000 | 1 | 1 |
| verapamil | Rattus norvegicus (Norway rat) | Ki | 1.7500 | 1 | 1 |
| celecoxib | Rattus norvegicus (Norway rat) | Ki | 50.0000 | 1 | 1 |
| dichlorphenamide | Rattus norvegicus (Norway rat) | Ki | 1.2000 | 1 | 1 |
| ethoxzolamide | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| fentanyl | Rattus norvegicus (Norway rat) | IC50 | 0.1888 | 6 | 7 |
| fentanyl | Rattus norvegicus (Norway rat) | Ki | 0.0734 | 5 | 8 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 7.0700 | 2 | 3 |
| hydrochlorothiazide | Rattus norvegicus (Norway rat) | Ki | 0.3280 | 1 | 1 |
| loperamide | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 1 | 1 |
| mafenide | Rattus norvegicus (Norway rat) | Ki | 25.0000 | 1 | 1 |
| methazolamide | Rattus norvegicus (Norway rat) | Ki | 0.0500 | 1 | 1 |
| ondansetron | Rattus norvegicus (Norway rat) | Ki | 2.9000 | 1 | 2 |
| oxybutynin | Rattus norvegicus (Norway rat) | Ki | 0.0008 | 1 | 1 |
| saccharin | Rattus norvegicus (Norway rat) | Ki | 18.5400 | 1 | 1 |
| sodium fluoride | Rattus norvegicus (Norway rat) | Ki | 300,000.0000 | 1 | 1 |
| sodium iodide | Rattus norvegicus (Norway rat) | Ki | 26,000.0000 | 1 | 1 |
| sulfanilamide | Rattus norvegicus (Norway rat) | Ki | 25.0000 | 1 | 1 |
| sulpiride | Rattus norvegicus (Norway rat) | Ki | 1.2000 | 1 | 1 |
| sulthiame | Rattus norvegicus (Norway rat) | Ki | 0.3740 | 1 | 1 |
| zonisamide | Rattus norvegicus (Norway rat) | Ki | 0.0560 | 1 | 1 |
| sulfamic acid | Rattus norvegicus (Norway rat) | Ki | 390.0000 | 1 | 1 |
| 4-toluenesulfonamide | Rattus norvegicus (Norway rat) | Ki | 78.5000 | 1 | 1 |
| 1,3-ditolylguanidine | Rattus norvegicus (Norway rat) | Ki | 3.9500 | 1 | 1 |
| benzenearsonic acid | Rattus norvegicus (Norway rat) | Ki | 49,200.0000 | 1 | 1 |
| fluorodeoxyuridylate | Rattus norvegicus (Norway rat) | Ki | 0.0140 | 1 | 1 |
| carzenide | Rattus norvegicus (Norway rat) | Ki | 0.1640 | 1 | 1 |
| sodium cyanide | Rattus norvegicus (Norway rat) | Ki | 20.0000 | 1 | 1 |
| ketobemidone | Rattus norvegicus (Norway rat) | IC50 | 7.0000 | 1 | 1 |
| sodium carbonate | Rattus norvegicus (Norway rat) | Ki | 73,000.0000 | 1 | 1 |
| Berberine chloride (TN) | Rattus norvegicus (Norway rat) | IC50 | 0.3740 | 1 | 1 |
| etonitazene | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 2 | 3 |
| benzolamide | Rattus norvegicus (Norway rat) | Ki | 0.0150 | 1 | 1 |
| nitroxoline | Rattus norvegicus (Norway rat) | IC50 | 6.0000 | 1 | 1 |
| sodium nitrate | Rattus norvegicus (Norway rat) | Ki | 35,000.0000 | 1 | 1 |
| sodium pyrophosphate | Rattus norvegicus (Norway rat) | Ki | 48,500.0000 | 1 | 1 |
| sodium sulfate | Rattus norvegicus (Norway rat) | Ki | 200,000.0000 | 1 | 1 |
| sodium selenate | Rattus norvegicus (Norway rat) | Ki | 112,000.0000 | 1 | 1 |
| sodium bisulfide | Rattus norvegicus (Norway rat) | Ki | 40.0000 | 1 | 1 |
| sodium azide | Rattus norvegicus (Norway rat) | Ki | 1,510.0000 | 1 | 1 |
| sufentanil | Rattus norvegicus (Norway rat) | IC50 | 0.0014 | 2 | 2 |
| sufentanil | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 1 | 1 |
| alfentanil | Rattus norvegicus (Norway rat) | IC50 | 0.0389 | 1 | 1 |
| alfentanil | Rattus norvegicus (Norway rat) | Ki | 0.0082 | 1 | 1 |
| mirfentanil | Rattus norvegicus (Norway rat) | Ki | 0.0075 | 1 | 2 |
| remifentanil | Rattus norvegicus (Norway rat) | IC50 | 0.0006 | 1 | 1 |
| carfentanil | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 2 | 3 |
| 4-fluorofentanyl | Rattus norvegicus (Norway rat) | IC50 | 0.0005 | 1 | 1 |
| sodium persulfate | Rattus norvegicus (Norway rat) | Ki | 84.0000 | 1 | 1 |
| benzeneboronic acid | Rattus norvegicus (Norway rat) | Ki | 23,100.0000 | 1 | 1 |
| 4-amino-6-chloro-1,3-benzenedisulfonamide | Rattus norvegicus (Norway rat) | Ki | 8.4000 | 1 | 1 |
| dibenzthione | Rattus norvegicus (Norway rat) | IC50 | 27.9000 | 1 | 2 |
| disulphane | Rattus norvegicus (Norway rat) | Ki | 0.1640 | 1 | 1 |
| brinzolamide | Rattus norvegicus (Norway rat) | Ki | 45.0000 | 1 | 1 |
| 2,4-disulfamyl-5-trifluoromethylaniline | Rattus norvegicus (Norway rat) | Ki | 5.8000 | 1 | 1 |
| sulfamide | Rattus norvegicus (Norway rat) | Ki | 1,130.0000 | 1 | 1 |
| 5-amino-1,3,4-thiadiazole-2-sulfonamide | Rattus norvegicus (Norway rat) | Ki | 8.6000 | 1 | 1 |
| nicotine | Rattus norvegicus (Norway rat) | Ki | 0.4400 | 1 | 1 |
| bromodeoxyuridylate | Rattus norvegicus (Norway rat) | Ki | 1.4000 | 1 | 1 |
| enkephalin, d-penicillamine (2,5)- | Rattus norvegicus (Norway rat) | Ki | 0.3053 | 1 | 2 |
| enkephalin, ser(2), leu(5), thr(6)- | Rattus norvegicus (Norway rat) | Ki | 0.0310 | 1 | 1 |
| bw 373u86 | Rattus norvegicus (Norway rat) | IC50 | 0.9346 | 2 | 5 |
| bw 373u86 | Rattus norvegicus (Norway rat) | Ki | 0.0276 | 4 | 5 |
| morphiceptin | Rattus norvegicus (Norway rat) | IC50 | 0.0566 | 1 | 1 |
| morphiceptin | Rattus norvegicus (Norway rat) | Ki | 0.1075 | 2 | 2 |
| valdecoxib | Rattus norvegicus (Norway rat) | Ki | 54.0000 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Rattus norvegicus (Norway rat) | IC50 | 4.7722 | 3 | 6 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Rattus norvegicus (Norway rat) | Ki | 1.5685 | 8 | 13 |
| methotrexate | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 1 | 1 |
| salvinorin a | Rattus norvegicus (Norway rat) | Ki | 7.0000 | 4 | 4 |
| tyrosyl-seryl(o-tert-butyl)-glycyl-phenylalanyl-leucyl-threonine | Rattus norvegicus (Norway rat) | Ki | 0.3740 | 1 | 1 |
| 3,5-bis(trifluoromethyl)benzyl n-acetyltryptophan | Rattus norvegicus (Norway rat) | Ki | 0.0882 | 2 | 3 |
| ly 99335, (3r-cis)-isomer | Rattus norvegicus (Norway rat) | Ki | 0.0800 | 1 | 1 |
| sk&f 83959 | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| ly 106737 | Rattus norvegicus (Norway rat) | Ki | 0.0015 | 1 | 1 |
| 5-nitro-2'-deoxyuridine 5'-monophosphate | Rattus norvegicus (Norway rat) | Ki | 0.0290 | 1 | 1 |
| dexmethylphenidate hydrochloride | Rattus norvegicus (Norway rat) | Ki | 0.2700 | 1 | 1 |
| enkephalin, pen(2,5)-4-chloro-phe(4)- | Rattus norvegicus (Norway rat) | IC50 | 0.6090 | 1 | 1 |
| 5-trifluoromethyl-2'-deoxyuridylic acid | Rattus norvegicus (Norway rat) | Ki | 0.0390 | 1 | 1 |
| 4-(2-aminoethyl)benzenesulfonamide | Rattus norvegicus (Norway rat) | Ki | 21.0000 | 1 | 1 |
| varenicline | Rattus norvegicus (Norway rat) | Ki | 0.3900 | 1 | 1 |
| dizocilpine | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| deltorphin ii, ile(5,6)- | Rattus norvegicus (Norway rat) | Ki | 3.1880 | 1 | 2 |
| n-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide | Rattus norvegicus (Norway rat) | Ki | 0.0310 | 1 | 1 |
| sodium bromide | Rattus norvegicus (Norway rat) | Ki | 63,000.0000 | 1 | 1 |
| enkephalin, methionine | Rattus norvegicus (Norway rat) | IC50 | 0.1290 | 2 | 2 |
| enkephalin, methionine | Rattus norvegicus (Norway rat) | Ki | 0.0238 | 2 | 2 |
| 5-iodo-2'-deoxyuridine 5'-monophosphate | Rattus norvegicus (Norway rat) | Ki | 1.6000 | 1 | 1 |
| enkephalin, leucine | Rattus norvegicus (Norway rat) | Ki | 0.0143 | 3 | 3 |
| sodium thiocyanate | Rattus norvegicus (Norway rat) | Ki | 1,600.0000 | 1 | 1 |
| sodium bicarbonate | Rattus norvegicus (Norway rat) | Ki | 85,000.0000 | 1 | 1 |
| sodium perchlorate | Rattus norvegicus (Norway rat) | Ki | 200,000.0000 | 1 | 1 |
| ditiocarb sodium | Rattus norvegicus (Norway rat) | Ki | 3.1000 | 1 | 1 |
| etorphine | Rattus norvegicus (Norway rat) | IC50 | 0.0001 | 1 | 1 |
| etorphine | Rattus norvegicus (Norway rat) | Ki | 0.2002 | 4 | 5 |
| tyrosyl-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-phenylalanyl-phenylalanine | Rattus norvegicus (Norway rat) | IC50 | 17.6200 | 2 | 5 |
| cocaine hydrochloride | Rattus norvegicus (Norway rat) | Ki | 1.9300 | 1 | 1 |
| deltorphin | Rattus norvegicus (Norway rat) | Ki | 0.3147 | 3 | 5 |
| u-50488 | Rattus norvegicus (Norway rat) | IC50 | 8.7167 | 2 | 3 |
| u-50488 | Rattus norvegicus (Norway rat) | Ki | 1.6012 | 4 | 5 |
| vx-745 | Rattus norvegicus (Norway rat) | IC50 | 0.0008 | 1 | 1 |
| dynorphin (1-11) | Rattus norvegicus (Norway rat) | Ki | 0.0035 | 1 | 1 |
| benzene-1-3-disulfonamide | Rattus norvegicus (Norway rat) | Ki | 0.0790 | 1 | 1 |
| dorzolamide | Rattus norvegicus (Norway rat) | Ki | 50.0000 | 1 | 1 |
| nalorphine | Rattus norvegicus (Norway rat) | IC50 | 0.0040 | 2 | 2 |
| naloxone | Rattus norvegicus (Norway rat) | IC50 | 0.0018 | 3 | 4 |
| naloxone | Rattus norvegicus (Norway rat) | Ki | 0.0018 | 4 | 5 |
| oxycodone | Rattus norvegicus (Norway rat) | Ki | 0.0436 | 1 | 1 |
| oxymorphone | Rattus norvegicus (Norway rat) | Ki | 0.0169 | 4 | 4 |
| topiramate | Rattus norvegicus (Norway rat) | Ki | 0.2500 | 1 | 1 |
| morphine | Rattus norvegicus (Norway rat) | IC50 | 0.0385 | 11 | 13 |
| morphine | Rattus norvegicus (Norway rat) | Ki | 0.0112 | 16 | 26 |
| (2S)-2-(3-oxo-1H-isoindol-2-yl)-3-phenylpropanoic acid | Rattus norvegicus (Norway rat) | IC50 | 200.0000 | 1 | 0 |
| endomorphin 1 | Rattus norvegicus (Norway rat) | IC50 | 0.0005 | 1 | 1 |
| endomorphin 1 | Rattus norvegicus (Norway rat) | Ki | 0.0044 | 11 | 12 |
| endomorphin 2 | Rattus norvegicus (Norway rat) | IC50 | 0.0010 | 1 | 1 |
| endomorphin 2 | Rattus norvegicus (Norway rat) | Ki | 0.0046 | 15 | 16 |
| notopterol | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| levallorphan | Rattus norvegicus (Norway rat) | IC50 | 0.0008 | 1 | 2 |
| naltrexone | Rattus norvegicus (Norway rat) | IC50 | 0.0005 | 2 | 3 |
| naltrexone | Rattus norvegicus (Norway rat) | Ki | 0.0026 | 11 | 16 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Rattus norvegicus (Norway rat) | IC50 | 0.0132 | 4 | 4 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Rattus norvegicus (Norway rat) | Ki | 0.0026 | 11 | 12 |
| norbinaltorphimine | Rattus norvegicus (Norway rat) | Ki | 0.0383 | 8 | 11 |
| nalorphine hydrochloride | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 1 | 1 |
| dermorphin | Rattus norvegicus (Norway rat) | IC50 | 0.0043 | 2 | 2 |
| dermorphin | Rattus norvegicus (Norway rat) | Ki | 0.0007 | 1 | 2 |
| enkephalinamide-leu, ala(2)- | Rattus norvegicus (Norway rat) | Ki | 0.0059 | 2 | 3 |
| 14-methoxymetopon | Rattus norvegicus (Norway rat) | Ki | 0.0001 | 2 | 4 |
| biphalin | Rattus norvegicus (Norway rat) | IC50 | 0.0060 | 1 | 1 |
| biphalin | Rattus norvegicus (Norway rat) | Ki | 0.0016 | 12 | 12 |
| tyrosyl alanyl-glycyl-phenylalaninamide | Rattus norvegicus (Norway rat) | IC50 | 0.0059 | 4 | 4 |
| tyrosyl alanyl-glycyl-phenylalaninamide | Rattus norvegicus (Norway rat) | Ki | 0.0523 | 5 | 6 |
| oxymorphindole | Rattus norvegicus (Norway rat) | Ki | 0.5122 | 2 | 4 |
| naltrindole | Rattus norvegicus (Norway rat) | Ki | 0.0383 | 13 | 17 |
| cyprodime | Rattus norvegicus (Norway rat) | IC50 | 0.0472 | 1 | 2 |
| cyprodime | Rattus norvegicus (Norway rat) | Ki | 0.0107 | 1 | 1 |
| 3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(-)-isomer | Rattus norvegicus (Norway rat) | Ki | 1.3970 | 1 | 1 |
| enkephalin, leucine-2-alanine | Rattus norvegicus (Norway rat) | IC50 | 0.0419 | 1 | 1 |
| enkephalin, leucine-2-alanine | Rattus norvegicus (Norway rat) | Ki | 0.0095 | 3 | 5 |
| cilansetron | Rattus norvegicus (Norway rat) | Ki | 8.5000 | 1 | 2 |
| l 371257 | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| 3-(biphenyl-4-yl)-3-hydroxyquinuclidine | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 1 | 1 |
| spc-839 | Rattus norvegicus (Norway rat) | IC50 | 0.2527 | 2 | 3 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Rattus norvegicus (Norway rat) | Ki | 0.0258 | 6 | 6 |
| o-demethyltramadol | Rattus norvegicus (Norway rat) | Ki | 0.0130 | 1 | 1 |
| ly 255582 | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 2 | 5 |
| 6'-guanidinonaltrindole | Rattus norvegicus (Norway rat) | Ki | 0.0818 | 1 | 2 |
| tan 67 | Rattus norvegicus (Norway rat) | Ki | 0.2841 | 1 | 1 |
| deltorphin ii, ala(2)- | Rattus norvegicus (Norway rat) | Ki | 0.5000 | 1 | 1 |
| deltorphin i, ala(2)- | Rattus norvegicus (Norway rat) | Ki | 0.2499 | 5 | 7 |
| snap 6201 | Rattus norvegicus (Norway rat) | Ki | 4.0000 | 1 | 1 |
| ufp-502 | Rattus norvegicus (Norway rat) | Ki | 0.0005 | 2 | 2 |
| dynorphin a (1-11)-amide | Rattus norvegicus (Norway rat) | Ki | 0.0019 | 3 | 4 |
| h-dmt-tic-gly-nh-bzl | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 2 | 2 |
| eluxadoline | Rattus norvegicus (Norway rat) | Ki | 0.0009 | 1 | 1 |
| adl 5859 | Rattus norvegicus (Norway rat) | IC50 | 78.0000 | 1 | 1 |
| salvinorin b | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| sazetidine-a | Rattus norvegicus (Norway rat) | Ki | 1.9000 | 1 | 1 |
| 14-o-methyloxymorphone | Rattus norvegicus (Norway rat) | Ki | 0.0001 | 1 | 1 |
| somatostatin | Rattus norvegicus (Norway rat) | IC50 | 0.0060 | 1 | 5 |
| 5-chloro-2'-deoxyuridine 5'-triphosphate | Rattus norvegicus (Norway rat) | Ki | 0.1900 | 1 | 1 |
| sodium bisulfite | Rattus norvegicus (Norway rat) | Ki | 89,000.0000 | 1 | 1 |
| sodium nitrite | Rattus norvegicus (Norway rat) | Ki | 63,000.0000 | 1 | 1 |
| sgi 1776 | Rattus norvegicus (Norway rat) | IC50 | 0.3620 | 1 | 1 |
| salvinorin b ethoxymethyl ether | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| dynorphins | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 1 | 1 |
| 7-spiroindanyloxymorphone | Rattus norvegicus (Norway rat) | Ki | 0.0821 | 3 | 3 |
| cj 15,208 | Rattus norvegicus (Norway rat) | Ki | 0.5630 | 3 | 3 |
Drugs with Activation Measurements
Drugs with Other Measurements
Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Discovery of a new family of carbonic anhydrases in the malaria pathogen Plasmodium falciparum--the η-carbonic anhydrases.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 24, Issue:18, 2014
A class of sulfonamides with strong inhibitory action against the α-carbonic anhydrase from Trypanosoma cruzi.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Affinity of fentanyl and its derivatives for the σMedChemComm, , Jul-01, Volume: 10, Issue:7, 2019
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties.Journal of medicinal chemistry, , Volume: 32, Issue:3, 1989
Probes for narcotic receptor mediated phenomena. 12. cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for delta opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity.Journal of medicinal chemistry, , Volume: 29, Issue:6, 1986
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
Synthesis and stereochemistry of 7-phenyl-2-propionanilidobenzo[a]quinolizidine derivatives. Structural probes of fentanyl analgesics.Journal of medicinal chemistry, , Volume: 24, Issue:1, 1981
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Affinity of fentanyl and its derivatives for the σMedChemComm, , Jul-01, Volume: 10, Issue:7, 2019
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
Affinity of fentanyl and its derivatives for the σMedChemComm, , Jul-01, Volume: 10, Issue:7, 2019
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80)Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 2006
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Jul-09, Volume: 11, Issue:13, 2001
4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80)Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective κ-opioid receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.Journal of medicinal chemistry, , Volume: 31, Issue:10, 1988
Preparation and analgesic properties of amino acid derivatives of (-)-5,9 alpha-diethyl-2'-hydroxybenzomorphan.Journal of medicinal chemistry, , Volume: 24, Issue:11, 1981
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Conformationally restricted deltorphin analogues.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective κ-opioid receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Synthesis and evaluation of isothiocyanate-containing derivatives of the delta-opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP) as potential affinity labels for delta-opioid receptors.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors.Journal of medicinal chemistry, , Apr-03, Volume: 35, Issue:7, 1992
Conformationally restricted deltorphin analogues.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
Function of negative charge in the "address domain" of deltorphins.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Evaluation of N-substitution in 6,7-benzomorphan compounds.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists.Journal of medicinal chemistry, , Jun-25, Volume: 36, Issue:13, 1993
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
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
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 10, Issue:8, 2000
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.Bioorganic & medicinal chemistry letters, , Mar-20, Volume: 10, Issue:6, 2000
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties.Journal of medicinal chemistry, , Volume: 32, Issue:3, 1989
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
Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties.Journal of medicinal chemistry, , Volume: 26, Issue:1, 1983
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.Journal of medicinal chemistry, , Volume: 21, Issue:1, 1978
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
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
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.Journal of medicinal chemistry, , Volume: 21, Issue:1, 1978
Discovery of an Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic μ-Opioid Receptor (MOR) Agonist/δ-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.Journal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 2010
Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans.Bioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
Synthesis, conformation, and biological characterization of a sugar derivative of morphine that is a potent, long-lasting, and nontolerant antinociceptive.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Jul-09, Volume: 11, Issue:13, 2001
Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists.Journal of medicinal chemistry, , Jun-25, Volume: 36, Issue:13, 1993
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
3,7-Diazabicyclane: a new narcotic analgesic.Journal of medicinal chemistry, , Volume: 29, Issue:10, 1986
Novel nonnarcotic analgesics with an improved therapeutic ratio. Structure-activity relationships of 8-(methylthio)- and 8-(acylthio)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines.Journal of medicinal chemistry, , Volume: 28, Issue:11, 1985
Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties.Journal of medicinal chemistry, , Volume: 26, Issue:1, 1983
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
Synthesis and stereochemistry of 7-phenyl-2-propionanilidobenzo[a]quinolizidine derivatives. Structural probes of fentanyl analgesics.Journal of medicinal chemistry, , Volume: 24, Issue:1, 1981
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.Journal of medicinal chemistry, , Volume: 21, Issue:1, 1978
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.Journal of medicinal chemistry, , Volume: 21, Issue:5, 1978
N-(2,4,5-Trihydroxyphenehtyl)normetazocine, a potential irreversible inhibitor of the narcotic receptor.Journal of medicinal chemistry, , Volume: 20, Issue:5, 1977
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
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
Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Effect of anchoring 4-anilidopiperidines to opioid peptides.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 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
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
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
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
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
Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation.European journal of medicinal chemistry, , Volume: 68, 2013
The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 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
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 2006
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
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
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
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.Journal of medicinal chemistry, , Volume: 21, Issue:1, 1978
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Chemical space screening around PheBioorganic & medicinal chemistry letters, , 07-15, Volume: 28, Issue:13, 2018
Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Novel cyclic biphalin analogue with improved antinociceptive properties.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation.European journal of medicinal chemistry, , Volume: 68, 2013
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Development of potent μ and δ opioid agonists with high lipophilicity.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Evaluation of N-substitution in 6,7-benzomorphan compounds.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
Function of negative charge in the "address domain" of deltorphins.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
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
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.Journal of medicinal chemistry, , Volume: 30, Issue:5, 1987
Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydronororipavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistryJournal of medicinal chemistry, , Volume: 29, Issue:11, 1986
[no title available]ACS medicinal chemistry letters, , Nov-09, Volume: 8, Issue:11, 2017
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Function of negative charge in the "address domain" of deltorphins.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Novel cyclic biphalin analogue with improved antinociceptive properties.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Effect of anchoring 4-anilidopiperidines to opioid peptides.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Synthesis and biological activity of the first cyclic biphalin analogues.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.Bioorganic & medicinal chemistry, , 12-01, Volume: 51, 2021
Development of potent μ and δ opioid agonists with high lipophilicity.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 20, Issue:14, 2010
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.Journal of medicinal chemistry, , Apr-26, Volume: 44, Issue:9, 2001
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 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-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.Bioorganic & medicinal chemistry letters, , Nov-06, Volume: 10, Issue:21, 2000
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.Journal of medicinal chemistry, , May-06, Volume: 42, Issue:9, 1999
Delta opioid binding selectivity of 3-ether analogs of naltrindole.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 9, Issue:24, 1999
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
Discovery of an Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Function of negative charge in the "address domain" of deltorphins.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
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
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
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
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Conformationally restricted deltorphin analogues.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites.Journal of medicinal chemistry, , Dec-11, Volume: 35, Issue:25, 1992
Function of negative charge in the "address domain" of deltorphins.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.Bioorganic & medicinal chemistry, , Aug-15, Volume: 18, Issue:16, 2010
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.Journal of medicinal chemistry, , Sep-24, Volume: 52, Issue:18, 2009
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Development of κ opioid receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013