Page last updated: 2024-08-07 16:56:16
Mu-type opioid receptor
[no definition available]
Synonyms
M-OR-1;
MOR-1
Research
Bioassay Publications (142)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 7 (4.93) | 18.7374 |
1990's | 36 (25.35) | 18.2507 |
2000's | 60 (42.25) | 29.6817 |
2010's | 37 (26.06) | 24.3611 |
2020's | 2 (1.41) | 2.80 |
Compounds (188)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bremazocine | Cavia porcellus (domestic guinea pig) | IC50 | 0.0018 | 1 | 1 |
acetazolamide | Cavia porcellus (domestic guinea pig) | Ki | 0.1707 | 3 | 3 |
celecoxib | Cavia porcellus (domestic guinea pig) | IC50 | 7.7000 | 1 | 1 |
celecoxib | Cavia porcellus (domestic guinea pig) | Ki | 0.0210 | 1 | 1 |
cgs 15943 | Cavia porcellus (domestic guinea pig) | Ki | 0.0004 | 1 | 1 |
clonidine | Cavia porcellus (domestic guinea pig) | Ki | 0.0141 | 1 | 1 |
dichlorphenamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0380 | 1 | 1 |
ethoxzolamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0080 | 1 | 1 |
fentanyl | Cavia porcellus (domestic guinea pig) | IC50 | 0.0031 | 1 | 2 |
fentanyl | Cavia porcellus (domestic guinea pig) | Ki | 0.0059 | 1 | 1 |
hydrochlorothiazide | Cavia porcellus (domestic guinea pig) | Ki | 0.2900 | 1 | 1 |
ibuprofen | Cavia porcellus (domestic guinea pig) | IC50 | 2.9000 | 1 | 1 |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Cavia porcellus (domestic guinea pig) | IC50 | 1.6000 | 1 | 1 |
mafenide | Cavia porcellus (domestic guinea pig) | Ki | 0.1700 | 1 | 1 |
meperidine | Cavia porcellus (domestic guinea pig) | IC50 | 0.5000 | 1 | 1 |
methazolamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0140 | 1 | 1 |
pentazocine | Cavia porcellus (domestic guinea pig) | Ki | 0.0054 | 1 | 1 |
moxonidine | Cavia porcellus (domestic guinea pig) | Ki | 0.0778 | 1 | 1 |
rofecoxib | Cavia porcellus (domestic guinea pig) | IC50 | 100.0000 | 1 | 1 |
saccharin | Cavia porcellus (domestic guinea pig) | Ki | 5.9590 | 1 | 1 |
sulfanilamide | Cavia porcellus (domestic guinea pig) | Ki | 0.2400 | 1 | 1 |
sulpiride | Cavia porcellus (domestic guinea pig) | Ki | 0.0400 | 1 | 1 |
sulthiame | Cavia porcellus (domestic guinea pig) | Ki | 0.0090 | 1 | 1 |
trimethoprim | Cavia porcellus (domestic guinea pig) | IC50 | 2.8000 | 1 | 1 |
whi p180 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0500 | 1 | 1 |
zonisamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0350 | 1 | 1 |
4-toluenesulfonamide | Cavia porcellus (domestic guinea pig) | Ki | 0.3200 | 1 | 1 |
phenidone | Cavia porcellus (domestic guinea pig) | IC50 | 0.4200 | 1 | 1 |
1,3-ditolylguanidine | Cavia porcellus (domestic guinea pig) | Ki | 0.0710 | 1 | 2 |
carzenide | Cavia porcellus (domestic guinea pig) | Ki | 0.0460 | 1 | 1 |
glycyl-glycyl-glycine | Cavia porcellus (domestic guinea pig) | IC50 | 1,070.0000 | 1 | 1 |
glycylglycine | Cavia porcellus (domestic guinea pig) | IC50 | 820.0000 | 1 | 1 |
Berberine chloride (TN) | Cavia porcellus (domestic guinea pig) | IC50 | 9.2920 | 2 | 2 |
benzolamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0090 | 1 | 1 |
alfentanil | Cavia porcellus (domestic guinea pig) | IC50 | 0.0150 | 1 | 2 |
tolrestat | Cavia porcellus (domestic guinea pig) | IC50 | 0.0300 | 1 | 1 |
piritrexim | Cavia porcellus (domestic guinea pig) | IC50 | 0.0043 | 1 | 1 |
spiradoline | Cavia porcellus (domestic guinea pig) | Ki | 1.6715 | 3 | 8 |
4-amino-6-chloro-1,3-benzenedisulfonamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0750 | 1 | 1 |
disulphane | Cavia porcellus (domestic guinea pig) | Ki | 0.0460 | 1 | 1 |
rilmenidine | Cavia porcellus (domestic guinea pig) | Ki | 0.0831 | 1 | 1 |
brinzolamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0030 | 1 | 1 |
2,4-disulfamyl-5-trifluoromethylaniline | Cavia porcellus (domestic guinea pig) | Ki | 0.0630 | 1 | 1 |
tyrosyltyrosine | Cavia porcellus (domestic guinea pig) | IC50 | 60.0000 | 1 | 1 |
leucylleucine | Cavia porcellus (domestic guinea pig) | IC50 | 170.0000 | 1 | 1 |
rosiglitazone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0380 | 1 | 1 |
5-amino-1,3,4-thiadiazole-2-sulfonamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0600 | 1 | 1 |
phenylalanylphenylalanylamide | Cavia porcellus (domestic guinea pig) | IC50 | 80.0000 | 1 | 1 |
Trp-Trp | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
nicotine | Cavia porcellus (domestic guinea pig) | Ki | 0.2260 | 2 | 2 |
glycyltryptophan | Cavia porcellus (domestic guinea pig) | IC50 | 520.0000 | 1 | 1 |
glycyltyrosine | Cavia porcellus (domestic guinea pig) | IC50 | 120.0000 | 1 | 1 |
glycylleucine | Cavia porcellus (domestic guinea pig) | IC50 | 70.0000 | 1 | 1 |
alanyltyrosine | Cavia porcellus (domestic guinea pig) | IC50 | 170.0000 | 1 | 1 |
glycyl-l-phenylalanine | Cavia porcellus (domestic guinea pig) | IC50 | 170.0000 | 1 | 1 |
glycylsarcosine | Cavia porcellus (domestic guinea pig) | IC50 | 1,160.0000 | 1 | 1 |
alanylphenylalanine | Cavia porcellus (domestic guinea pig) | IC50 | 70.0000 | 1 | 1 |
tryptophylglycine | Cavia porcellus (domestic guinea pig) | IC50 | 730.0000 | 1 | 1 |
glycylaspartic acid | Cavia porcellus (domestic guinea pig) | IC50 | 380.0000 | 1 | 1 |
n-glycylglutamic acid | Cavia porcellus (domestic guinea pig) | IC50 | 650.0000 | 1 | 1 |
histidylglycine | Cavia porcellus (domestic guinea pig) | IC50 | 340.0000 | 1 | 1 |
enkephalin, d-penicillamine (2,5)- | Cavia porcellus (domestic guinea pig) | Ki | 0.0017 | 1 | 1 |
sr141716 | Cavia porcellus (domestic guinea pig) | IC50 | 0.1080 | 1 | 1 |
u 69593 | Cavia porcellus (domestic guinea pig) | IC50 | 0.5880 | 2 | 3 |
u 69593 | Cavia porcellus (domestic guinea pig) | Ki | 0.2464 | 5 | 11 |
valylvaline | Cavia porcellus (domestic guinea pig) | IC50 | 210.0000 | 1 | 1 |
tifluadom | Cavia porcellus (domestic guinea pig) | Ki | 0.0019 | 1 | 1 |
valdecoxib | Cavia porcellus (domestic guinea pig) | Ki | 0.0430 | 1 | 1 |
tyrosyl-arginyl-phenylalanyl-lysinamide | Cavia porcellus (domestic guinea pig) | IC50 | 0.2540 | 1 | 1 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | IC50 | 10.0000 | 1 | 1 |
dermorphin, arg(2)- | Cavia porcellus (domestic guinea pig) | IC50 | 0.0900 | 1 | 1 |
2-(3,4-dichlorophenyl)-n-methyl-n-(1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl)acetamide | Cavia porcellus (domestic guinea pig) | IC50 | 1.7990 | 1 | 3 |
glycyl-leucyl-phenylalanine | Cavia porcellus (domestic guinea pig) | IC50 | 980.0000 | 1 | 1 |
lysyllysine | Cavia porcellus (domestic guinea pig) | IC50 | 10,900.0000 | 1 | 1 |
2-(4-morpholinyl)-4h-1-benzopyran-4-one | Cavia porcellus (domestic guinea pig) | IC50 | 10.0000 | 1 | 1 |
3,5-bis(trifluoromethyl)benzyl n-acetyltryptophan | Cavia porcellus (domestic guinea pig) | IC50 | 0.3981 | 1 | 1 |
3,5-bis(trifluoromethyl)benzyl n-acetyltryptophan | Cavia porcellus (domestic guinea pig) | Ki | 0.1340 | 1 | 1 |
ly 99335, (3r-cis)-isomer | Cavia porcellus (domestic guinea pig) | Ki | 0.0800 | 1 | 1 |
ly 106737 | Cavia porcellus (domestic guinea pig) | Ki | 0.0015 | 1 | 1 |
aspartylglycine | Cavia porcellus (domestic guinea pig) | IC50 | 810.0000 | 1 | 1 |
arginylarginine | Cavia porcellus (domestic guinea pig) | IC50 | 7,310.0000 | 1 | 1 |
enkephalin, pen(2,5)-4-chloro-phe(4)- | Cavia porcellus (domestic guinea pig) | Ki | 0.1800 | 1 | 1 |
n-valyltryptophan | Cavia porcellus (domestic guinea pig) | IC50 | 100.0000 | 1 | 1 |
4-(2-aminoethyl)benzenesulfonamide | Cavia porcellus (domestic guinea pig) | Ki | 0.1600 | 1 | 1 |
varenicline | Cavia porcellus (domestic guinea pig) | Ki | 0.1952 | 2 | 2 |
zm 241385 | Cavia porcellus (domestic guinea pig) | Ki | 0.0008 | 1 | 1 |
sch 58261 | Cavia porcellus (domestic guinea pig) | Ki | 0.0006 | 1 | 1 |
prolylglutamic acid | Cavia porcellus (domestic guinea pig) | IC50 | 12,300.0000 | 1 | 1 |
n-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0150 | 1 | 1 |
sorbinil | Cavia porcellus (domestic guinea pig) | IC50 | 1.1000 | 1 | 1 |
halenaquinone | Cavia porcellus (domestic guinea pig) | IC50 | 3.7000 | 1 | 1 |
glutamyl-glutamic acid | Cavia porcellus (domestic guinea pig) | IC50 | 620.0000 | 1 | 1 |
davidigenin | Cavia porcellus (domestic guinea pig) | IC50 | 1,000.0000 | 1 | 1 |
enkephalin, methionine | Cavia porcellus (domestic guinea pig) | Ki | 0.0069 | 1 | 1 |
enkephalin, leucine | Cavia porcellus (domestic guinea pig) | IC50 | 0.2460 | 1 | 1 |
enkephalin, leucine | Cavia porcellus (domestic guinea pig) | Ki | 0.3800 | 1 | 1 |
aspartyl-aspartic acid | Cavia porcellus (domestic guinea pig) | IC50 | 630.0000 | 1 | 1 |
n-glycylalanine | Cavia porcellus (domestic guinea pig) | IC50 | 1,820.0000 | 1 | 1 |
glycylproline | Cavia porcellus (domestic guinea pig) | IC50 | 330.0000 | 1 | 1 |
mitragynine | Cavia porcellus (domestic guinea pig) | Ki | 0.0072 | 1 | 1 |
u-50488 | Cavia porcellus (domestic guinea pig) | Ki | 0.5226 | 6 | 13 |
ketazocine | Cavia porcellus (domestic guinea pig) | Ki | 0.0033 | 1 | 1 |
glycyllysine | Cavia porcellus (domestic guinea pig) | IC50 | 1,250.0000 | 1 | 1 |
ici 199441 | Cavia porcellus (domestic guinea pig) | Ki | 0.0001 | 1 | 1 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Cavia porcellus (domestic guinea pig) | Ki | 0.1140 | 1 | 1 |
benzene-1-3-disulfonamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0080 | 1 | 1 |
mangostin | Cavia porcellus (domestic guinea pig) | IC50 | 0.5800 | 1 | 1 |
dorzolamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0090 | 1 | 1 |
naloxone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0089 | 1 | 1 |
naloxone | Cavia porcellus (domestic guinea pig) | Ki | 0.0017 | 2 | 2 |
oxymorphone | Cavia porcellus (domestic guinea pig) | Ki | 0.0150 | 1 | 1 |
topiramate | Cavia porcellus (domestic guinea pig) | Ki | 0.0100 | 1 | 1 |
morphine | Cavia porcellus (domestic guinea pig) | IC50 | 0.2020 | 4 | 4 |
morphine | Cavia porcellus (domestic guinea pig) | Ki | 0.0413 | 15 | 24 |
su 5402 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0200 | 1 | 1 |
7-benzylidenenaltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0260 | 1 | 2 |
endomorphin 1 | Cavia porcellus (domestic guinea pig) | Ki | 0.0046 | 1 | 2 |
j 113397 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0023 | 1 | 2 |
semaxinib | Cavia porcellus (domestic guinea pig) | IC50 | 0.2000 | 1 | 1 |
su 11248 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0180 | 1 | 1 |
levorphanol | Cavia porcellus (domestic guinea pig) | IC50 | 0.0006 | 1 | 2 |
levorphanol | Cavia porcellus (domestic guinea pig) | Ki | 0.0002 | 1 | 1 |
cyclorphan | Cavia porcellus (domestic guinea pig) | Ki | 0.0001 | 1 | 1 |
naltrexone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0004 | 3 | 3 |
naltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0011 | 16 | 21 |
n-methylnaltrindole | Cavia porcellus (domestic guinea pig) | Ki | 0.0392 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | IC50 | 0.0283 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | Ki | 0.0009 | 3 | 3 |
norbinaltorphimine | Cavia porcellus (domestic guinea pig) | Ki | 0.0173 | 12 | 19 |
alanylalanine | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
dermorphin | Cavia porcellus (domestic guinea pig) | IC50 | 0.0026 | 3 | 3 |
6 beta-hydroxynaltrexone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0013 | 2 | 3 |
14-methoxymetopon | Cavia porcellus (domestic guinea pig) | Ki | 0.3040 | 1 | 1 |
biphalin | Cavia porcellus (domestic guinea pig) | IC50 | 0.0025 | 1 | 1 |
biphalin | Cavia porcellus (domestic guinea pig) | Ki | 0.0014 | 1 | 2 |
phenylalanylalanine | Cavia porcellus (domestic guinea pig) | IC50 | 70.0000 | 1 | 1 |
alanyltyrosine | Cavia porcellus (domestic guinea pig) | IC50 | 110.0000 | 1 | 1 |
naltrindole | Cavia porcellus (domestic guinea pig) | Ki | 0.0104 | 10 | 15 |
prolylglycine | Cavia porcellus (domestic guinea pig) | IC50 | 16,000.0000 | 1 | 1 |
arginyllysine | Cavia porcellus (domestic guinea pig) | IC50 | 8,110.0000 | 1 | 1 |
manoalide | Cavia porcellus (domestic guinea pig) | IC50 | 0.5000 | 1 | 1 |
7-benzylidenenaltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0330 | 1 | 2 |
(2E,4E)-N-isobutyl-2,4-dodecadienamide | Cavia porcellus (domestic guinea pig) | Ki | 0.0520 | 1 | 1 |
trk 820 | Cavia porcellus (domestic guinea pig) | Ki | 0.0006 | 2 | 2 |
clocinnamox | Cavia porcellus (domestic guinea pig) | Ki | 0.0027 | 1 | 1 |
vilazodone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0003 | 1 | 1 |
phenylalanylglycine | Cavia porcellus (domestic guinea pig) | IC50 | 170.0000 | 1 | 1 |
histidylhistidine | Cavia porcellus (domestic guinea pig) | IC50 | 400.0000 | 1 | 1 |
lysylglutamic acid | Cavia porcellus (domestic guinea pig) | IC50 | 820.0000 | 1 | 1 |
Ala-Lys | Cavia porcellus (domestic guinea pig) | IC50 | 280.0000 | 1 | 1 |
valyl-valyl-valine | Cavia porcellus (domestic guinea pig) | IC50 | 230.0000 | 1 | 1 |
lysylglycine | Cavia porcellus (domestic guinea pig) | IC50 | 380.0000 | 1 | 1 |
glycylhistidine | Cavia porcellus (domestic guinea pig) | IC50 | 810.0000 | 1 | 1 |
prolyl-serine | Cavia porcellus (domestic guinea pig) | IC50 | 16,000.0000 | 1 | 1 |
sodium selenate | Cavia porcellus (domestic guinea pig) | Ki | 0.0002 | 1 | 1 |
lu 28-179 | Cavia porcellus (domestic guinea pig) | Ki | 0.0170 | 1 | 1 |
st 1535 | Cavia porcellus (domestic guinea pig) | Ki | 0.0066 | 1 | 1 |
ly 255582 | Cavia porcellus (domestic guinea pig) | Ki | 0.0001 | 2 | 3 |
dysidenin | Cavia porcellus (domestic guinea pig) | Ki | 9.0000 | 1 | 1 |
deltorphin ii, ala(2)- | Cavia porcellus (domestic guinea pig) | Ki | 0.5000 | 1 | 2 |
deltorphin i, ala(2)- | Cavia porcellus (domestic guinea pig) | Ki | 0.6770 | 1 | 3 |
8-carboxamidocyclazocine | Cavia porcellus (domestic guinea pig) | Ki | 0.0004 | 2 | 2 |
snap 6201 | Cavia porcellus (domestic guinea pig) | Ki | 4.0000 | 2 | 3 |
ufp-502 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0355 | 1 | 1 |
2-(2-fluoro-5-methylphenyl)-4,5-dihydro-1h-imidazole | Cavia porcellus (domestic guinea pig) | Ki | 0.0053 | 1 | 1 |
PB28 | Cavia porcellus (domestic guinea pig) | Ki | 0.0004 | 1 | 1 |
dynorphin a (1-11)-amide | Cavia porcellus (domestic guinea pig) | IC50 | 0.0099 | 2 | 4 |
dynorphin a (1-11)-amide | Cavia porcellus (domestic guinea pig) | Ki | 0.0007 | 1 | 1 |
h-dmt-tic-gly-nh-bzl | Cavia porcellus (domestic guinea pig) | Ki | 0.0000 | 1 | 1 |
ki 8751 | Cavia porcellus (domestic guinea pig) | IC50 | 2.4000 | 1 | 1 |
nu 7441 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0300 | 1 | 1 |
adl 5859 | Cavia porcellus (domestic guinea pig) | IC50 | 78.0000 | 1 | 1 |
prolyl-proline | Cavia porcellus (domestic guinea pig) | IC50 | 800.0000 | 1 | 1 |
ku-0060648 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0050 | 1 | 1 |
sazetidine-a | Cavia porcellus (domestic guinea pig) | Ki | 0.9500 | 2 | 2 |
acyline | Cavia porcellus (domestic guinea pig) | IC50 | 0.0005 | 1 | 1 |
azd1283 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0110 | 1 | 1 |
halisulfate 1 | Cavia porcellus (domestic guinea pig) | IC50 | 12.6000 | 1 | 1 |
a-922500 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0200 | 1 | 1 |
dynorphins | Cavia porcellus (domestic guinea pig) | Ki | 0.0147 | 3 | 4 |
7-hydroxymitragynine | Cavia porcellus (domestic guinea pig) | Ki | 0.0114 | 2 | 2 |
7-spiroindanyloxymorphone | Cavia porcellus (domestic guinea pig) | Ki | 0.0106 | 2 | 4 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
loperamide | Cavia porcellus (domestic guinea pig) | EC50 | 0.0580 | 1 | 1 |
estrone | Cavia porcellus (domestic guinea pig) | EC50 | 0.0080 | 1 | 1 |
alpha-aminopyridine | Cavia porcellus (domestic guinea pig) | Kd | 4,000.0000 | 1 | 1 |
1,2-Dihydroquinolin-2-imine | Cavia porcellus (domestic guinea pig) | Kd | 125.0000 | 1 | 1 |
captopril | Cavia porcellus (domestic guinea pig) | EC50 | 1,422.6600 | 1 | 1 |
quinpirole | Cavia porcellus (domestic guinea pig) | EC50 | 0.0510 | 1 | 1 |
spiradoline | Cavia porcellus (domestic guinea pig) | EC50 | 0.0180 | 1 | 1 |
1-aminoisoquinoline | Cavia porcellus (domestic guinea pig) | Kd | 650.0000 | 1 | 1 |
u 69593 | Cavia porcellus (domestic guinea pig) | EC50 | 0.0077 | 1 | 1 |
u 69593 | Cavia porcellus (domestic guinea pig) | Kd | 1.2672 | 4 | 5 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | Kd | 0.4950 | 4 | 4 |
u-50488 | Cavia porcellus (domestic guinea pig) | EC50 | 0.0460 | 1 | 2 |
naloxone | Cavia porcellus (domestic guinea pig) | Kd | 0.0002 | 1 | 1 |
endomorphin 1 | Cavia porcellus (domestic guinea pig) | EC50 | 0.9320 | 1 | 1 |
endomorphin 2 | Cavia porcellus (domestic guinea pig) | EC50 | 1.0000 | 1 | 1 |
cyclorphan | Cavia porcellus (domestic guinea pig) | EC50 | 0.0002 | 1 | 2 |
naltrexone | Cavia porcellus (domestic guinea pig) | EC50 | 0.0019 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | EC50 | 0.0325 | 5 | 8 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | Kd | 0.5920 | 2 | 3 |
biphalin | Cavia porcellus (domestic guinea pig) | EC50 | 0.0011 | 2 | 3 |
tyrosyl alanyl-glycyl-phenylalaninamide | Cavia porcellus (domestic guinea pig) | EC50 | 0.0117 | 1 | 2 |
naltrindole | Cavia porcellus (domestic guinea pig) | EC50 | 0.0050 | 1 | 1 |
trk 820 | Cavia porcellus (domestic guinea pig) | EC50 | 0.0006 | 1 | 1 |
enkephalin, leucine-2-alanine | Cavia porcellus (domestic guinea pig) | EC50 | 0.0540 | 1 | 1 |
sodium selenate | Cavia porcellus (domestic guinea pig) | EC50 | 0.0013 | 1 | 2 |
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Cavia porcellus (domestic guinea pig) | Kd | 0.0000 | 1 | 1 |
4-iodo-2,5-dimethoxyphenylisopropylamine, (r)-isomer | Cavia porcellus (domestic guinea pig) | EC50 | 0.0119 | 1 | 1 |
deltorphin i, ala(2)- | Cavia porcellus (domestic guinea pig) | EC50 | 0.0000 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
nordazepam | Cavia porcellus (domestic guinea pig) | Activity | 17.0000 | 1 | 1 |
u 69593 | Cavia porcellus (domestic guinea pig) | ED50 | 1.7775 | 2 | 4 |
u 69593 | Cavia porcellus (domestic guinea pig) | Emax | 0.1703 | 4 | 6 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | ED50 | 0.5840 | 2 | 4 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | Emax | 0.1347 | 4 | 6 |
7-benzylidenenaltrexone | Cavia porcellus (domestic guinea pig) | Ke | 0.0083 | 1 | 2 |
naltrexone | Cavia porcellus (domestic guinea pig) | Ke | 0.0010 | 3 | 4 |
n-methylnaltrindole | Cavia porcellus (domestic guinea pig) | Ke | 0.0110 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | ED50 | 0.5920 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | Emax | 0.1230 | 2 | 2 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | pEC50 | 0.0074 | 1 | 1 |
norbinaltorphimine | Cavia porcellus (domestic guinea pig) | Ke | 0.0148 | 8 | 10 |
binaltorphimine | Cavia porcellus (domestic guinea pig) | Ke | 0.0110 | 1 | 1 |
naltrexone hydrochloride | Cavia porcellus (domestic guinea pig) | Ke | 0.0011 | 2 | 2 |
oxymorphindole | Cavia porcellus (domestic guinea pig) | Ke | 0.1110 | 1 | 1 |
naltrindole | Cavia porcellus (domestic guinea pig) | Ke | 0.0309 | 4 | 7 |
cyprodime | Cavia porcellus (domestic guinea pig) | Ke | 0.0286 | 2 | 2 |
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Cavia porcellus (domestic guinea pig) | Ke | 0.0300 | 1 | 2 |
ly 255582 | Cavia porcellus (domestic guinea pig) | Ke | 0.0000 | 1 | 2 |
ici 174865 | Cavia porcellus (domestic guinea pig) | Ke | 1.6670 | 1 | 1 |
Isatin-pyrazole benzenesulfonamide hybrids potently inhibit tumor-associated carbonic anhydrase isoforms IX and XII.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
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
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
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
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.Journal of medicinal chemistry, , Feb-27, Volume: 46, Issue:5, 2003
Selective reversible and irreversible ligands for the kappa opioid receptor.Journal of medicinal chemistry, , Jun-12, Volume: 35, Issue:12, 1992
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Novel cyclic biphalin analogue with improved antinociceptive properties.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
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
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
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
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
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
(+/-)-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
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
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
Selective reversible and irreversible ligands for the kappa opioid receptor.Journal of medicinal chemistry, , Jun-12, Volume: 35, Issue:12, 1992
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.Journal of medicinal chemistry, , Aug-07, Volume: 35, Issue:16, 1992
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Synthesis of 8-aminomorphans with high KOR affinity.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
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 opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.Journal of medicinal chemistry, , Sep-16, Volume: 37, Issue:19, 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
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Synthesis of 8-aminomorphans with high KOR affinity.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Orally active opioid compounds from a non-poppy source.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
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 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
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
3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.Bioorganic & medicinal chemistry letters, , Jul-09, Volume: 11, Issue:13, 2001
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.Journal of medicinal chemistry, , Sep-16, Volume: 37, Issue:19, 1994
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.Journal of medicinal chemistry, , Aug-07, Volume: 35, Issue:16, 1992
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.Journal of medicinal chemistry, , Volume: 30, Issue:9, 1987
Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics.Journal of medicinal chemistry, , Volume: 23, Issue:9, 1980
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
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
Effect of anchoring 4-anilidopiperidines to opioid peptides.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
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
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
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
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 2010
Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
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
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
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
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.Bioorganic & medicinal chemistry letters, , Jul-09, Volume: 11, Issue:13, 2001
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
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
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
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.Journal of medicinal chemistry, , Dec-09, Volume: 37, Issue:25, 1994
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
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.Journal of medicinal chemistry, , Volume: 33, Issue:6, 1990
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Peptides as receptor selectivity modulators of opiate pharmacophores.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
Chemical space screening around PheBioorganic & medicinal chemistry letters, , 07-15, Volume: 28, Issue:13, 2018
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, 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
Development of potent μ and δ opioid agonists with high lipophilicity.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 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
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
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 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
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
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
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 of 6,14-epoxymorphinan derivatives and their pharmacologies.Bioorganic & medicinal chemistry, , Feb-01, Volume: 19, Issue:3, 2011
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Importance of phenolic address groups in opioid kappa receptor selective antagonists.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
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
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
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
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
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
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists.Journal of medicinal chemistry, , Jan-08, Volume: 36, Issue:1, 1993
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
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
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]ACS medicinal chemistry letters, , Nov-09, Volume: 8, Issue:11, 2017
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.Journal of medicinal chemistry, , Volume: 30, Issue:9, 1987
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
Effect of anchoring 4-anilidopiperidines to opioid peptides.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
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
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
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 opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
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, 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
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
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Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.Bioorganic & medicinal chemistry letters, , Apr-09, Volume: 11, Issue:7, 2001
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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 of peptidomimetic delta opioid receptor antagonists using the message-address concept.Journal of medicinal chemistry, , Volume: 33, Issue:6, 1990
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Progress in the development of more effective and safer analgesics for pain management.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.Bioorganic & medicinal chemistry, , Feb-01, Volume: 19, Issue:3, 2011
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
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
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
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
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
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
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Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
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[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
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