Page last updated: 2024-08-07 16:37:24
Kappa-type opioid receptor
A kappa-type opioid receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41145]
Synonyms
K-OR-1;
KOR-1
Research
Bioassay Publications (317)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 7 (2.21) | 18.7374 |
1990's | 14 (4.42) | 18.2507 |
2000's | 131 (41.32) | 29.6817 |
2010's | 142 (44.79) | 24.3611 |
2020's | 23 (7.26) | 2.80 |
Compounds (194)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bremazocine | Homo sapiens (human) | IC50 | 0.0008 | 2 | 3 |
bremazocine | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
amiodarone | Homo sapiens (human) | IC50 | 16.6800 | 1 | 0 |
amiodarone | Homo sapiens (human) | Ki | 6.6720 | 1 | 0 |
astemizole | Homo sapiens (human) | IC50 | 6.6160 | 1 | 0 |
astemizole | Homo sapiens (human) | Ki | 2.6460 | 1 | 0 |
bisacodyl | Homo sapiens (human) | IC50 | 2.4370 | 1 | 0 |
bisacodyl | Homo sapiens (human) | Ki | 0.9750 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | IC50 | 11.0820 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | Ki | 4.4330 | 1 | 0 |
clotrimazole | Homo sapiens (human) | IC50 | 6.3030 | 1 | 0 |
clotrimazole | Homo sapiens (human) | Ki | 2.5210 | 1 | 0 |
disulfiram | Homo sapiens (human) | IC50 | 6.1030 | 1 | 0 |
disulfiram | Homo sapiens (human) | Ki | 2.4410 | 1 | 0 |
domperidone | Homo sapiens (human) | IC50 | 6.9940 | 1 | 0 |
domperidone | Homo sapiens (human) | Ki | 2.7980 | 1 | 0 |
econazole | Homo sapiens (human) | IC50 | 8.6160 | 1 | 0 |
econazole | Homo sapiens (human) | Ki | 3.4460 | 1 | 0 |
fentanyl | Homo sapiens (human) | IC50 | 1.5800 | 1 | 1 |
fentanyl | Homo sapiens (human) | Ki | 0.1965 | 1 | 1 |
fluphenazine | Homo sapiens (human) | IC50 | 24.7270 | 1 | 0 |
fluphenazine | Homo sapiens (human) | Ki | 9.8910 | 1 | 0 |
fluspirilene | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
gr 89696 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 3 |
gr 89696 | Homo sapiens (human) | Ki | 0.1802 | 2 | 2 |
haloprogin | Homo sapiens (human) | IC50 | 1.1470 | 1 | 0 |
haloprogin | Homo sapiens (human) | Ki | 0.4590 | 1 | 0 |
ici 204448 | Homo sapiens (human) | Ki | 0.0027 | 1 | 1 |
loperamide | Homo sapiens (human) | IC50 | 3.1250 | 1 | 0 |
loperamide | Homo sapiens (human) | Ki | 1.2500 | 1 | 0 |
meperidine | Homo sapiens (human) | IC50 | 14.2900 | 3 | 3 |
methadone | Homo sapiens (human) | IC50 | 0.5120 | 1 | 1 |
miconazole | Homo sapiens (human) | IC50 | 6.5940 | 1 | 0 |
miconazole | Homo sapiens (human) | Ki | 2.6370 | 1 | 0 |
propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
raloxifene | Homo sapiens (human) | IC50 | 1.6020 | 1 | 0 |
raloxifene | Homo sapiens (human) | Ki | 0.6410 | 1 | 0 |
thioridazine | Homo sapiens (human) | IC50 | 2.4900 | 1 | 0 |
thioridazine | Homo sapiens (human) | Ki | 0.9960 | 1 | 0 |
ultram | Homo sapiens (human) | Ki | 0.0140 | 1 | 1 |
ethinyl estradiol | Homo sapiens (human) | IC50 | 25.8940 | 1 | 0 |
ethinyl estradiol | Homo sapiens (human) | Ki | 10.3580 | 1 | 0 |
dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 1.2430 | 1 | 0 |
dibenzothiazyl disulfide | Homo sapiens (human) | Ki | 0.4970 | 1 | 0 |
indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
gentian violet | Homo sapiens (human) | IC50 | 1.5400 | 1 | 0 |
gentian violet | Homo sapiens (human) | Ki | 0.6160 | 1 | 0 |
pimozide | Homo sapiens (human) | IC50 | 0.9900 | 1 | 1 |
cyclazocine | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
danazol | Homo sapiens (human) | IC50 | 15.5180 | 1 | 0 |
danazol | Homo sapiens (human) | Ki | 6.2070 | 1 | 0 |
penfluridol | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
tramadol | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
mifepristone | Homo sapiens (human) | IC50 | 20.0960 | 1 | 0 |
mifepristone | Homo sapiens (human) | Ki | 8.0380 | 1 | 0 |
spiradoline | Homo sapiens (human) | IC50 | 0.0083 | 1 | 0 |
spiradoline | Homo sapiens (human) | Ki | 0.0033 | 1 | 0 |
enadoline | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
carfentanil | Homo sapiens (human) | Ki | 0.0431 | 1 | 1 |
nelfinavir | Homo sapiens (human) | IC50 | 35.9960 | 1 | 0 |
nelfinavir | Homo sapiens (human) | Ki | 14.3980 | 1 | 0 |
loperamide hydrochloride | Homo sapiens (human) | IC50 | 0.1550 | 1 | 1 |
enkephalin, d-penicillamine (2,5)- | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
vanoxerine | Homo sapiens (human) | IC50 | 2.1400 | 1 | 1 |
u 69593 | Homo sapiens (human) | IC50 | 0.0580 | 4 | 5 |
u 69593 | Homo sapiens (human) | Ki | 0.2420 | 13 | 38 |
gr 127935 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
tifluadom | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
bw 373u86 | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
bw 373u86 | Homo sapiens (human) | Ki | 1.7650 | 2 | 2 |
enkephalin-leu, arg(6)- | Homo sapiens (human) | Ki | 0.4040 | 1 | 1 |
tyrosyl-arginyl-phenylalanyl-lysinamide | Homo sapiens (human) | Ki | 4.2300 | 1 | 1 |
met-enkephalinamide | Homo sapiens (human) | Ki | 0.2100 | 1 | 1 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | IC50 | 2.4800 | 2 | 2 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | Ki | 3.7463 | 3 | 3 |
4-methoxymethylfentanyl | Homo sapiens (human) | Ki | 0.0630 | 1 | 1 |
salvinorin a | Homo sapiens (human) | Ki | 0.3451 | 20 | 49 |
ly 99335, (3r-cis)-isomer | Homo sapiens (human) | Ki | 0.8330 | 1 | 1 |
ly 106737 | Homo sapiens (human) | Ki | 0.0255 | 6 | 6 |
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(+-)-isomer | Homo sapiens (human) | Ki | 0.0014 | 4 | 4 |
nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
n-methyl-n-(1-phenyl-2-(1-pyrrolidinyl)ethyl)phenylacetamide | Homo sapiens (human) | Ki | 0.0058 | 1 | 1 |
ritonavir | Homo sapiens (human) | IC50 | 13.6550 | 1 | 0 |
ritonavir | Homo sapiens (human) | Ki | 5.4620 | 1 | 0 |
saquinavir | Homo sapiens (human) | IC50 | 6.9510 | 1 | 0 |
saquinavir | Homo sapiens (human) | Ki | 2.7800 | 1 | 0 |
pentazocine | Homo sapiens (human) | Ki | 0.0022 | 1 | 1 |
enkephalin, methionine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
diprenorphine | Homo sapiens (human) | Ki | 0.0003 | 5 | 5 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 4.5630 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | Ki | 1.8250 | 1 | 0 |
enkephalin, leucine | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
cannabidiol | Homo sapiens (human) | Ki | 2.3000 | 1 | 1 |
buprenorphine | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
etorphine | Homo sapiens (human) | Ki | 0.0005 | 2 | 2 |
tamoxifen | Homo sapiens (human) | IC50 | 15.6290 | 1 | 0 |
tamoxifen | Homo sapiens (human) | Ki | 6.2520 | 1 | 0 |
hirsutine, (16e,20beta)-isomer | Homo sapiens (human) | Ki | 1.9100 | 1 | 1 |
mitragynine | Homo sapiens (human) | Ki | 0.4850 | 2 | 2 |
u-50488 | Homo sapiens (human) | IC50 | 0.0537 | 13 | 14 |
u-50488 | Homo sapiens (human) | Ki | 0.0083 | 25 | 26 |
paynantheine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
paynantheine | Homo sapiens (human) | Ki | 2.5600 | 1 | 1 |
metazocine | Homo sapiens (human) | Ki | 0.0099 | 1 | 1 |
dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0025 | 1 | 1 |
ici 199441 | Homo sapiens (human) | Ki | 0.0000 | 4 | 4 |
dynorphin (1-11) | Homo sapiens (human) | IC50 | 0.0066 | 2 | 2 |
dynorphin (1-11) | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | IC50 | 0.6187 | 6 | 6 |
brl 52537 | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
flunarizine hydrochloride | Homo sapiens (human) | IC50 | 9.4800 | 1 | 1 |
codeine | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
codeine | Homo sapiens (human) | Ki | 25.4110 | 1 | 1 |
hydrocodone | Homo sapiens (human) | Ki | 0.2600 | 1 | 1 |
hydromorphone | Homo sapiens (human) | Ki | 0.0028 | 1 | 1 |
nalmefene | Homo sapiens (human) | Ki | 0.0006 | 4 | 4 |
nalorphine | Homo sapiens (human) | Ki | 0.0012 | 2 | 2 |
naloxone | Homo sapiens (human) | IC50 | 0.0796 | 8 | 7 |
naloxone | Homo sapiens (human) | Ki | 0.0321 | 16 | 15 |
oxymorphone | Homo sapiens (human) | Ki | 0.0253 | 1 | 1 |
morphine | Homo sapiens (human) | IC50 | 0.6550 | 3 | 3 |
morphine | Homo sapiens (human) | Ki | 0.1098 | 26 | 26 |
7-benzylidenenaltrexone | Homo sapiens (human) | Ki | 0.0306 | 2 | 2 |
alpha-neoendorphin | Homo sapiens (human) | Ki | 0.0024 | 1 | 1 |
beta-funaltrexamine | Homo sapiens (human) | Ki | 0.0009 | 2 | 2 |
endomorphin 1 | Homo sapiens (human) | Ki | 2.4412 | 3 | 5 |
endomorphin 2 | Homo sapiens (human) | Ki | 1.1513 | 4 | 6 |
j 113397 | Homo sapiens (human) | IC50 | 1.5000 | 2 | 2 |
j 113397 | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
l 745870 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
nalbuphine | Homo sapiens (human) | IC50 | 0.0970 | 2 | 1 |
nalbuphine | Homo sapiens (human) | Ki | 0.0164 | 3 | 2 |
n-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide | Homo sapiens (human) | IC50 | 7.5120 | 1 | 1 |
n-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide | Homo sapiens (human) | Ki | 1.0572 | 2 | 2 |
notopterol | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
levorphanol | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
levorphanol | Homo sapiens (human) | Ki | 0.0023 | 6 | 6 |
cyclorphan | Homo sapiens (human) | Ki | 0.0000 | 8 | 8 |
naltrexone | Homo sapiens (human) | IC50 | 0.0377 | 8 | 9 |
naltrexone | Homo sapiens (human) | Ki | 0.0024 | 28 | 29 |
butorphanol | Homo sapiens (human) | Ki | 0.0002 | 3 | 3 |
methylnaltrexone | Homo sapiens (human) | Ki | 0.0321 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | Ki | 3.4116 | 7 | 7 |
naloxone hydrochloride | Homo sapiens (human) | IC50 | 0.0049 | 2 | 2 |
norbinaltorphimine | Homo sapiens (human) | IC50 | 0.0036 | 7 | 7 |
norbinaltorphimine | Homo sapiens (human) | Ki | 0.0013 | 24 | 24 |
dermorphin | Homo sapiens (human) | Ki | 8.1620 | 1 | 1 |
naltrexone hydrochloride | Homo sapiens (human) | IC50 | 0.0006 | 2 | 2 |
6 beta-hydroxynaltrexone | Homo sapiens (human) | IC50 | 0.0083 | 2 | 5 |
6 beta-hydroxynaltrexone | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
14-methoxymetopon | Homo sapiens (human) | Ki | 0.1148 | 3 | 3 |
biphalin | Homo sapiens (human) | Ki | 0.2700 | 1 | 1 |
alvimopan anhydrous | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
tyrosyl alanyl-glycyl-phenylalaninamide | Homo sapiens (human) | IC50 | 0.2239 | 1 | 1 |
oxymorphindole | Homo sapiens (human) | Ki | 0.4555 | 2 | 2 |
naltrindole | Homo sapiens (human) | Ki | 0.0169 | 12 | 12 |
trk 820 | Homo sapiens (human) | Ki | 0.0426 | 4 | 4 |
clocinnamox | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
clocinnamox | Homo sapiens (human) | Ki | 0.0014 | 4 | 4 |
gr 103545 | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(-)-isomer | Homo sapiens (human) | Ki | 0.1730 | 2 | 2 |
nalfurafine hydrochloride | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
naloxonazine | Homo sapiens (human) | IC50 | 0.0850 | 1 | 0 |
naloxonazine | Homo sapiens (human) | Ki | 0.0340 | 1 | 0 |
sodium selenate | Homo sapiens (human) | Ki | 0.0001 | 15 | 15 |
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Homo sapiens (human) | Ki | 0.0001 | 3 | 3 |
o-demethyltramadol | Homo sapiens (human) | Ki | 5.2250 | 2 | 2 |
ro 64-6198 | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
sr 14150 | Homo sapiens (human) | Ki | 0.0427 | 2 | 2 |
ly 255582 | Homo sapiens (human) | Ki | 0.0036 | 4 | 4 |
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
sb-612111 | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
deltorphin i, ala(2)- | Homo sapiens (human) | IC50 | 7.3300 | 1 | 1 |
8-carboxamidocyclazocine | Homo sapiens (human) | Ki | 0.0001 | 3 | 3 |
akuammicine | Homo sapiens (human) | Ki | 0.0842 | 1 | 2 |
6-deoxy-6-fluoronaltrexone | Homo sapiens (human) | IC50 | 0.0079 | 1 | 1 |
dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0046 | 1 | 1 |
dynorphin a (1-11)-amide | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
dynorphin a (1-11)-amide | Homo sapiens (human) | Ki | 0.0001 | 3 | 3 |
amd 070 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
mesyl salvinorin b | Homo sapiens (human) | Ki | 0.0023 | 2 | 2 |
naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester | Homo sapiens (human) | Ki | 0.0900 | 3 | 3 |
salvinorin b | Homo sapiens (human) | Ki | 1.8118 | 6 | 6 |
way 207024 | Homo sapiens (human) | Ki | 0.5500 | 1 | 1 |
14-o-methyloxymorphone | Homo sapiens (human) | Ki | 0.0101 | 1 | 1 |
mitragynine, (3beta,16e,20beta)-isomer | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
mitragynine, (3beta,16e,20beta)-isomer | Homo sapiens (human) | Ki | 0.2225 | 2 | 2 |
mitragynine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
mitragynine | Homo sapiens (human) | Ki | 3.2000 | 1 | 1 |
a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
morphine sulfate | Homo sapiens (human) | IC50 | 0.1205 | 2 | 2 |
nociceptin | Homo sapiens (human) | Ki | 2.6078 | 6 | 6 |
dynorphin (1-17) | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
1-(1-(1-methylcyclooctyl)-4-piperidinyl)-2-((3r)-3-piperidinyl)-1h-benzimidazole | Homo sapiens (human) | Ki | 0.0231 | 1 | 1 |
salvinorin b ethoxymethyl ether | Homo sapiens (human) | Ki | 0.0017 | 2 | 2 |
dynorphins | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
dynorphins | Homo sapiens (human) | Ki | 0.2835 | 3 | 28 |
ly2456302 | Homo sapiens (human) | Ki | 0.0008 | 3 | 3 |
7-hydroxymitragynine | Homo sapiens (human) | Ki | 0.0741 | 1 | 1 |
mitragynine pseudoindoxyl | Homo sapiens (human) | IC50 | 0.1318 | 2 | 2 |
mitragynine pseudoindoxyl | Homo sapiens (human) | Ki | 0.0790 | 1 | 1 |
7-spiroindanyloxymorphone | Homo sapiens (human) | Ki | 1.5770 | 2 | 2 |
gsk 1059865 | Homo sapiens (human) | Ki | 0.3200 | 1 | 1 |
nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
cj 15,208 | Homo sapiens (human) | IC50 | 0.2435 | 2 | 2 |
cj 15,208 | Homo sapiens (human) | Ki | 0.0305 | 2 | 2 |
pf-04455242 | Homo sapiens (human) | Ki | 0.0018 | 3 | 3 |
2-[5-[(3,4-dichlorophenyl)methylthio]-4-(2-furanylmethyl)-1,2,4-triazol-3-yl]pyridine | Homo sapiens (human) | Ki | 0.0403 | 1 | 1 |
4-[[(4-ethylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | IC50 | 1.8350 | 2 | 2 |
LSM-2536 | Homo sapiens (human) | IC50 | 0.0810 | 3 | 3 |
n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 7.0407 | 2 | 3 |
3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
22-thiocyanatosalvinorin a | Homo sapiens (human) | Ki | 0.0006 | 2 | 2 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
propranolol | Homo sapiens (human) | EC50 | 5.0119 | 1 | 1 |
suramin | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
adenosine diphosphate | Homo sapiens (human) | EC50 | 11.0000 | 1 | 1 |
spiradoline | Homo sapiens (human) | EC50 | 0.0180 | 1 | 1 |
alpha,beta-methyleneadenosine 5'-triphosphate | Homo sapiens (human) | EC50 | 8.0000 | 1 | 1 |
u 69593 | Homo sapiens (human) | EC50 | 0.1892 | 31 | 56 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | EC50 | 5.2640 | 1 | 1 |
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Homo sapiens (human) | Kd | 0.6290 | 1 | 1 |
salvinorin a | Homo sapiens (human) | EC50 | 0.0184 | 33 | 60 |
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(+-)-isomer | Homo sapiens (human) | EC50 | 0.0076 | 2 | 2 |
asimadoline | Homo sapiens (human) | EC50 | 0.0005 | 1 | 1 |
n-methyl-n-(1-phenyl-2-(1-pyrrolidinyl)ethyl)phenylacetamide | Homo sapiens (human) | EC50 | 0.0500 | 1 | 1 |
adenosine 5'-o-(3-thiotriphosphate) | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
diprenorphine | Homo sapiens (human) | Kd | 0.0023 | 1 | 26 |
enkephalin, leucine | Homo sapiens (human) | EC50 | 0.0800 | 3 | 3 |
4-methyl-N-[1-[2-(1-pyrrolidinyl)ethyl]-2-benzimidazolyl]benzamide | Homo sapiens (human) | EC50 | 0.0390 | 1 | 1 |
mitragynine | Homo sapiens (human) | EC50 | 8.5000 | 1 | 1 |
u-50488 | Homo sapiens (human) | EC50 | 0.0416 | 32 | 32 |
metazocine | Homo sapiens (human) | EC50 | 0.1200 | 1 | 1 |
ketazocine | Homo sapiens (human) | EC50 | 0.0033 | 1 | 1 |
ici 199441 | Homo sapiens (human) | EC50 | 0.0003 | 3 | 3 |
hydromorphone | Homo sapiens (human) | EC50 | 0.0110 | 1 | 1 |
naloxone | Homo sapiens (human) | EC50 | 0.0083 | 2 | 2 |
naloxone | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
oxycodone | Homo sapiens (human) | EC50 | 16.0000 | 1 | 1 |
morphine | Homo sapiens (human) | EC50 | 0.4443 | 6 | 6 |
2-methylthio-atp | Homo sapiens (human) | EC50 | 0.6000 | 1 | 1 |
nalbuphine | Homo sapiens (human) | EC50 | 0.0995 | 4 | 4 |
dihydromorphine | Homo sapiens (human) | Kd | 0.8300 | 1 | 1 |
cyclorphan | Homo sapiens (human) | EC50 | 0.0002 | 7 | 7 |
naltrexone | Homo sapiens (human) | EC50 | 0.0020 | 3 | 3 |
butorphanol | Homo sapiens (human) | EC50 | 0.0029 | 1 | 1 |
methylnaltrexone | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | EC50 | 6.1217 | 3 | 3 |
norbinaltorphimine | Homo sapiens (human) | EC50 | 0.0060 | 1 | 1 |
naltrindole | Homo sapiens (human) | EC50 | 0.0050 | 1 | 1 |
cyprodime | Homo sapiens (human) | EC50 | 0.1170 | 1 | 1 |
trk 820 | Homo sapiens (human) | EC50 | 0.0223 | 5 | 5 |
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(-)-isomer | Homo sapiens (human) | EC50 | 0.0313 | 3 | 3 |
enkephalin, leucine-2-alanine | Homo sapiens (human) | Kd | 0.6250 | 1 | 1 |
nalfurafine hydrochloride | Homo sapiens (human) | EC50 | 0.0000 | 2 | 2 |
sodium selenate | Homo sapiens (human) | EC50 | 0.0013 | 8 | 8 |
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Homo sapiens (human) | Kd | 0.0000 | 1 | 1 |
sr 14150 | Homo sapiens (human) | EC50 | 0.2760 | 1 | 1 |
6'-guanidinonaltrindole | Homo sapiens (human) | EC50 | 0.0014 | 2 | 2 |
8-carboxamidocyclazocine | Homo sapiens (human) | EC50 | 0.0044 | 2 | 2 |
akuammicine | Homo sapiens (human) | EC50 | 39.8107 | 1 | 1 |
dynorphin a (1-11)-amide | Homo sapiens (human) | EC50 | 0.0007 | 2 | 2 |
mesyl salvinorin b | Homo sapiens (human) | EC50 | 0.0300 | 1 | 1 |
9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester | Homo sapiens (human) | EC50 | 0.9367 | 3 | 3 |
salvinorin b | Homo sapiens (human) | EC50 | 0.1862 | 4 | 4 |
14-o-methyloxymorphone | Homo sapiens (human) | EC50 | 0.1160 | 1 | 1 |
nociceptin | Homo sapiens (human) | EC50 | 0.0785 | 1 | 1 |
dynorphin (1-17) | Homo sapiens (human) | EC50 | 0.0024 | 4 | 4 |
1-(1-(1-methylcyclooctyl)-4-piperidinyl)-2-((3r)-3-piperidinyl)-1h-benzimidazole | Homo sapiens (human) | EC50 | 0.0800 | 1 | 1 |
salvinorin b ethoxymethyl ether | Homo sapiens (human) | EC50 | 0.0001 | 1 | 1 |
dynorphins | Homo sapiens (human) | EC50 | 0.1169 | 4 | 28 |
mitragynine pseudoindoxyl | Homo sapiens (human) | EC50 | 0.0017 | 2 | 2 |
2-[5-[(3,4-dichlorophenyl)methylthio]-4-(2-furanylmethyl)-1,2,4-triazol-3-yl]pyridine | Homo sapiens (human) | EC50 | 37.6825 | 4 | 4 |
trv130 | Homo sapiens (human) | EC50 | 5.7000 | 2 | 2 |
3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Homo sapiens (human) | EC50 | 0.1572 | 3 | 3 |
22-thiocyanatosalvinorin a | Homo sapiens (human) | EC50 | 0.2838 | 4 | 4 |
22-thiocyanatosalvinorin a | Homo sapiens (human) | Kd | 0.0006 | 1 | 1 |
Drugs with Other Measurements
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Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.Bioorganic & medicinal chemistry, , Apr-01, Volume: 22, Issue:7, 2014
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A highly selective kappa-opioid receptor agonist with low addictive potential and dependence liability.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
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A perspective on natural products research and ethnopharmacology in Mexico: the eagle and the serpent on the prickly pear cactus.Journal of natural products, , Mar-28, Volume: 77, Issue:3, 2014
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Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
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Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
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Isolation and Pharmacological Characterization of Six Opioidergic Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Discovery 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
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Opioid Receptor Modulators with a Cinnamyl Group.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral κ-opioid receptor agonists.Bioorganic & medicinal chemistry, , 07-01, Volume: 24, Issue:13, 2016
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Evaluation of N-substituent structural variations in opioid receptor profile of LP1.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Synthesis of tripeptides containing D-Trp substituted at the indole ring, assessment of opioid receptor binding and in vivo central antinociception.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 22, Issue:24, 2012
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
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Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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[no title available]Journal of natural products, , 03-26, Volume: 84, Issue:3, 2021
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[no title available]European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
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[no title available],
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14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
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14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
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Structural Requirements for CNS Active Opioid Glycopeptides.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
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Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
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New scaffolds in the development of mu opioid-receptor ligands.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
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Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Synthesis and Evaluation of a Novel Bivalent Selective Antagonist for the Mu-Delta Opioid Receptor Heterodimer that Reduces Morphine Withdrawal in Mice.Journal of medicinal chemistry, , Jul-26, Volume: 61, Issue:14, 2018
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.Bioorganic & medicinal chemistry, , Jul-15, Volume: 23, Issue:14, 2015
Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Development of κ opioid receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
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Generation of novel radiolabeled opiates through site-selective iodination.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic).Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
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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 a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
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
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
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
Structure-activity relationships of dynorphin a analogues modified in the address sequence.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
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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
[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
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Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.Bioorganic & medicinal chemistry letters, , Oct-16, Volume: 10, Issue:20, 2000
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Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 30, Issue:12, 2020
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Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
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Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
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Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 59, 2022
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
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Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
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Discovery of highly selective κ-opioid receptor agonists: 10α-Hydroxy TRK-820 derivatives.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 27, Issue:16, 2017
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.Journal of medicinal chemistry, , 02-09, Volume: 60, Issue:3, 2017
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Multitarget opioid ligands in pain relief: New players in an old game.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
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Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
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2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Generation of novel radiolabeled opiates through site-selective iodination.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
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[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Herkinorin analogues with differential beta-arrestin-2 interactions.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
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Addressing Structural Flexibility at the A-Ring on Salvinorin A: Discovery of a Potent Kappa-Opioid Agonist with Enhanced Metabolic Stability.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
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
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Herkinorin analogues with differential beta-arrestin-2 interactions.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
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Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists.Journal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
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Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent aJournal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues.Journal of medicinal chemistry, , Dec-26, Volume: 57, Issue:24, 2014
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 18, Issue:12, 2008
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
Structure-Activity Relationships of [des-ArgJournal of medicinal chemistry, , 11-23, Volume: 59, Issue:22, 2016
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.Journal of medicinal chemistry, , Nov-25, Volume: 58, Issue:22, 2015
Chemotype-selective modes of action of κ-opioid receptor agonists.The Journal of biological chemistry, , Nov-29, Volume: 288, Issue:48, 2013
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
[no title available]ACS medicinal chemistry letters, , Jul-13, Volume: 8, Issue:7, 2017
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Development of κ opioid receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Antagonists of the kappa opioid receptor.Bioorganic & medicinal chemistry letters, , May-01, Volume: 24, Issue:9, 2014
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Progress in the development of more effective and safer analgesics for pain management.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor.ACS medicinal chemistry letters, , Jul-13, Volume: 8, Issue:7, 2017
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Progress in the development of more effective and safer analgesics for pain management.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Progress in the development of more effective and safer analgesics for pain management.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
Enables
This protein enables 5 target(s):
Target | Category | Definition |
G protein-coupled opioid receptor activity | molecular function | Combining with an opioid (any narcotic derived from or resembling opium), and transmitting the signal across the membrane by activating an associated G-protein. [GOC:ai, GOC:bf, PMID:20494127] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
receptor serine/threonine kinase binding | molecular function | Binding to a receptor that possesses protein serine/threonine kinase activity. [GOC:mah] |
dynorphin receptor activity | molecular function | Combining with a dynorphin peptide, and transmitting the signal across the membrane by activating an associated G-protein. Dynorphin is any opioid peptide that is generated by cleavage of the precursor protein prodynorphin. [GOC:bf, Wikipedia:Dynorphin] |
neuropeptide binding | molecular function | Interacting selectively and non-covalently and stoichiometrically with neuropeptides, peptides with direct synaptic effects (peptide neurotransmitters) or indirect modulatory effects on the nervous system (peptide neuromodulators). [http://www.wormbook.org/chapters/www_neuropeptides/neuropeptides.html] |
Located In
This protein is located in 13 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
sarcoplasmic reticulum | cellular component | A fine reticular network of membrane-limited elements that pervades the sarcoplasm of a muscle cell; continuous over large portions of the cell and with the nuclear envelope; that part of the endoplasmic reticulum specialized for calcium release, uptake and storage. [GOC:mtg_muscle, ISBN:0124325653, ISBN:0198547684] |
T-tubule | cellular component | Invagination of the plasma membrane of a muscle cell that extends inward from the cell surface around each myofibril. The ends of T-tubules make contact with the sarcoplasmic reticulum membrane. [GOC:mtg_muscle, ISBN:0815316194] |
dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
synaptic vesicle membrane | cellular component | The lipid bilayer surrounding a synaptic vesicle. [GOC:mah] |
presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
perikaryon | cellular component | The portion of the cell soma (neuronal cell body) that excludes the nucleus. [GOC:jl] |
axon terminus | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl] |
postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
Active In
This protein is active in 2 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Involved In
This protein is involved in 30 target(s):
Target | Category | Definition |
immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
sensory perception | biological process | The series of events required for an organism to receive a sensory stimulus, convert it to a molecular signal, and recognize and characterize the signal. This is a neurological process. [GOC:ai, GOC:dph] |
locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
sensory perception of pain | biological process | The series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators] |
adenylate cyclase-inhibiting opioid receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by an opioid binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
response to insulin | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732] |
positive regulation of dopamine secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of dopamine. [GOC:sl] |
negative regulation of luteinizing hormone secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of luteinizing hormone. [GOC:mah] |
response to nicotine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nicotine stimulus. [GOC:bf, GOC:ef, ISBN:0198506732, ISBN:0582227089] |
G protein-coupled opioid receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by an opioid binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:bf, PMID:20494127] |
maternal behavior | biological process | Female behaviors associated with the care and rearing of offspring. [GOC:curators] |
eating behavior | biological process | The specific behavior of an organism relating to the intake of food, any substance (usually solid) that can be metabolized by an organism to give energy and build tissue. [GOC:jl, GOC:pr, PMID:19361967] |
response to estrogen | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by an estrogen, C18 steroid hormones that can stimulate the development of female sexual characteristics. [GOC:jl, ISBN:0198506732] |
estrous cycle | biological process | A type of ovulation cycle, which occurs in most mammalian therian females, where the endometrium is resorbed if pregnancy does not occur. [GOC:jl, Wikipedia:Estrous_cycle] |
response to ethanol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ethanol stimulus. [GOC:go_curators] |
regulation of saliva secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of saliva from a cell or a tissue. [GOC:ai] |
behavioral response to cocaine | biological process | Any process that results in a change in the behavior of an organism as a result of a cocaine stimulus. [GOC:jid] |
sensory perception of temperature stimulus | biological process | The series of events required for an organism to receive a sensory temperature stimulus, convert it to a molecular signal, and recognize and characterize the signal. This is a neurological process. [GOC:ai] |
defense response to virus | biological process | Reactions triggered in response to the presence of a virus that act to protect the cell or organism. [GOC:ai] |
cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
cellular response to glucose stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a glucose stimulus. [GOC:mah] |
positive regulation of p38MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of p38MAPK cascade. [GOC:TermGenie] |
positive regulation of potassium ion transmembrane transport | biological process | Any process that activates or increases the frequency, rate or extent of potassium ion transmembrane transport. [GOC:BHF, GOC:TermGenie] |
response to acrylamide | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an acrylamide stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:16292499] |
positive regulation of eating behavior | biological process | Any process that activates or increases the frequency, rate or extent of eating behavior. [GO_REF:0000058, GOC:TermGenie, PMID:11961051] |
conditioned place preference | biological process | The associative learning process by which an animal learns and remembers an association between a neutral, unchanging environment and a putatively rewarding, internal state produced by a xenobiotic or drug. [PMID:21549821] |
neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |