Page last updated: 2024-12-04

bucladesine

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Description

Bucladesine: A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bucladesine : A 3',5'-cyclic purine nucleotide that is the 2'-butanoate ester and 6-N-butanoyl derivative of 3',5'-cyclic AMP. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

macrocarpal C: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9687
CHEMBL ID485980
CHEBI ID50095
SCHEMBL ID62065
SCHEMBL ID20817487
MeSH IDM0006259
PubMed CID23663967
CHEMBL ID1522836
CHEBI ID31313
SCHEMBL ID93707
MeSH IDM0006259
PubMed CID454459
CHEMBL ID466994
CHEBI ID175636
SCHEMBL ID136282
MeSH IDM0006259

Synonyms (196)

Synonym
BRD-A94624445-236-02-2
n6,o2'-dibutyryl 3',5'-adenosine monophosphate
dibutyryl adenosine cyclic monophosphate
adenosine, n-(1-oxobutyl)-, cyclic 3',5'-(hydrogen phosphate) 2'-butanoate
einecs 206-649-8
n6,o2'-dibutyryl adenosine-3',5'-phosphate
n6,o2'-dibutyryl cyclic adenosine 3',5'-monophosphoric acid
n6,o2'-dibutyrylcyclic adenosine 3',5'-phosphate
nsc 143108
n6,o2'-dibutyrylcyclic amp
n6,2'-o-dibutyryl cyclic 3',5'-amp
bucladesinum [latin]
n6,o2-dibutyryl-adenosine 3',5'-cyclic monophosphate
n6,2'-o-dibutyryladenosine 3',5'-monophosphate
n(sup 6),o(sup 2')-dibutyryl camp
n6,o2'-dibutyryl 3',5'-amp
butyramide, n-(9-beta-d-ribofuranosyl-9h-purin-6-yl)-, cyclic 3',5'-(hydrogen phosphate) 2'-butyrate
cyclic amp n(sup 6),2'-o-dibutyrate
ccris 2053
n6,2'-o-dibutyryl cyclic 3',5'-adenosine monophosphate
bucladesina [spanish]
amp, cyclic dibutyryl
cyclic n6-dibutyryl-amp
n6,o2'-dibutyryl cyclic 3',5'-amp
n6,o2'-dibutyryl cyclic adenosine 3',5'-monophosphate
n6,o2'-dibutyryl-3',5'-cyclic amp
butyramide, n-(9-beta-d-ribofuranosyl-9h-furin-6-yl)-, cyclic 3',5'-(hydrogen phosphate) 2'-butyrate
dibutyryl camp
n(6),o(2)'-dibutyryladenosine-3',5'-monophosphate
n6,2'-dibutyryladenosine cyclic 3',5'-(hydrogen phosphate)
brn 0871714
n-(9-(beta-d-ribofuranosyl)-9h-purin-6-yl)butyramide cyclic 3',5'-(hydrogen phosphate) 2'-butyrate
dibutyryl acid, amp
dt 5621
3',5'-cyclic amp dibutyrate
bucladesine [inn]
n(sup 6),o(sup 2')-dibutyryl cyclic amp
n6,o2'-dibutyryl adenosine 3',5'-cyclic monophosphate
dibutyrylic cyclic amp
dbc-amp
n-(9-beta-d-ribofuranosyl)-9h-purin-6-yl)butyramide cyclic 3',5'-(hydrogen phosphate) 2'-butyrate
n(sup 6),2'-o-dibutyryl cyclic amp
n6,o2'-dibutyryladenosine 3',5'-monophosphate
n(sup 6),2'-o-dibutyryl camp
n6,o2'-dibutyryladenosine cyclic 3',5'-phosphate
dibutyl cyclic amp
n6,2'-o-dibutyryladenosine cyclic 3',5'-phosphate
n6,2-o-dibutyryladenosine 3',5'-cyclic monophosphate
bucladesina
n(6),2'-o-dibutyryl cyclic amp
n(6),o(2')-dibutyryladenosine 3',5'-monophosphate
n(6),o(2')-dibutyryl cyclic 3',5'-amp
6-n-butanoyl-2'-o-butanoyladenosine 3',5'-(hydrogen phosphate)
n(6),o(2')-dibutyryl cyclic amp
n(6),o(2')-dibutyryl adenosine 3',5'-cyclic monophosphate
n(6),o(2')-dibutyryl-3',5'-cyclic amp
CHEBI:50095 ,
n(6),2'-o-dibutyryl camp
n(6),o(2')-dibutyryl camp
bucladesinum
BIO1_000426
BIO1_000915
BIO1_001404
D07546
bucladesine (inn)
phosphoric acid, n6,2'-o-dibutryladenosine 3'-5'-cyclic
[(4ar,6r,7r,7ar)-6-[6-(butanoylamino)purin-9-yl]-2-hydroxy-2-oxo-4a,6,7,7a-tetrahydro-4h-furo[3,2-d][1,3,2]dioxaphosphinin-7-yl] butanoate
dibutyrl cylic amp
dibutyryl adenosine 3',5'-cyclic phosphate
dibutyryl 3',5'-cyclic amp
dibutyryl adenosine 3',5'-monophosphate
nsc-143108
dibutyryl-3',5'-amp
dibutyryl cyclic amp
dibutyryladenosine cyclic monophosphate
dibutyryl cyclic 3',5'-adenylic acid
dibutyryl cyclic adenosine monophosphate
dibutyryladenosine 3',5'-cyclic monophosphate
cyclic amp dibutyrate
dibutyryl cyclic adenosine 3',5'-monophosphate
BSPBIO_000997
(4ar,6r,7r,7ar)-6-[6-(butanoylamino)-9h-purin-9-yl]-2-hydroxy-2-oxidotetrahydro-4h-furo[3,2-d][1,3,2]dioxaphosphinin-7-yl butanoate
CHEMBL485980
unii-63x7mbt2lq
63x7mbt2lq ,
dtxcid9020459
dtxsid1040459 ,
tox21_110864
cas-362-74-3
gtpl5485
(4ar,6r,7r,7ar)-6-(6-butanamido-9h-purin-9-yl)-2-hydroxy-2-oxo-hexahydro-1,3,5,2$l^{5}-furo[3,2-d][1,3,2$l^{5}]dioxaphosphinin-7-yl butanoate
SCHEMBL62065
bucladesine [who-dd]
bucladesine [mi]
n-(9-.beta.-d-ribofuranosyl)-9h-purin-6-yl)butyramide cyclic 3',5'-(hydrogen phosphate) 2'-butyrate
(n6,2'-o-dibutyryl-adenosine-3',5'-mono-phosphate
dibutyryladenosine cyclic 3',5'-phosphate
(4ar,6r,7r,7ar)-6-(6-butanamido-9h-purin-9-yl)-7-(butanoyloxy)-2-hydroxy-hexahydro-2|e?-furo[3,2-d][1,3,2]dioxaphosphinin-2-olate
SR-01000003174-2
sr-01000003174
CJGYSWNGNKCJSB-YVLZZHOMSA-N
Q4983616
DB13242
SCHEMBL20817487
adenosine, n-(1-oxobutyl)-, cyclic 3',5'-(hydrogen phosphate)2'-butanoate
(4ar,6r,7r,7ar)-6-(6-butyramido-9h-purin-9-yl)-2-hydroxy-2-oxidotetrahydro-4h-furo[3,2-d][1,3,2]dioxaphosphinin-7-yl butyrate
dibutyrylcamp
butanoic acid, (4ar,6r,7r,7ar)-tetrahydro-2-hydroxy-2-oxido-6-[6-[(1-oxobutyl)amino]-9h-purin-9-yl]-4h-furo[3,2-d]-1,3,2-dioxaphosphorin-7-yl ester
AKOS040744554
MLS002207119
MLS001148197 ,
MLS000028684 ,
n6,2'-o-dibutyryladenosine-3',5'-cyclic monophosphate sodium salt
actosin
dbcamp.na
dt-5621
bucladesine sodium
sodium dibutyryl 3',5'-cyclic amp
adenosine, n-(1-oxobutyl)-, cyclic 3',5'-(hydrogen phosphate)-2'-butanoate, monosodium salt
adenosine, n-(1-oxobutyl)-, cyclic 3',5'-(hydrogen phosphate) 2'-butanoate, monosodium salt
dt 5621 sodium salt
sodium dibutyryl cyclic adenosine-3',5'-monophosphate
dibutyl cyclic amp sodium salt
einecs 241-059-4
sodium dibutyryl camp
dibutyl cyclic amp sodium
monosodium dibutyryl cyclic amp
butyramide, n-(9-beta-d-ribofuranosyl-9h-purin-6-yl)-, cyclic hydrogen phosphate, butyrate (ester), monosodium salt
dibutyl camp sodium salt
bucladesine sodium salt
bucladesine
dbcamp
16980-89-5
n6,2'-o-dibutyryladenosine 3',5'-cyclic monophosphate sodium salt, >=96% (hplc), powder
n6,2'-o-dibutyryladenosine 3',5'-cyclic monophosphate sodium salt, >=97% (hplc), powder
bucladesine sodium (jan)
D01238
actosin (tn)
smr000058940
19436-29-4
unii-4dzn2c97a7
4dzn2c97a7 ,
bucladesine sodium [jan]
n6-02'-dibutyrycyclic amp, sodium salt
einecs 243-065-2
dibutyryl 3',5'-cyclic amp sodium
adenosine, n-(1-oxobutyl)-, cyclic 3',5'-(hydrogen phosphate) 2'-butanoate, sodium salt
n6,o2'-dibutyry cyclic amp, sodium salt
sodium dibutyryl 3',5'-camp
HMS2231C19
dibutyryl-camp
sodium dibutyryl adenosine-3,5-cyclic phosphate
dibutyryl adenosine cyclic monophosphate sodium salt
bucladesine sodium salt [mi]
bucladesine sodium [who-dd]
dibutyryl cyclic amp sodium
bucladesine sodium [mart.]
n-(9-.beta.-d-ribofuranosyl-9h-purin-6-yl)butyramide cyclic 3',5'-(hydrogen phosphate) 2'-butyrate sodium
bucladesine (sodium)
HY-B0764
SCHEMBL93707
MLS006010661
dibutyryl-camp, sodium salt
n6,o2'-dibutyryl adenosine 3',5'-cyclic monophosphate sodium salt
sodium;[(4ar,6r,7r,7ar)-6-[6-(butanoylamino)purin-9-yl]-2-oxido-2-oxo-4a,6,7,7a-tetrahydro-4h-furo[3,2-d][1,3,2]dioxaphosphinin-7-yl] butanoate
CHEMBL1522836
AC-31719
AKOS024456413
HMS3403A19
OPERA_ID_1706
mfcd00005843
bucladesine (sodium salt)
dibutyryl-camp sodium salt
dc2797
CHEBI:31313
n6,2'-o-dibutyryladenosine 3',5'-cyclic monophosphate sodium salt
sodium (4ar,6r,7r,7ar)-6-(6-butyramido-9h-purin-9-yl)-7-(butyryloxy)tetrahydro-4h-furo[3,2-d][1,3,2]dioxaphosphinin-2-olate 2-oxide
adenosine 3',5'-cyclic monophosphate, n,o2'-dibutyryl-, sodium salt - cas 16980-89-5
dibutyryl camp (sodium salt);dbcamp (sodium salt)
HMS3412M09
n-6,o-2'-dibutyryladenosine cyclic 3',5'-monophosphate sodium salt
Q27259467
4h-furo[3,2-d]-1,3,2-dioxaphosphorin, adenosine deriv
BP-58715
CHEBI:175636
142628-53-3
macrocarpal c
5-[(1r)-1-((11s)-3,3,11-trimethyl-7-methylenetricyclo[6.3.0.0<2,4>]undec-11-yl)-3-methylbutyl]-2,4,6-trihydroxybenzene-1,3-dicarbaldehyde
5-[(1r)-1-[(1ar,4ar,7s,7ar,7br)-1,1,7-trimethyl-4-methylene-1a,2,3,4a,5,6,7a,7b-octahydrocyclopropa[h]azulen-7-yl]-3-methyl-butyl]-2,4,6-trihydroxy-benzene-1,3-dicarbaldehyde
CHEMBL466994
5-((1r)-1-((11s)-3,3,11-trimethyl-7-methylenetricyclo(6.3.0.0(2,4))undec-11-yl)-3-methylbutyl)-2,4,6-trihydroxybenzene-1,3-dicarbaldehyde
SCHEMBL136282
DTXSID50162107
AKOS032948488
macrocarpal c/g
FS-10349

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Of nine test chemicals, acrylamide and N-hydroxymethylacrylamide were most toxic compared with others on the basis of ED50 value."( Cytotoxicity of acrylamide and related compounds to mouse neuroblastoma and rat schwannoma cells.
Hashimoto, K; Hayashi, M; Miki, N; Tanii, H, 1988
)
0.27
" This system has been applied to the quantitation of toxic activities that disrupt cell monolayers and their neutralization."( A semi-automated system for the assessment of toxicity to cultured mammalian cells based on detection of changes in staining properties.
Barer, MR; Drasar, BS; Mann, GF, 1986
)
0.27
"5 X 10(-3) M was toxic to all cell lines."( Lymphotoxic activity of methyl prednisolone in vitro--I. Comparative toxicity of methyl prednisolone in human cell lines of B and T origin.
Bell, JB; Hall, JG; Hobbs, SM; Jackson, E; Millar, BC, 1987
)
0.27
" We examined in primary cultured hippocampal neurons whether the protein kinases PKC, PKA, CaM-II, and cGMP-dependent protein kinase modified the toxic effects of anoxia and NO."( Protein kinases modulate the sensitivity of hippocampal neurons to nitric oxide toxicity and anoxia.
Boniece, IR; Maiese, K; Skurat, K; Wagner, JA, 1993
)
0.29
" Similar (protective) effect had also verapamil, calcium channel blocker, when given in non toxic doses and at the same time schedule as db-cAMP Combination of db-cAMP and verapamil had not synergistic effect in protection from D-GalN+LPS hepatotoxicity; the survival of mice was similar to that seen in protection caused by each agent alone."( The effect of cyclic adenosine monophosphate (cAMP) on acute liver toxicity in mice induced by D-galactosamine and lipopolysaccharide.
Cavar, I; Culo, F; Erceg, D; Kelava, T; Pasalić, M, 2010
)
0.36

Compound-Compound Interactions

ExcerptReferenceRelevance
"Dibutyryl cyclic AMP was administered to 7 cases with hepatocellular carcinoma and its tumor thrombosis in portal vein, combined with intraarterial infusion of Mitomycin C or Adriamycin with implanted reservoir."( [Effect of dibutyryl cyclic AMP in the treatment of hepatocellular carcinoma--intraarterial infusion therapy combined with anticancer agent for hepatocellular carcinoma with portal vein thrombosis].
Fukui, H; Kitagami, K; Matsumoto, M; Nakano, H; Nakayama, M; Okamoto, Y; Tsujii, T, 1992
)
0.28
" To analyse these effects and to delineate new combination strategies in immunotherapy, we have investigated immunomodulatory properties of PTX in combination with dexamethasone (DEX) or cyclosporin A (CsA)."( Pentoxifylline exerts synergistic immunomodulatory effects in combination with dexamethasone or cyclosporin A.
Ernst, M; Funk, JO; Schönharting, MM; Zabel, P, 1995
)
0.29
"In the present work, nerve growth factor (NGF) was used in combination with the calcium ionophore, ionomycin or dibutyryl cyclic AMP (dbcAMP), to study the connection between neuronal differentiation and extracellular signal-regulated kinase (ERK) activation of PC12 rat pheochromocytoma cells expressing a dominant negative, Ha-Ras Asn17 protein."( Nerve growth factor in combination with second messenger analogues causes neuronal differentiation of PC12 cells expressing a dominant inhibitory Ras protein without inducing activation of extracellular signal-regulated kinases.
Boglári, G; Szeberényi, J, 2001
)
0.31

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" The data also indicate that some factors may act specifically on BP synthesis, without affecting IGF synthesis, and in this way play a role in regulating the bioavailability of the IGFs."( FGFs stimulate IGF binding protein synthesis without affecting IGF synthesis in rat astroblasts in primary culture.
Binoux, M; Janet, T; Labourdette, G; Loret, C; Schneid, H, 1991
)
0.28
" It is appropriate to evaluate the bioavailability in damaged skin models for a drug, such as DBcAMP, which is used in the treatment of skin ulcer."( Effect of vehicles on percutaneous absorption of bucladesine (dibutyryl cyclic AMP) in normal and damaged rat skin.
Mafune, E; Takahashi, M; Takasugi, N, 1995
)
0.29
" The beta-adrenergic antagonist sotalol (10-4 M) reduced LL absorption rate from -1."( The regulation of lung liquid absorption by endogenous cAMP in postnatal sheep lungs perfused in situ.
Benjamin, AR; Stephens, RH; Walters, DV, 1998
)
0.3
" However, the mechanism and the participating molecules that regulate the bioavailability of TJ proteins are entirely unknown."( cAMP perturbs inter-Sertoli tight junction permeability barrier in vitro via its effect on proteasome-sensitive ubiquitination of occludin.
Lee, WM; Lui, WY, 2005
)
0.33

Dosage Studied

ExcerptRelevanceReference
" A dose-response analysis was performed and the results indicate that 1 mug/ml of parathyroid hormone was the minimal effective dose."( Effects of parathyroid hormone on H+ and NH+4 excretion in toad urinary bladder.
Frazier, LW, 1976
)
0.26
" When the testicular tissue pieces were incubated with different doses of HCG or dibutyryl cAMP and testosterone production was measured, identical dose-response curves for old and young tissue were obtained."( In vitro and in vivo studies on Leydig cell function in old rats.
Geiss, M; Pirke, KM; Vogt, HJ, 1978
)
0.26
" The dose-response effects of IBX on growth inhibition of malignant cells in mixed cultures appear to correlate well with its ability to elevate cAMP levels."( Modulation of cellular interactions between C3H/10T1/2 cells and their transformed counterparts by phosphodiesterase inhibitors.
Bertram, JS, 1979
)
0.26
" A dose-response relationship of PGE1 (0."( Compartive behavioral effects of dibutyryl cyclic AMP and prostaglandin E1 in mice.
Olson, JW; Weiner, M, 1975
)
0.25
" Intravenous injection of parathyroid hormone over the dosage range from 1-50 mug/kg resulted in a dose-dependent increase in phosphate and cyclic AMP excretion with both D-fed and D-deficient thyroparathyroidectomized rats."( Renal adenylate cyclase and the interrelationship between parathyroid hormone and vitamin D in the regulation of urinary phosphate and adenosine cyclic 3',5'-monophosphate excretion.
Anast, CS; Forte, LR; Nickols, GA, 1976
)
0.26
" Lithium significantly inhibited the phosphaturic response to PTH at a dosage of 90 mug/kg/hr but did not affect the response to 30 mug/kg/hr."( Selective lithium inhibition of hormonal phosphaturic responses.
Steele, TH, 1976
)
0.26
" Based on a dose-response analysis, 1-methyl-3-isobutylxanthine was 200 times more potent than aminophylline."( Insect prothoracic glands: a role for cyclic AMP in the stimulation of alpha-ecdysone secretion.
Bollenbacher, WE; Gilbert, LI; Vedeckis, WV,
)
0.13
" The ability of dibutyryl cyclic AMP to elevate ornithine decarboxylase activity was found to be concentration-dependent, and a dose-response relationship very similar to that for the induction of tyrosine aminotransferase by dibutyryl cyclic AMP was observed in these cells."( Induction of ornithine decarboxylase in Reuber H35 rat hepatoma cells.
Byus, CV; Russel, DH; Wicks, WD,
)
0.13
" Dose-response curves studies suggested that inosine, but not uridine, has a common receptor site with epinephrine in adipose tissue."( Effects of uridine and inosine on glucose metabolism in skeletal muscle and activated lipolysis in adipose tissue.
Hait, G; Kypson, J, 1976
)
0.26
" The dichotomy in the dose-response pattern between the two parameters indicated that the effect of high TSH concentrations on the release was induced at a step beyond cAMP accumulation."( The mechanism of damping of the serum thyroxine and triidothyronine levels caused by increasing thyrotropin dosage in mice.
Gafni, M; Gross, J; Saddok, C; Sirkis, N, 1977
)
0.26
" The histamine respiratory dose-response curve was shifted to the left in the presence of the phosphodiesterase inhibitor aminophylline."( Potentiation by carbachol and aminophylline of histamine- and db-cAMP-induced parietal cell activity in isolated gastric glands.
Berglindh, T, 1977
)
0.26
" DbcAMP (in each dosage administered) decreased, NA content of cortex and of pons with medulla oblongata."( Influence of dibutyryl cyclic AMP on the level of catecholamines and 5-hydroxytryptamine in discrete areas of rat brain.
Drybański, A; Herman, ZS; Kmieciak-Kolada, K, 1977
)
0.26
" In this in vitro system another cell activity, T4 synthesis, was stimulated in an essentially identical fashion by TSH and dibutyryl cyclic AMP (time course of action, dose-response relationship)."( Thyroxine secretion by isolated hog thyroid cells: a cyclic AMP independent pathway.
Mornex, R; Munari, Y; Rostagnat, A; Rousset, B, 1977
)
0.26
" The dose-response pattern for the cAMP-stimulated decrease in enzyme activities parallels the pattern for the cAMP-stimulated, cell cycle-specific (G1) growth arrest of S49 cells."( Cyclic AMP-dependent protein kinase mediates a cyclic AMP-stimulated decrease in ornithine and S-adenosylmethionine decarboxylase activities.
Fenno, J; Insel, PA, 1978
)
0.26
" In addition, calcium effects on PTH-sensitive adenylate cyclase follow a different calcium dose-response than PTH-like metabolic changes."( Induction of metabolic changes and down regulation of bovine parathyroid hormone-responsive adenylate cyclase are dissociable in isolated osteoclastic and osteoblastic bone cells.
Wong, GL, 1979
)
0.26
" The dose-response relationships and kinetics of histamine and BK-A release from antigen-challenged peripheral leukocytes are similar."( Anaphylactic relase of a basophil kallikrein-like activity. II. A mediator of immediate hypersensitivity reactions.
Lichtenstein, LM; Newball, HH; Talamo, RC, 1979
)
0.26
" They demonstrate that taurocholate synthesis is increasing rapidly during the final stages of gestation and show that cortisol augments taurocholate synthesis in a dose-response pattern."( Synthesis of taurocholate by rat fetal liver in organ culture: effects of cortisol in vitro.
Graham, TO; Lester, R; Little, JM; Van Thiel, DH, 1979
)
0.26
" A beta 1-pattern was seen in both regions when lipolysis dose-response curves were arranged in order of potency."( Mechanisms for differences in lipolysis between human subcutaneous and omental fat cells.
Arner, P; Hellmér, J; Marcus, C; Sonnenfeld, T, 1992
)
0.28
" Steroidogenesis was dose-dependently increased by both gonadotrophins, with LH having the significantly greater effect over the entire dose-response range (1-100 micrograms/l)."( Mediation of gonadotrophin-stimulated growth and differentiation of human granulosa cells by adenosine-3',5'-monophosphate: one molecule, two messages.
Baird, DT; Hillier, SG; Yong, EL, 1992
)
0.28
"It was recently observed that treatment of patients with a high dosage of human interleukin (IL-2) resulted in suppression of plasma concentrations of testosterone."( Direct and indirect effects of murine interleukin-2, gamma interferon, and tumor necrosis factor on testosterone synthesis in mouse Leydig cells.
Bishop, DK; Cardoso de Sousa, JC; Dacosta, N; Meikle, AW; Samlowski, WE,
)
0.13
" Increasing concentrations of LH stimulated both inhibin and testosterone immunoactivity in the incubation media over a similar dose-response range, with a 2- to 4-fold rise in I-inhibin secretion at maximal doses of LH."( The role of calcium in luteinizing hormone/human chorionic gonadotrophin stimulation of Leydig cell immunoactive inhibin secretion in vitro.
de Kretser, DM; Hedger, MP; Risbridger, GP; Simpson, BJ, 1991
)
0.28
" Its dose-response ran roughly parallel to that of a bafilomycin A1-induced lysosomal pH increase."( Induction of neurite outgrowth of PC12 cells by an inhibitor of vacuolar H(+)-ATPase, bafilomycin A1.
Ohkuma, S; Tamura, H, 1991
)
0.28
" The dose-response of pancreatic enzyme secretion to PACAP 38 was nearly identical with that to VIP."( The stimulatory effect of PACAP 38 on amylase release in dispersed rat pancreatic acini.
Kashimura, J; Kikuchi, Y; Koizumi, M; Shimosegawa, T; Toyota, T, 1991
)
0.28
" The dose-response curves for priming were identical to those for triggering of an increase in [Ca2+]i and pHi."( Stimulation and priming of human neutrophils by interleukin-8: cooperation with tumor necrosis factor and colony-stimulating factors.
Kasahara, T; Kitagawa, S; Matsushima, K; Saito, M; Takaku, F; Yuo, A, 1991
)
0.28
" The dose-response curve showed a peak action at 1 mM (Bu)2cAMP."( The mechanism of parathyroid hormone action on calcium reabsorption by the distal tubule.
Bouhtiauy, I; Brunette, MG; Lajeunesse, D, 1991
)
0.28
" Inhibition by cAMP was achieved by shifting the Ca2+ dose-response curve for secretion to the right; this was observed for the release of both specific granules (vitamin B12 binding protein) and azurophil granules (B-glucuronidase)."( Cyclic AMP inhibits secretion from electroporated human neutrophils.
Kuczynski, B; Smolen, JE; Stoehr, SJ, 1991
)
0.28
" Cyclic AMP-dependent kinase shifted the dose-response curve for inositol 1,4,5-trisphosphate-mediated Ca2+ release to the left by a factor of 4 and increased the total amount of Ca2+ released by 25%."( The mechanism for synergism between phospholipase C- and adenylylcyclase-linked hormones in liver. Cyclic AMP-dependent kinase augments inositol trisphosphate-mediated Ca2+ mobilization without increasing the cellular levels of inositol polyphosphates.
Bird, GS; Burgess, GM; Obie, JF; Putney, JW, 1991
)
0.28
" Furthermore, Ti/CD3 stimulation did not influence the kinetics or dose-response of GTP[S]-induced inositol phosphate production, suggesting that the Ti/CD3 complex does not regulate guanine nucleotide exchange on the G protein pool stimulated by GTP[S]."( An analysis of the role of guanine nucleotide binding proteins in antigen receptor/CD3 antigen coupling to phospholipase C.
Cantrell, DA; Graves, JD, 1991
)
0.28
" An increase in GFAP content which did not correlate with drug dosage or DNA synthesis was noted in the MTX-treated cultures."( Effect of methotrexate on glial fibrillary acidic protein content of astrocytes in primary culture.
Bruce-Gregorios, JH; Chen, MG; Norenberg, MD; Soucy, DM, 1991
)
0.28
" Dose-response depression in both hCG- and db-cAMP-stimulated T production were seen with Cd2+, Co2+, Cu2+, Hg2+, Ni2+, and Zn2+ treatment."( Effect of cadmium and other metal cations on in vitro Leydig cell testosterone production.
Laskey, JW; Phelps, PV, 1991
)
0.28
" However, dose-response experiments disclosed that the 50% effective concentration (EC50) was significantly higher in cells isolated from obese rats compared with lean ones (EC50 115 vs."( Defective metabolic effects of norepinephrine and insulin in obese Zucker rat brown adipose tissue.
Bukowiecki, LJ; Collet, A; Géloën, A; Marette, A, 1990
)
0.28
" Dose-response experiments revealed a K0."( Functional reconstitution of fMet-Leu-Phe receptor in Xenopus laevis oocytes.
Coats, WD; Navarro, J, 1990
)
0.28
"Phorbol myristate acetate (PMA) inhibits glucagon-stimulated cyclic AMP accumulation and shifts to the right the dose-response curve to glucagon for ureagenesis."( Modulation of glucagon actions by phorbol myristate acetate in isolated hepatocytes. Effect of hypothyroidism.
García-Sáinz, JA; Hernández-Sotomayor, SM; Hruby, VJ; Macías-Silva, M; Torres-Márquez, ME; Trivedi, D, 1990
)
0.28
" Although charcoal-extracted rat serum log dose-response relationships were nonparallel with the standard, serum displayed an apparent relative bioactivity of approximately 20% that of normal IF based on ED50 comparisons."( The quantification of steroidogenesis-stimulating activity in testicular interstitial fluid by an in vitro bioassay employing adult rat Leydig cells.
de Kretser, DM; Hedger, MP; Risbridger, GP; Robertson, DM, 1990
)
0.28
" The VIP/PHM-27 gene dosage was unchanged by Bt2cAMP and phorbol esters."( Synergistic stimulation of VIP/PHM-27 gene expression by cyclic AMP and phorbol esters in human neuroblastoma cells.
Hayakawa, Y; Nishizawa, M; Ohsawa, K; Okamoto, H; Yamagami, T; Yamamoto, H; Yanaihara, N, 1985
)
0.27
" A dose-response study showed that FSH pretreatment produced three separate effects on Sertoli cell steroidogenesis: an increased basal production of estrogen; a decreased maximal response when doses of 10 ng/ml FSH or higher were employed in the preincubation; and a decreased sensitivity of the Sertoli cell to FSH."( Effect of phosphodiesterase inhibitors on Sertoli cell refractoriness: reversal of the impaired androgen aromatization.
Conti, M; Geremia, R; Monaco, L; Stefanini, M, 1986
)
0.27
" In dose-response studies, PMA stimulated amylase release independently of db-cAMP, but potentiated the effect of carbachol."( Phorbol ester stimulates amylase secretion from rat parotid cells.
Ichida, T; Takuma, T, 1986
)
0.27
" Dose-response curves to K+ show that following differentiation, cells become more sensitive, releasing transmitter at lower K+ concentrations."( Nerve growth factor modulates the drug sensitivity of neurotransmitter release from PC-12 cells.
Kongsamut, S; Miller, RJ, 1986
)
0.27
" Dose-response curves to TG showed nonparallel increases in both parameters."( Stimulation of oxyntic and histaminergic cells in gastric mucosa by gastrin C-terminal tetrapeptide.
Michelangeli, F; Ruiz, MC, 1986
)
0.27
" Neither xanthine shifted the calcium dose-response when PMNs were activated with calcium ionophore."( Therapeutic concentrations of theophylline and enprofylline potentiate catecholamine effects and inhibit leukocyte activation.
Crowley, JJ; Cusack, BJ; Nielson, CP; Vestal, RE, 1986
)
0.27
" The dose-response curves of the strips from both strains for alpha-adrenoceptor stimulation with NA determined after pretreatment with CTX were comparable to those determined in the absence of timolol."( Role of stimulatory GTP-binding protein (Gs) in reduced beta-adrenoceptor coupling in the femoral artery of spontaneously hypertensive rats.
Asano, M; Masuzawa, K; Matsuda, T, 1988
)
0.27
" However, the inhibitory dose-response curves of adenylate cyclase to R-PIA, nicotinic acid, GTP, guanylylimidodiphosphate, and guanosine 5'-O-(3-thiotriphosphate) were unaltered by adrenalectomy, indicating that the inhibitory function of Gi is unimpaired by adrenalectomy."( Role of adenosine 3',5'-monophosphate and the Ri-receptor Gi-coupled adenylate cyclase inhibitory pathway in the mechanism whereby adrenalectomy increases the adenosine antilipolytic effect in rat fat cells.
de Mazancourt, P; Giot, J; Giudicelli, Y; Lacasa, D, 1989
)
0.28
" Dose-response experiments revealed that insulin stimulated D-glucose transport and 2-deoxyglucose uptake between 10(-11) and 10(-7) M with a maximal four- to sixfold stimulation."( Stimulation of glucose transport by insulin and norepinephrine in isolated rat brown adipocytes.
Bukowiecki, LJ; Marette, A, 1989
)
0.28
" Forskolin, cholera toxin and dibutyryl cyclic AMP also affected C6 cell proliferation, and the dose-response for decreasing the receptor was very similar to that observed for the inhibition of cell growth, suggesting a relationship between both phenomena."( Effects of cyclic AMP elevation on the levels of insulin receptors in glial C6 cells.
Aranda, A; Montiel, F; Pascual, A, 1989
)
0.28
" The epinephrine dose-response curve in the presence of 10(-8) M met-enkephalin was similar to that of epinephrine alone."( Combinative ligand-receptor interactions: effects of cAMP, epinephrine, and met-enkephalin on RAW264 macrophage morphology, spreading, adherence, and microfilaments.
Martin, SM; Petty, HR, 1989
)
0.28
"16E cells with a dose-response curve (ED50, 4 nM) very similar to that observed for the modulation of mucin secretion."( Functional VIP receptors in the human mucus-secreting colonic epithelial cell line CL.16E.
Augeron, C; Grasset, E; Laboisse, C; Laburthe, M; Maoret, JJ; Roumagnac, I; Rouyer-Fessard, C, 1989
)
0.28
" In slices from methamphetamine-treated rats, the dose-response curve for the dopamine hyperpolarization was shifted to the left of that seen in neurones from control rats by a factor of approximately 100."( Enhancement of dopamine actions on rat nucleus accumbens neurones in vitro after methamphetamine pre-treatment.
Higashi, H; Inanaga, K; Nishi, S; Uchimura, N, 1989
)
0.28
" Protein kinase inhibitors block v-Src- and v-Fps-induced 9E3 gene expression with the same dose-response curves seen for PKC agonist-induced 9E3 gene expression."( Evidence that v-src and v-fps gene products use a protein kinase C-mediated pathway to induce expression of a transformation-related gene.
Berg, KL; Foster, DA; Joseph, C; Qureshi, SA; Spangler, R, 1989
)
0.28
" Dose-response curves for inositol phospholipid synthesis stimulated by carbachol and CCK-8 in mouse acini were biphasic and superimposable with those of amylase secretion."( The effects of gamma-hexachlorocyclohexane on amylase secretion and inositol phospholipid metabolism in mouse pancreatic acini.
Crouch, MF; Roberts, ML, 1985
)
0.27
" Imipramine and nortriptyline also caused a rightward shift in the dose-response curve of histamine-induced cAMP generation."( Tricyclic antidepressants and acid secretory response of rabbit gastric cells.
Batzri, S, 1985
)
0.27
" Similar dose-response curves were obtained for the effect of AII on labeling of the 17."( Effects of atrial natriuretic peptide, angiotensin, cyclic AMP, and potassium on protein phosphorylation in adrenal glomerulosa cells.
Elliott, ME; Goodfriend, TL, 1987
)
0.27
" ANP shifted the dibutyryl cAMP dose-response curve slightly to the right but did not blunt the maximal aldosterone secretory response."( Effect of atrial natriuretic peptide on ACTH, dibutyryl cAMP, angiotensin II and potassium-stimulated aldosterone secretion by rat adrenal glomerulosa cells.
Brown, RD; Kem, DC; Schiebinger, RJ, 1988
)
0.27
" The dose-response relations for the increase in inositol phosphates closely paralleled the binding of carbachol to muscarinic receptors with a Km of 17 microM."( Stimulation of acid secretion and phosphoinositol production by rat parietal cell muscarinic M2 receptors.
Herz, A; Paumgartner, G; Pfeiffer, A; Rochlitz, H, 1988
)
0.27
" Neither GE 410 nor dbcGMP affected the ACH and histamine (His) response of the muscle strips but both antagonists shifted the dose-response curve of CCK 7 to the right, GE 410 (cholecystokinin antagonist) being a much more potent antagonist of CCK 7 as compared to dbcGMP."( Responses of guinea-pig gastric, ileal and gall bladder smooth muscle to desamino-cholecystokinin-octapeptide (CCK 7).
Henklein, P; Milenov, K; Nieber, K; Oehme, P; Rakovska, A, 1988
)
0.27
" Upon single administration to OB rats, rolipram at a dosage of 1 mg/kg body weight suppressed the muricide for 2 hr after its administration."( The effect of a selective phosphodiesterase inhibitor, rolipram, on muricide in olfactory bulbectomized rats.
Hara, K; Ikoma, Y; Kimura, K; Mizokawa, T; Oshino, N; Ueki, S; Yamamoto, T, 1988
)
0.27
" In vitro, the antagonist had no detectable agonist activity in the concentration used, had no effect on the maximal LH release which can be induced by LRH and shifted the dose-response line of LRH to the right, without changing its slope."( Effect of pretreatment of long-term ovariectomized rats with an LRH antagonist on LH release in vitro by LRH, elevated K+ or N6-monobutyryl adenosine 3',5'-monophosphate (mbcAMP) plus theophylline.
van Dieten, JA; van Rees, GP, 1985
)
0.27
" The dose-response curve to forskolin was bell-shaped (as is seen with TSH and LATS-B) with the ascending limb of the curve produced by 10(-13) M to 10(-12) M forskolin after a 3 min exposure time."( Forskolin stimulation of naphthylamidase in guinea pig thyroid sections detected with a cytochemical bioassay.
Ealey, PA; Ekins, RP; Kohn, LD; Marshall, NJ, 1985
)
0.27
" Subsequent LH responses to GnRH in those cells pretreated with GnRH and KCl were markedly reduced and the dose-response characteristics altered such that the curves were non-sigmoidal."( Increased gonadotrophin releasing hormone receptors on pituitary gonadotrophs: effect on subsequent LH secretion.
Clayton, RN; Naik, SI; Young, LS, 1985
)
0.27
" The first response, most notably involving a decrease in phosphatidylinositol content, was (a) observed at lower carbachol concentrations in dose-response studies, (b) inhibited by incubation in Ca2+-free media containing 1 mM EGTA, (c) associated with increases in inositol monophosphate production, and (d) provoked by all tissue secretagogues (carbachol, cholecystokinin, secretin, insulin, dibutyryl cAMP and the ionophore A23187), regardless of whether their mechanism of action primarily involved Ca2+ mobilization or cAMP generation."( Phosphatidylinositol hydrolysis and phosphatidylinositol 4',5-diphosphate hydrolysis are separable responses during secretagogue action in the rat pancreas.
Davis, JS; Farese, RV; Larson, RE; Orchard, JL; Sabir, MA, 1985
)
0.27
" In contrast, PGD2 acted as a weak and partial inhibitor in guinea-pig platelet aggregation, producing a bell-shaped dose-response relationship."( Interaction of prostaglandin D2 with prostacyclin, carbacyclin and the hydantoin prostaglandin, BW245C, in guinea-pig platelets.
Hamid, S; Whittle, BJ, 1985
)
0.27
" The extent of the parallel downward shift of the TRH dose-response curve was proportional to dose and duration of prior TRH exposure."( Modulation of thyrotrophin release from an intracellular pool by pre-exposure to thyrotrophin-releasing hormone and dibutyryl cyclic AMP.
Davis, JR; Sheppard, MC, 1986
)
0.27
" The dose-response curve for HL-60 differentiation was consistent with the published 50% inhibitory dose for inhibition of calmodulin-activated phosphodiesterase and with the calmodulin drug-binding potential of N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide and N-(4-aminobutyl)-5-chloro-2-naphthalenesulfonamide and their less active congeners, N-(6-aminohexyl)-1-naphthalenesulfonamide and N-(4-aminobutyl)-2-naphthalenesulfonamide."( Induction of myeloid differentiation of HL-60 cells with naphthalene sulfonamide calmodulin antagonists.
Branch, ME; Niedel, J; Sedwick, WD; Veigl, ML, 1986
)
0.27
" The dose-response curve for ODC induction by PTH was parallel to that of PTH-stimulated proteoglycan synthesis both in TPA-treated chondrocytes and in normal chondrocytes."( Comparison of inhibition by a tumor promoter (12-O-tetradecanoylphorbol-13-acetate) of expression of the differentiated phenotype of chondrocytes in rabbit costal chondrocytes in culture with inhibition by retinoic acid.
Enomoto, M; Fukuo, K; Kumahara, Y; Suzuki, F; Tajima, K; Takigawa, M, 1986
)
0.27
" The GH responses to the combined addition of TRH with all doses of GRF or DBcAMP were fully additive, causing parallel elevations of the dose-response curves."( TRH and GRF stimulate release of growth hormone through different mechanisms.
Szabo, M, 1986
)
0.27
" Pretreatment of cells with forskolin led to a parallel upward shift in the subsequent TRH dose-response curve, without a significant change in median effective dose or any change in cellular TSH content."( A modulatory role for cyclic AMP in the control of thyrotrophin release: studies with forskolin and dibutyryl cyclic AMP.
Davis, JR; Sheppard, MC, 1986
)
0.27
"01; analysis of variance) than that by similar preparations at 250 days because a dose-response relationship was not observed for incubations of luteal tissue with LH at 270 days of gestation."( Progesterone secretion by the bovine fetoplacental unit and responsiveness of corpora lutea to steroidogenic stimuli at two stages of gestation.
Hixon, JE; Pimentel, CA; Pimentel, SM; Wagner, WC; Weston, PG, 1986
)
0.27
" After chronic withdrawal of TSH from the growth medium, the magnitude of the response to NE is considerably reduced; however, there is no substantial shift in the dose-response curve."( Norepinephrine and thyroid-stimulating hormone induce inositol phosphate accumulation in FRTL-5 cells.
Alling, DW; Bone, EA; Grollman, EF, 1986
)
0.27
" Dose-response curves with partially purified preparations from human and rat origin yield parallel dose-response curves."( A Leydig cell stimulatory factor produced by human testicular tubules.
Cailleau, J; Verhoeven, G, 1987
)
0.27
" This inhibitory effect of low concentrations of ethacrynic acid could be surmounted by high, supramaximal dosage levels of vasopressin."( Effects of ethacrynic acid on the isolated collecting tubule.
Abramow, M, 1974
)
0.25
" Different dose-response curves were obtained for cytostasis and inhibition of [(3)H]-nucleoside incorporation, and changes in [(3)H]thymidine uptake were detected within 15 min of treatment with the inhibitors."( Rapid changes in nucleoside transport induced by growth inhibitors. Studies with neoplastic mast cells.
Lingwood, CA; Thomas, DB, 1974
)
0.25
" This phosphorylation of the receptor is dose-dependent with respect to isoproterenol and exhibits a dose-response curve coincidental with that for isoproterenol-induced desensitization of adenylate cyclase."( Desensitization of turkey erythrocyte adenylate cyclase. Beta-adrenergic receptor phosphorylation is correlated with attenuation of adenylate cyclase activity.
Caron, MG; Lefkowitz, RJ; Nambi, P; Peters, JR; Sibley, DR, 1984
)
0.27
" Dose-response curves were constructed for the inhibitory action of these agents on both cellular parameters and their interrelationship examined by regression analysis."( Effect of cyclic AMP on cellular contractility and DNA synthesis in chorioretinal fibroblasts maintained in collagen matrices.
Constable, IJ; Martin, CE; van Bockxmeer, FM, 1984
)
0.27
" N-OH-AAF dependent ODC induction displayed an almost linear dose-response in the dose range up to 94."( Induction of ornithine decarboxylase and augmentation of tyrosine aminotransferase activity by N-hydroxy-2-acetylaminofluorene and 2-acetylaminofluorene in rat liver. Influence of sex, retinylacetate, indomethacin, and pentachlorophenol.
Bakker, O; Bisschop, A; Meerman, JH; Stavenuiter, JF; van der Heijden, CA; van Wijk, R, 1984
)
0.27
" The order of potency and effective dosage range to induce the behavioral alterations were, in descending order, rolipram (0."( Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors.
Wachtel, H, 1982
)
0.26
" In dose-response studies with the cAMP analog, dibutyryl cyclic AMP (dbcAMP), we found that the RPE pigment did not exhibit intermediate states of aggregation with increasing concentrations of dbcAMP but instead changed abruptly from the fully light-adapted to the fully dark-adapted retinomotor positions between 10 microM and 50 microM exogenous dbcAMP concentrations."( Retinomotor pigment migration in the teleost retinal pigment epithelium. II. Cyclic-3',5'-adenosine monophosphate induction of dark-adaptive movement in vitro.
Basinger, S; Burnside, B, 1983
)
0.27
" Atropine (100 microM) produced a rightward shift of the dose-response curve, indicating the presence of a muscarinic receptor."( Regulation of pepsinogen release from canine chief cells in primary monolayer culture.
Amirian, DA; Ayalon, A; Sanders, MJ; Soll, AH, 1983
)
0.27
" At a low dosage of AXM (0."( Effect of acetoxycycloheximide and dibutyryladenosine cyclic 3':5'-monophosphate on axonal regeneration in the goldfish optic nerve.
Grafstein, B; McQuarrie, IG, 1983
)
0.27
" Significantly, the dose-response curves for isoproterenol stimulation of lipolysis and respiration were both shifted by adenosine to higher agonist concentrations by the same order of magnitude, providing additional evidence for a tight coupling between lipolysis and respiration."( Control of brown adipose tissue lipolysis and respiration by adenosine.
Bukowiecki, LJ; Szillat, D, 1983
)
0.27
" The dose-response curves to ACh showed nonparallel increases in H+ secretion and histamine release."( Evidence for a direct action of acetylcholine on the gastric oxyntic cell of the amphibian.
Michelangeli, F; Ruiz, MC, 1984
)
0.27
" The dose-response curve for cAMP formation stimulated by epinephrine was shifted 1 log unit to the right in uremic muscle and adenylyl cyclase stimulation by epinephrine was shifted 1 log unit."( Skeletal muscle amino acid metabolism in chronic uremia.
Garber, AJ; Maillet, C, 1980
)
0.26
" Progesterone decreased the secretion of hCG in a dose-response manner (r = -0."( Suppression of human chorionic gonadotropin by progestational steroids.
Dickson, LR; Jawad, MJ; Wilson, EA, 1980
)
0.26
" The dose-response to ionophore A23187 (1."( Role of calcium in antral gastrin release.
Harty, RF; Maico, DG; McGuigan, JE, 1981
)
0.26
" As shown by dose-response studies, VIP is by far the most effective inducer (Ka equals 4 x 10(-10) M) of the cyclic AMP phosphodiesterase activity; partial activation of the enzyme is obtained by 3 x 10(-7) M secretin, 10(-5) M isoproterenol and 10(-5) M PGE1; PGE2 and epinephrine are without effect."( Parallel activation of cyclic AMP phosphodiesterase and cyclic AMP-dependent protein kinase in two human gut adenocarcinoma cells (HT 29 and HRT 18) in culture, by vasoactive intestinal peptide (VIP) and other effectors activating the cyclic AMP system.
Ahmed, OA; Mangeat, P; Marchis-Mouren, G; Marvaldi, J, 1981
)
0.26
" Dose-response curves for glycosylation in response to 8-Br-cAMP and GnRH were parallel."( Differential effects of cyclic nucleotide analogues and GnRH on LH synthesis and release.
Jackson, GL; Liu, TC, 1981
)
0.26
"To investigate the mechanism of intracellular transmission of three representative stimuli for gastric acid secretion, the dose-response relations of cyclic nucleotides accompanied by acid secretion stimulated by histamine, pentagastrin and bethanechol were comparatively studied using an in vitro preparation of guinea pig gastric mucosa surviving with a constant potential difference and acid secretion sensitive to amytal."( Cyclic nucleotide response to acid-secreting stimuli in guinea pig gastric mucosa in vitro.
Matsumoto, H; Miyoshi, A; Ohe, K; Shirakawa, T, 1981
)
0.26
" A dose-response relationship could be demonstrated in propranolol treated dogs by administering DB-cAMP at 10, 100 and 1000 micrograms/min at low but not at control blood pressure."( Conditions for stimulation of renin release by cyclic AMP in anaesthetized dogs.
Eide, I; Holdaas, H; Kiil, F; Langård, O, 1981
)
0.26
" Bile production was, however, increased by supplementary glucagon infusion, when a submaximal dosage of insulin was given."( Interaction of insulin, glucagon, and DBcAMP on bile acid-independent bile production in the rat.
Larsen, JA; Thomsen, OO, 1982
)
0.26
" A role for cAMP-dependent protein kinase activation in regulating mucin secretion was strongly suggested by the following: (1) the kinase activity ratio increased rapidly after beta-adrenergic receptor stimulation; (2) dose-response relationship of the kinase activation following beta-adrenergic receptor activation correlated with isoproterenol induced mucin release; (3) termination of beta-adrenergic mediated mucin secretion caused a rapid decrease in the kinase activity ratio; (4) dibutyryl cyclic AMP stimulation caused an increase in the kinase ratio; whereas (5) pure cholinergic and pure alpha-adrenergic receptor stimulation had no effect on endogenous kinase activity."( Role of cyclic AMP-dependent protein kinase activation in regulating rat submandibular mucin secretion.
Barzen, KA; Deisher, LM; Quissell, DO, 1983
)
0.27
" The present experiments demonstrated that this effect, previously termed "priming", was accompanied by a 60% increase in the volume of the PC12 cells, and that the dose-response curves for NGF-mediated induction of fiber outgrowth and for the increase in cell volume were very similar."( Relationship between NGF-mediated volume increase and "priming effect" in fast and slow reacting clones of PC12 pheochromocytoma cells. Role of cAMP.
Heumann, R; Kachel, V; Thoenen, H, 1983
)
0.27
" CCK-27-32-NH2 caused a parallel rightward shift in the dose-response curve for the stimulation of amylase secretion caused by cholecystokinin and inhibited binding of 125I-labeled cholecystokinin to pancreatic acini."( Cholecystokinin-27-32-amide. A member of a new class of cholecystokinin receptor antagonists.
Briet, C; Gardner, JD; Jensen, RT; Martinez, J; Spanarkel, M, 1983
)
0.27
" The dose-response curve was similar to most other nerve growth factor-induced responses in PC12 cells."( Regulation of the multiple forms of dopamine beta-hydroxylase by nerve growth factor, dexamethasone, and dibutyryl cyclic AMP in the PC12 pheochromocytoma cell line.
Goldstein, M; Greene, LA; Sabban, EL, 1983
)
0.27
" dosing of SCH 28080, 1 mg/kg, indicating that the antisecretory action of SCH 28080 was not secondary to changes in gastric blood flow."( Studies on the mechanisms of the antisecretory and cytoprotective actions of SCH 28080.
Barnett, A; Casciano, C; Chiu, PJ; Long, JF; Tetzloff, G, 1983
)
0.27
" They are further discussed with respect to a better understanding of dose-response curves for chemical and physiological inactivation."( Effect of irradiated dib-cAMP on the tonic and phasic activity of human myometrium.
Klöter, H; Schachinger, L; Schippel, C; Srivastava, A, 1983
)
0.27
" o-GH and o-PRL induced marginal increases in production and p-ACTH had a very modest inverse dose-response effect."( Estradiol-17 beta and 17 alpha, 20 beta-dihydroxy-4-pregnen-3-one production by isolated ovarian follicles of amago salmon (Oncorhynchus rhodurus) in response to mammalian pituitary and placental hormones and salmon gonadotropin.
Nagahama, Y; Ueda, H; Young, G, 1983
)
0.27
" Time course and insulin dose-response experiments indicate an additional proximal alteration."( beta-Adrenergic desensitization by chronic insulin exposure in 3T3-L1 cultured adipocytes.
Olansky, L; Pohl, SL, 1984
)
0.27
" In dose-response studies, the contents of these phospholipids and pyruvate dehydrogenase activity increased in parallel in response to increasing concentrations of insulin."( The mechanism of action of insulin on phospholipid metabolism in rat adipose tissue. Requirement for protein synthesis and a carbohydrate source, and relationship to activation of pyruvate dehydrogenase.
Barnes, D; Farese, RV; Larson, RE; Sabir, MA; Trudeau, WL, 1984
)
0.27
" The dose-response curves of induction of HGF secretion by cholera toxin and forskolin were nearly parallel with those of the intracellular cAMP levels."( Expression of hepatocyte growth factor is up-regulated through activation of a cAMP-mediated pathway.
Gohda, E; Iwao, M; Kataoka, H; Matsunaga, T; Takebe, T; Wu, YL; Yamamoto, I, 1994
)
0.29
" However, the dose-response curve for pentagastrin in the presence of ranitidine plus IBMX was similar to that obtained in the absence of IBMX."( Gastrin action on aminopyrine accumulation in isolated pig parietal cells requires cAMP.
Cabero, JL; Li, ZQ; Mårdh, S, 1993
)
0.29
"0 mg/kg) accelerated mucociliary activity (at the highest dosage tested, 24."( Cyclic adenosine monophosphate stimulation of mucociliary activity in the upper airways in vivo.
Cervin, A; Dolata, J; Lindberg, S; Mercke, U, 1995
)
0.29
" In the presence of 200 microM Rp-cAMPS, the dose-response curves of the dopamine D1 receptor agonists SKF 38393 and fenoldopam were shifted to the left and maximal agonist responses were markedly increased."( Inhibition of dopamine agonist-induced phosphoinositide hydrolysis by concomitant stimulation of cyclic AMP formation in brain slices.
Friedman, E; Undie, AS, 1994
)
0.29
" The dose-response relationship yielded a bell-shaped curve with a peak at 1 microM."( Enhancement of neuronal calcium channel currents by the nootropic agent, nefiracetam (DM-9384), in NG108-15 cells.
Watabe, S; Yoshii, M, 1994
)
0.29
" Ethanol stimulated iodide uptake in a dose-response manner in TSH-free medium."( Ethanol has thyrotropin-like activity in cultured porcine thyroid follicles.
Nasu, M; Sugawara, M, 1993
)
0.29
" While there was a clear effect of dBcAMP-induced differentiation on the maximal NE-induced PI-response, no effect on the dose-response relationship was detectable, resulting in similar EC50-values for astrocytes cultured either in the absence or presence of dBcAMP."( Dibutyryl cyclic AMP-induced morphological differentiation of rat brain astrocytes increases alpha 1-adrenoceptor induced phosphoinositide breakdown by a mechanism involving protein synthesis.
Fahrig, T; Sommermeyer, H, 1993
)
0.29
" The dose-response curve was bell-shaped."( Pituitary adenylate cyclase-activating polypeptide protects rat-cultured cortical neurons from glutamate-induced cytotoxicity.
Hirai, A; Morio, H; Saito, Y; Tamura, Y; Tatsuno, I, 1996
)
0.29
" Theophylline, an antagonist of P1 adenosine receptor, completely reversed the effect of adenosine on the furosemide-sensitive ATPase activity in a dose-response manner."( Effect of adenosine on the ouabain-insensitive Na+-ATPase activity from basolateral membrane of the proximal tubule.
Caruso-Neves, C; Chagas, C; Francisco-Pedro, LG; Lopes, AG; Souza, LP, 1997
)
0.3
" Spontaneous Ca2+ oscillations were entirely suppressed by microinjection of heparin (25 microM final intracellular concentration), an antagonist of inositol trisphosphate (IP3) receptor, whereas fertilization-induced Ca2+ oscillations were only partially inhibited by heparin even at a high dosage of 600 microM."( Spontaneous and fertilization-induced Ca2+ oscillations in mouse immature germinal vesicle-stage oocytes.
Deng, MQ; Huang, XY; Sun, FZ; Tang, TS, 1998
)
0.3
" We used primary cerebrocortical cell cultures from fetal mice to examine the dose-response and time-course of ppSom gene expression in response to the cyclic-AMP analogs, dibutyrl-cAMP (dbcAMP), and 8-bromo-cAMP (8-BrcAMP)."( Regulation of the preprosomatostatin gene by cyclic-AMP in cerebrocortical neurons.
Capone, G; Choi, C; Vertifuille, J, 1998
)
0.3
"Reciprocal dose-response curves for the effects of the two hormones in intestine and liver were demonstrated: glucagon 37 was one order of magnitude more potent than glucagon 29 in increasing intestinal absorption of glucose via the SGLT1."( Enteric glucagon 37 rather than pancreatic glucagon 29 stimulates glucose absorption in rat intestine.
Hunger, A; Jungermann, K; Scholtka, B; Stümpel, F, 1998
)
0.3
" The dose-response curves for ATP4- show that IBaL and IBaN proportionally increased with ATP4- concentrations up to 1 mM at three different Mg2+ concentrations."( Regulation of L- and N-types of Ca2+ channels by intracellular ATP4- in frog dorsal root ganglion neurons.
Seyama, I; Yamaoka, K; Yuki, T, 1999
)
0.3
"1 mM)-stimulated AP accumulation, which was dose-dependently inhibited by higher concentrations of TPA with corresponding shifts in the dose-response curve for carbachol-stimulated AP accumulation."( Effects of phorbol ester treatment on dibutyryl cyclic adenosine-5' monophosphate- and carbachol-stimulated aminopyrine accumulation in isolated rat parietal cells.
Kopp, R; Pfeiffer, A, 2000
)
0.31
" The Ca(2+) response occurred in all-or-none fashion and the half-maximal dosage of U50488H (812."( Cyclic AMP regulates the calcium transients released from IP(3)-sensitive stores by activation of rat kappa-opioid receptors expressed in CHO cells.
Allen, CN; Grandy, DK; Ikeda, M; Nelson, CS; Shinagawa, H; Shinoe, T; Sugiyama, T; Yoshioka, T, 2001
)
0.31
" Results showed that progesterone production gradually increased as the dosage of combined water and ethanol extracted CS increased, and there was a statistically significant difference in progesterone production stimulated by 20 mg/ml of CS extracts compared to the control."( Effects of extracted Cordyceps sinensis on steroidogenesis in MA-10 mouse Leydig tumor cells.
Chen, CF; Chuang, YM; Huang, BM; Leu, SF, 2000
)
0.31
" These data suggest that lead directly inhibited steroidogenesis by decreasing StAR protein expression and the activities of P450scc and 3beta-HSD enzymes with a dose-response trend in MA-10 cells."( The inhibitory effects of lead on steroidogenesis in MA-10 mouse Leydig tumor cells.
Huang, BM; Lai, HY; Liu, MY; Tsai, ML; Yang, BC; Yang, HY, 2001
)
0.31
" Although there was a trend towards a dose-response effect, mean StAR mRNA levels were only significantly affected by the highest concentration of ACTH used (1,500 ng/mL), which induced a less than 2-fold increase in StAR transcripts."( Effects of ACTH and cAMP on steroidogenic acute regulatory protein and P450 11beta-hydroxylase messenger RNAs in rainbow trout interrenal cells: relationship with in vitro cortisol production.
Hagen, IJ; Kusakabe, M; Young, G, 2006
)
0.33
" Cell pre-treatment with the IL-1sR antagonist produced a rightward shift of IL-1 dose-response effect with a corresponding decrease in IL-1 potency."( Synergistic effects of cAMP-dependent signalling pathways and IL-1 on IL-6 production by H19-7/IGF-IR neuronal cells.
Bergamaschi, A; Corsi, M; Garnier, MJ, 2006
)
0.33
"For normal sperm with normal sperm-ZP binding, both PMA and dbcAMP significantly enhanced sperm-ZP binding in a dose-response manner."( Enhancement of sperm-zona pellucida (ZP) binding capacity by activation of protein kinase A and C pathways in certain infertile men with defective sperm-ZP binding.
Baker, HW; Liu, DY; Liu, ML, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
agonistSubstance which binds to cell receptors normally responding to naturally occurring substances and which produces a response of its own.
vasodilator agentA drug used to cause dilation of the blood vessels.
cardiotonic drugA drug that has a strengthening effect on the heart or that can increase cardiac output.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
butyrate esterAny carboxylic ester where the carboxylic acid component is butyric acid.
3',5'-cyclic purine nucleotide
butanamidesA fatty amide derived based on a butanamide skeleton and its substituted derivatives.
3',5'-cyclic purine nucleotide
sesquiterpenoidAny terpenoid derived from a sesquiterpene. The term includes compounds in which the C15 skeleton of the parent sesquiterpene has been rearranged or modified by the removal of one or more skeletal atoms (generally methyl groups).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
estrogen nuclear receptor alphaHomo sapiens (human)Potency16.93010.000229.305416,493.5996AID743069
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency23.71010.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency23.71010.011912.222168.7989AID651632
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency12.58930.003245.467312,589.2998AID2517
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency11.58210.004110.890331.5287AID504467
vasopressin V1b receptorHomo sapiens (human)Potency1.37610.194416.018043.6206AID492948
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency10.00000.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency10.00000.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency10.00000.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency22.38720.004611.374133.4983AID624297
relaxin receptor 1 isoform 1Homo sapiens (human)Potency0.71960.038814.350143.6206AID2676; AID489012; AID492949
relaxin receptor 2 isoform 1Homo sapiens (human)Potency1.37610.048815.980148.9431AID489043
neuropeptide S receptor isoform AHomo sapiens (human)Potency0.32280.015812.3113615.5000AID1461; AID1489; AID1491; AID2567; AID2568
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cAMP-dependent protein kinase type I-alpha regulatory subunitBos taurus (cattle)EC50 (µMol)4.47700.06804.12407.8270AID504887; AID504896
cAMP-dependent protein kinase type II-beta regulatory subunitHomo sapiens (human)EC50 (µMol)5.37800.08852.54055.3780AID504888; AID504893
cAMP-dependent protein kinase catalytic subunit beta isoform 1Mus musculus (house mouse)EC50 (µMol)4.47700.06804.12407.8270AID504887; AID504896
cAMP-dependent protein kinase catalytic subunit beta isoform 3Homo sapiens (human)EC50 (µMol)5.37800.08852.54055.3780AID504888; AID504893
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (77)

Assay IDTitleYearJournalArticle
AID377220Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA2000Journal of natural products, Sep, Volume: 63, Issue:9
In vitro antiinflammatory effects of neolignan woorenosides from the rhizomes of Coptis japonica.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID614287Antimicrobial activity against Mucor mucedo IFO 7684 at 100 uM after 24 hrs by broth microdilution method2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Antifungal thiopeptide cyclothiazomycin B1 exhibits growth inhibition accompanying morphological changes via binding to fungal cell wall chitin.
AID377224Inhibition of IL2-dependent mouse CTLL2 cell proliferation after 48 hrs by MTT assay2000Journal of natural products, Sep, Volume: 63, Issue:9
In vitro antiinflammatory effects of neolignan woorenosides from the rhizomes of Coptis japonica.
AID1631748Neuroprotective activity in Sprague-Dawley rat DA neuron death PD model assessed as survival of Th immunopositive cells at 1 mM after 10 days by immunofluorescence assay relative to control2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
New 6-Aminoquinoxaline Derivatives with Neuroprotective Effect on Dopaminergic Neurons in Cellular and Animal Parkinson Disease Models.
AID614290Induction of morphological changes in Mucor mucedo IFO 7684 assessed as thickening of hyphae at 100 uM after 24 hrs by microscopic analysis2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Antifungal thiopeptide cyclothiazomycin B1 exhibits growth inhibition accompanying morphological changes via binding to fungal cell wall chitin.
AID1174514Antiproliferative activity at Sprague-Dawley rat DA neurons assessed as reduction of [3H]-thymidine incorporation at 1 mM after 8 days by liquid scintillation spectrometry2015European journal of medicinal chemistry, Jan-07, Volume: 89Neuroprotective effects of a brain permeant 6-aminoquinoxaline derivative in cell culture conditions that model the loss of dopaminergic neurons in Parkinson disease.
AID513640Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 500 uM after 24 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID513641Induction of autophagy in human SK-N-SH cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 500 uM after 48 hrs by densitometric analysis2008Nature chemical biology, May, Volume: 4, Issue:5
Novel targets for Huntington's disease in an mTOR-independent autophagy pathway.
AID1631752Neuroprotective activity in Sprague-Dawley rat astrocytes assessed as effect on vimentin positive cell density and morphology at 1 mM by fluorescence microscopic method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
New 6-Aminoquinoxaline Derivatives with Neuroprotective Effect on Dopaminergic Neurons in Cellular and Animal Parkinson Disease Models.
AID1174520Neuroprotective effect in Sprague-Dawley rat DA neurons at 1 mM after 10 days by immunofluorescence assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Neuroprotective effects of a brain permeant 6-aminoquinoxaline derivative in cell culture conditions that model the loss of dopaminergic neurons in Parkinson disease.
AID492252Neuritogenic effect in rat DA neurons assessed as total neurite length per tyrosine hydrolase immunopositive neurons at 200 nM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Tryptamine-derived alkaloids from Annonaceae exerting neurotrophin-like properties on primary dopaminergic neurons.
AID1123314Cytotoxicity against HGPRTase-deficient mouse S49 cells assessed as growth inhibition at 500 uM after 20 to 49 hrs by time-course study1979Journal of medicinal chemistry, Jul, Volume: 22, Issue:7
2'-O-Acyl-6-thioinosine cyclic 3',5'-phosphates as prodrugs of thioinosinic acid.
AID492250Neuroprotective activity against degeneration of rat DA neurons assessed as tyrosine hydrolase immunopositive neurons immunofluorescence staining at 200 nM relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Tryptamine-derived alkaloids from Annonaceae exerting neurotrophin-like properties on primary dopaminergic neurons.
AID1123313Cytotoxicity against HGPRTase-deficient mouse S49 cells assessed as growth inhibition at 500 uM after 20 to 49 hrs by time-course study in presence of theophylline1979Journal of medicinal chemistry, Jul, Volume: 22, Issue:7
2'-O-Acyl-6-thioinosine cyclic 3',5'-phosphates as prodrugs of thioinosinic acid.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1631771Neuroprotective activity in Sprague-Dawley rat DA neuron death PD model assessed as increase in [2,5,6-3H]DA uptake at 1 mM after 10 days by liquid scintillation counting spectrometric analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
New 6-Aminoquinoxaline Derivatives with Neuroprotective Effect on Dopaminergic Neurons in Cellular and Animal Parkinson Disease Models.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID504883Counterscreen for activators of the Protein Kinase A-R1A (PKA-R1A) complex: fluorescence polarization-based biochemical high throughput dose response assay to identify fluorescence polarization assay artifacts2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504893Counterscreen for activators of the Protein Kinase A-R1A (PKA-R1A) complex: fluorescence polarization-based biochemical high throughput dose response assay to identify activators of the Protein Kinase A-R2B (PKA-R2B) complex2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504890Counterscreen for activators of the Protein Kinase A-R2B (PKA-R2B) complex: fluorescence polarization-based biochemical high throughput dose response assay to identify fluorescence polarization assay artifacts2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID504896Counterscreen for activators of the Protein Kinase A-R2B (PKA-R2B) complex: fluorescence polarization-based biochemical high throughput dose response assay to identify activators of the Protein Kinase A-R1A (PKA-R1A) complex2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID504800Fluorescence polarization-based biochemical high throughput confirmation assay for activators of the Protein Kinase A-R1A (PKA-R1A) complex2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID504797Fluorescence polarization-based biochemical high throughput confirmation assay for activators of the Protein Kinase A-R2B (PKA-R2B) complex2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID504887Fluorescence polarization-based biochemical high throughput dose response assay for activators of the Protein Kinase A-R1A (PKA-R1A) complex2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID504796Counterscreen for activators of the Protein Kinase A-R2B (PKA-R2B) complex: fluorescence polarization-based biochemical high throughput screening assay to identify fluorescence polarization assay artifacts2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504799Counterscreen for activators of the Protein Kinase A-R1A (PKA-R1A) complex: fluorescence polarization-based biochemical high throughput screening assay to identify fluorescence polarization assay artifacts2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504888Fluorescence polarization-based biochemical high throughput dose response assay for activators of the Protein Kinase A-R2B (PKA-R2B) complex2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1145903Induction of serum thyroxine level in Swiss mouse measured per 100 ml at 1 mg, iv after 1 hr by radioimmunoassay (Rvb = 4.20 +/- 0.25 to 6.06 +/- 0.36 ug)1976Journal of medicinal chemistry, Jul, Volume: 19, Issue:7
Synthesis of new cyclic nucleotides and their differential stimulatory effects on thyroid function in mice.
AID1145902Toxicity in iv dosed mouse1976Journal of medicinal chemistry, Jul, Volume: 19, Issue:7
Synthesis of new cyclic nucleotides and their differential stimulatory effects on thyroid function in mice.
AID1145897Induction of radioiodine secretion from 14 days iodine-poor diet fed mouse thyroid assessed as blood [125I] level at 60 mg/kg, iv after 2 hrs pretreated with 10 ug L-thyroxine and [125-I] relative to control by McKenzie Bioassay1976Journal of medicinal chemistry, Jul, Volume: 19, Issue:7
Synthesis of new cyclic nucleotides and their differential stimulatory effects on thyroid function in mice.
AID1145898Induction of radioiodine secretion from 14 days iodine-poor diet fed mouse thyroid assessed as blood [125I] level at 30 mg/kg, iv after 2 hrs pretreated with 10 ug L-thyroxine and [125-I] relative to control by McKenzie Bioassay1976Journal of medicinal chemistry, Jul, Volume: 19, Issue:7
Synthesis of new cyclic nucleotides and their differential stimulatory effects on thyroid function in mice.
AID1145905Stability of the compound assessed as hydrolysis in presence of phosphodiesterase1976Journal of medicinal chemistry, Jul, Volume: 19, Issue:7
Synthesis of new cyclic nucleotides and their differential stimulatory effects on thyroid function in mice.
AID355152Antibacterial activity against Streptococcus mutans LA7 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355156Antibacterial activity against Porphyromonas gingivalis 33277 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355159Antibacterial activity against Capnocytophaga ochracea 33596 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID1315358Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Eucarobustols A-I, Conjugates of Sesquiterpenoids and Acylphloroglucinols from Eucalyptus robusta.
AID355163Inhibition of Streptococcus sobrinus glucosyltransferase assessed as blockade of adherent water insoluble glucan synthesis at 1 ug/mL1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355153Antibacterial activity against Streptococcus sobrinus 6715 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355155Antibacterial activity against Actinomyces viscosus 15987 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355161Inhibition of Streptococcus sobrinus glucosyltransferase assessed as blockade of adherent water insoluble glucan synthesis at 100 ug/mL1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355162Inhibition of Streptococcus sobrinus glucosyltransferase assessed as blockade of adherent water insoluble glucan synthesis at 10 ug/mL1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355157Antibacterial activity against Prevotella melaninogenica 25845 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355160Antibacterial activity against Fusobacterium nucleatum 25586 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355151Antibacterial activity against Streptococcus mutans Ingbritt by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID355154Antibacterial activity against Streptococcus sobrinus B13 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
AID1315357Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Eucarobustols A-I, Conjugates of Sesquiterpenoids and Acylphloroglucinols from Eucalyptus robusta.
AID355158Antibacterial activity against Prevotella intermedia 25611 by broth dilution method1996Journal of natural products, Sep, Volume: 59, Issue:9
Macrocarpals H, I, and J from the Leaves of Eucalyptus globulus.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9,539)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905203 (54.54)18.7374
1990's3062 (32.10)18.2507
2000's1012 (10.61)29.6817
2010's242 (2.54)24.3611
2020's20 (0.21)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials13 (0.13%)5.53%
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Reviews126 (1.29%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies31 (0.32%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
Other9,605 (98.26%)84.16%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]