Page last updated: 2024-12-05

mestranol

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Cross-References

ID SourceID
PubMed CID6291
CHEMBL ID1201151
CHEBI ID6784
SCHEMBL ID41391
MeSH IDM0013488

Synonyms (178)

Synonym
AC-13293
BIDD:ER0199
MLS001077321
BRD-K31920458-001-03-8
smr000059128
MLS000028595 ,
(17beta)-17-ethynyl-3-(methyloxy)estra-1,3,5(10)-trien-17-ol
3-methoxy-17-alpha-ethynyloestradiol
3,17-beta-dihydroxy-17-alpha-ethynyl-1,3,5(10)-estratriene-3-methyl ether
3-methoxy-17-alpha-19-norpregna-1,3,5(10)-trien-20-yn-17-ol
(+)-17-alpha-ethynyl-17-beta-hydroxy-3-methoxy-1,3,5(10)-oestratriene
3-methoxy-17-alpha-ethynyl-1,3,5(10)-estratrien-17-beta-ol
17alpha-ethinyl oestradiol 3-methyl ether
19-norpregna-1,3,5(10)-trien-20-yn-17-ol, 3-methoxy-, (17alpha)-
17beta-estradiol, 17-ethynyl-, 3-(methyl ether)
nsc 84032
3-methoxy-17alpha-ethinyloestradiol
17-alpha-ethynyl-3-methoxy-1,3,5(10)-estratrien-17-beta-ol
brn 2625905
inostral (steroid)
17alpha-ethynyloestradiol 3-methyl ether
3-methoxyethynyloestradiol
17-alpha-ethinyl estradiol 3-methyl ether
mestranolo [dcit]
delta-mve
epa pesticide chemical code 115401
ccris 377
17alpha-ethynylestradiol methyl ether
3-methoxy-17alpha-ethinylestradiol
caswell no. 547a
3-methylethynyloestradiol
17-alpha-ethynyloestradiol methyl ether
3-methoxy-19-nor-17-alpha-pregna-1,3,5(10)-trien-20-yn-17-ol
mestranolum [inn-latin]
3-methoxy-17alpha-ethynyl-1,3,5(10)-estratrien-17beta-ol
17-alpha-19-norpregna-1,3,5(10)-trien-20-yn-17-ol, 3-methoxy-
19-nor-17alpha-pregna-1,3,5(10)-trien-20-yn-17-ol, 3-methoxy-
3-methoxy-17alpha-ethynyloestradiol
17-ethynyloestradiol 3-methyl ether
3-methoxy-17alpha-ethynyl-1,3,5(10)-oestratrien-17beta-ol
(+)-17-alpha-ethynyl-17-beta-hydroxy-3-methoxy-1,3,5(10)-estratriene
3-methoxy-17-alpha-ethynyl-1,3,5(10)-oestratrien-17-beta-ol
17-alpha-ethinyl oestradiol 3-methyl ether
hsdb 3588
3-methoxy-17-alpha-ethinylestradiol
17-ethynyl-3-methoxy-1,3,5(10)-oestratien-17-beta-ol
17alpha-ethinyl estradiol 3-methyl ether
(17-alpha)-3-methoxy-19-norpregna-1,3,5(10)-trien-20-yn-17-ol
17alpha-19-norpregna-1,3,5(10)-trien-20-yn-17-ol, 3-methoxy-
17-alpha-ethynyl-3-methoxy-17-beta-hydroxy-delta-1,3,5(10)-oestratriene
einecs 200-777-8
menophase
estra-1,3,5(10)-trien-17beta-ol, 17-ethynyl-3-methoxy-
17-alpha-ethynyl-3-methoxy-17-beta-hydroxy-delta-1,3,5(10)-estratriene
17alpha-ethinylestradiol 3-methyl ether
3-methoxy-17-ethynyloestradiol-17-beta
estra-1,3,5(10)-trien-17-beta-ol, 17-alpha-ethynyl-3-methoxy-
3-methoxy-17-alpha-ethynylestradiol
3-methoxy-19-nor-17alpha-pregna-1,3,5(10)-trien-20-yn-17-ol
3-methoxy-17alpha-ethynylestradiol
mestranol [steroidal oestrogens]
3-methoxy-17-alpha-ethinyloestradiol
ai3-51798
component of ortho-novum
component of norinyl
PRESTWICK_966
cas-72-33-3
BPBIO1_000915
NCGC00179410-01
8027 c. b.
component of norquen
component of ovulen
ee(sub3)me
compound 33355
nsc84032
3-methylethynylestradiol
devocin
norquen
ethynylestradiol 3-methyl ether
3-o-methylethynylestradiol
ee3me
3-methoxyethynylestradiol
ovastol
ethinylestradiol 3-methyl ether
sc 4725
ethynylestradiol methyl ether
nsc-84032
(8r,9s,13s,14s,17r)-17-ethynyl-3-methoxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-17-ol
(+ )-17.alpha.-ethynyl-17.beta.-hydroxy-3-methoxy-1,3, 5(10)-oestratriene
17.alpha.-19-norpregna-1,3,5(10)-trien-20-yn-17-ol, 3-meth
(+)-17.alpha.-ethynyl-17.beta.-hydroxy-3-methoxy-1,3, 5(10)-estratriene
BSPBIO_000831
CHEBI:6784 ,
3-methoxy-19-norpregna-1,3,5(10)-trien-20-yn-17beta-ol
17-ethynyl-3-methoxyestra-1(10),2,4-trien-17beta-ol
(+)-17alpha-ethynyl-17beta-hydroxy-3-methoxy-1,3,5(10)-estratriene
mestranolum
17-ethynyl-3-methoxyoestra-1(10),2,4-trien-17beta-ol
(+)-17alpha-ethynyl-17beta-hydroxy-3-methoxy-1,3,5(10)-oestratriene
72-33-3
mestranol ,
C07618
mestranol, 99%
NCGC00093347-02
DB01357
D00575
mestranol (jp17/usp/inn)
PRESTWICK2_000846
PRESTWICK0_000846
PRESTWICK1_000846
SPBIO_002752
PRESTWICK3_000846
HMS2051J22
ee-3me
ee3 me
CHEMBL1201151
ee3-me
eei3me
(8r,9s,13s,14s,17r)-17-ethynyl-3-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6h-cyclopenta[a]phenanthren-17-ol
HMS1570J13
AKOS005267152
NCGC00093347-03
HMS2097J13
mestranolo
unii-b2v233xge7
b2v233xge7 ,
mestranol [usan:usp:inn:ban:jan]
dtxsid0020814 ,
NCGC00255342-01
dtxcid20814
tox21_301837
MLS001424224
tox21_111200
HMS2230L20
CCG-101067
mestranol [who-dd]
3-methoxy-19-nor-17.alpha.-pregna-1,3,5(10)-trien-20-yn-17-ol.
mestranol [usp-rs]
enovid component mestranol
mestranol [inn]
mestranol [usp monograph]
mestranol component of ovulen
mestranol [usan]
mestranol [vandf]
ovulen component mestranol
mestranol [jan]
mestranol [mi]
mestranol [ep monograph]
mestranol [hsdb]
mestranol [orange book]
mestranol [mart.]
mestranol component of enovid
S2125 ,
gtpl7087
HY-B0390
17-ethynyl-3-methoxyestra-1(10),2,4-trien-17-ol
NC00317
SCHEMBL41391
tox21_111200_1
NCGC00093347-05
OPERA_ID_872
(1s,10r,11s,14r,15s)-14-ethynyl-5-methoxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-trien-14-ol
SR-01000695429-4
sr-01000695429
mestranol, vetranal(tm), analytical standard
mestranol, united states pharmacopeia (usp) reference standard
mestranol, european pharmacopoeia (ep) reference standard
(17beta)-17-ethynyl-3-methoxyestra-1(10),2,4-trien-17-ol
ethynylestradiol-3-methyl ether
HMS3714J13
(17alpha)-3-methoxy-19-norpregna-1,3,5(10)-trien-20-yn-17-ol
Q904308
BRD-K31920458-001-23-6
C76306
(8r,13s,17r)-17-ethynyl-3-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6h-cyclopenta[a]phenanthren-17-ol
AS-56063
NCGC00093347-07
Z1557501642

Research Excerpts

Overview

Mestranol is a widely used estrogen. It is converted into its active metabolite ethinyl estradiol by cytochrome P450 (CYP) 2C9.

ExcerptReferenceRelevance
"Mestranol is a widely used estrogen, which is converted into its active metabolite ethinyl estradiol by cytochrome P450 (CYP) 2C9. "( Effect of CYP2C9 Genetic Polymorphism in a Chinese Population on the Metabolism of Mestranol in vitro.
Cai, JP; Dai, DP; Hu, GX; Hu, JH; Li, WS; Wang, L, 2015
)
2.08

Effects

ExcerptReferenceRelevance
"Mestranol has been said to have no diabetogenic effects when given as a combined pill, and to ameliorate maturity-onset diabetes."( [Diabetogenic effect of contraceptives].
Lederer, J, 1973
)
0.87

Treatment

The mestranol-treated rats had higher arterial pressures than the controls only after 6 mo of treatment. Rats treated with mestanol and/or norethynodrel had PRA and PRC values that were not different from the control rats.

ExcerptReferenceRelevance
"The mestranol-treated rats had higher arterial pressures than the controls only after 6 mo of treatment."( Body fluid volumes in rats with mestranol-induced hypertension.
Dostal, DE; Fowler, WL; Johnson, JA; Kurz, KD; Payne, CG; Zeigler, DW, 1986
)
1.04
"Rats treated with mestranol and/or norethynodrel had PRA and PRC values that were not different from the control rats; however, mestranol-treated rats and rats treated with mestranol plus norethynodrel had PRS values that were substantially (P less than 0.01) higher than the controls."( Renin-angiotensin mechanisms in oral contraceptive hypertension in conscious rats.
Fowler, WL; Johnson, JA; Kurz, KD; Payne, CG, 1985
)
0.59

Toxicity

ExcerptReferenceRelevance
" Also examined was the probability that a side effect would occur in the 2nd or 3rd cycle if the user had not experienced such an effect in the 1st cycle."( The probability of side effects with ovral, norinyl 1/50 and norlestrin.
Berger, GS; Edelman, DA; Talwar, PP, 1979
)
0.26
" The most common side effect was inter-menstrual bleeding with the 35-microgram pill."( Side effects and compliance with low- and conventional-dose oral contraceptives among adolescents.
Jay, MS; Litt, IF; Neel, EU, 1987
)
0.27
" The incidence of other adverse events was similar among treatment groups, an observation that supports the safety of both formulations."( Efficacy, cycle control, and safety of two triphasic oral contraceptives: Cyclessa (desogestrel/ethinyl estradiol) and ortho-Novum 7/7/7 (norethindrone/ethinyl estradiol): a randomized clinical trial.
Kaunitz, AM, 2000
)
0.31
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Pharmacokinetics

ExcerptReferenceRelevance
" The surface area under the curve of paracetamol concentration changes was found to diminish after the bilateral removal of ovaries; there was a shortening of the half-life period for the elimination phase, and also an increase of the total clearance."( [Effect of estrogens on pharmacokinetics of phenazone and N-acetyl-p-aminophenol].
Kwiatkowski, A, 1991
)
0.28
" The pharmacokinetic differences of EE whether caused by dietary, ethnic, or other factors are not merely differences in gastric absorption or renal excretion."( Selected aspects of the pharmacokinetics and metabolism of ethinyl estrogens and their clinical implications.
Goldzieher, JW, 1990
)
0.28
" Our studies show that this idea is untenable because the half-life of the sulfates is not long enough for such an effect."( Pharmacokinetics of ethinyl estradiol and mestranol.
Brody, SA; Goldzieher, JW, 1990
)
0.54
"We have examined the pharmacokinetic parameters derived from the analysis of plasma ethinyl estradiol (EE) and norethindrone levels after administration of a single dose of three bioequivalent norethindrone-1mg/mestranol (ME)-50 micrograms formulations (Ortho-NovumR 1/50, NorinylR 1/50 and Norcept-MR 1/50) and three norethindrone-1mg/ethinyl estradiol-35 micrograms formulations (Ortho-Novum 1/35R, NorinylR 1/35, Norcept-ER 1/35) in a randomized crossover design involving 24 women for the 35 micrograms and 27 women for the 50 micrograms agents."( Pharmacokinetics of three bioequivalent norethindrone/mestranol-50 micrograms and three norethindrone/ethinyl estradiol-35 micrograms OC formulations: are "low-dose" pills really lower?
Brody, SA; Goldzieher, JW; Turkes, A, 1989
)
0.71
" The pathophysiology of this almost fatal drug reaction is described as a pharmacokinetic interaction: the inherent hepatotoxicity of prothionamide-the drug finally prescribed during convalescence-was significantly potentiated by the Cyt-P-450-inducing effect of the progestagen component of the hormonal contraceptive."( [Fulminant liver failure in tuberculostatic therapy. A contribution to clinical aspects and pharmacokinetics].
Bülau, P; Köster, O; Lelbach, WK; Musch, E; Stiens, R, 1987
)
0.27
" The study revealed an increase in AUC and paracetamol half-life as well as decrease in the total body clearance."( Effect of mestranol on pharmacokinetics of paracetamol.
Droździk, M; Gawrońska-Szklarz, B; Kwiatkowski, A; Wójcicki, J, 1994
)
0.69
" On the base of these experiments there was able to make a conclusion that estrogens influence on the phenazone's pharmacokinetic probably by induction of microsomal enzymes of liver."( [Effect of mestranol on pharmacokinetics of phenazone in the rabbit].
Droździk, M; Gawrońska-Szklarz, B; Kwiatkowski, A; Wójcicki, J, 1996
)
0.68
"To study the pharmacokinetics of a combination oral contraceptive (OC) containing norethindrone and ethinyl estradiol during OC monotherapy, concomitant OC and topiramate (TPM) therapy, and concomitant OC and carbamazepine (CBZ) therapy in order to comparatively evaluate the pharmacokinetic interaction, which may cause contraceptive failure."( Effect of topiramate or carbamazepine on the pharmacokinetics of an oral contraceptive containing norethindrone and ethinyl estradiol in healthy obese and nonobese female subjects.
Bialer, M; Doose, DR; Jacobs, D; Padmanabhan, M; Schwabe, S; Wang, SS, 2003
)
0.32
"Using an optimized pharmacokinetic design, this study indicated men exhibit significantly higher zidovudine-monophosphate and zidovudine-triphosphate exposure following zidovudine oral administration, having implications for drug toxicity and overall tolerance of zidovudine therapy."( The impact of sex and contraceptive therapy on the plasma and intracellular pharmacokinetics of zidovudine.
Aberg, J; Aweeka, FT; Bardeguez, A; Coombs, RW; Lizak, P; Rosenkranz, SL; Segal, Y; Thevanayagam, L; Watts, DH, 2006
)
0.33

Compound-Compound Interactions

Mestranol in combination with ethynodiol diacetate, an oral contraceptive formulation, is isolated from the sample on a partition chromatographic column prior to colorimetric determination.

ExcerptReferenceRelevance
"Mestranol in combination with ethynodiol diacetate, an oral contraceptive formulation, is isolated from the sample on a partition chromatographic column prior to colorimetric determination."( Colorimetric determination of mestranol in combination with ethynodiol diacetate.
Wu, JY, 1975
)
1.99
"A collaborative study of the analysis of mestranol in combination with norethindrone or norethynodrel by column chromatography and ultraviolet determination is presented."( Collaborative study of the analysis of mestranol in combination with norethindrone or norethynodrel.
Brunner, CA, 1971
)
0.78

Bioavailability

ExcerptReferenceRelevance
" Studies on kinetics and bioavailability showed that after oral administration of EE 3-sulfate only about 20% appeared as free EE in the blood, while EE 17-sulfate produced about half this amount."( Selected aspects of the pharmacokinetics and metabolism of ethinyl estrogens and their clinical implications.
Goldzieher, JW, 1990
)
0.28
"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

Dosage Studied

Mestranol dosage above the ED50 reduced the tubal stay towards two days in comparison to five days in control animals. A marked decrease in serum and plasma AT3 activity was also observed for women taking low dosage combined OCs. Malignant neoplasms were seen in dogs given 10 and 25 times the proposed human dosage of anagestone acetate and ethynerone.

ExcerptRelevanceReference
" Knowledge of the relative amounts of estrogen and progestin in the available preparations permits a rational adjustment of dosage if side effects occur."( When patients 'can't' take the pill.
Freeman, WS, 1978
)
0.26
" The decreased glucose tolerance may be due as much to dosage levels as to any metabolic characteristics of the various oestrogens prescribed."( Effect of hormone replacement therapy on glucose tolerance in postmenopausal women.
Chakravarti, S; Oram, DH; Studd, JW; Thom, M, 1977
)
0.26
" Over the dosage range studied, the effects of the two kinds of estrogen were indistinguishable."( Comparative studies of the ethynyl estrogens used in oral contraceptives. VII. Effects with and without progestational agents on ultracentrifugally fractionated plasma lipoproteins in humans, baboons, and beagles.
Chenault, CB; de la Peña, A; Dozier, TS; Goldzieher, JW; Kraemer, DC, 1978
)
0.26
" Effects of the 2 kinds of estrogens were indistinguishable over the dosage range studied."( Comparative studies of the ethynyl estrogens used in oral contraceptives. VII. Effects with and without progestational agents on ultracentrifugally fractionated plasma lipoproteins in humans, baboons, and beagles.
Chenault, CB; de la Peña, A; Dozier, TS; Goldzieher, JW; Kraemer, DC, 1978
)
0.26
" Inhibition of the estrous cycle and vulvar enlargement were seen in all dosed dogs."( FDA studies of estrogen, progestogens, and estrogen/progestogen combinations in the dog and monkey.
Geil, RG; Lamar, JK, 1977
)
0.26
" Malignant neoplasms were seen in dogs given 10 and 25 times the proposed human dosage of anagestone acetate plus mestranol and 25 times the proposed human dosage of WY-4355 plus mestranol and ethynerone plus mestranol."( Mammary nodules in beagle dogs administered investigational oral contraceptive steroids.
Casey, HW; Geil, RG; Giles, RC; Kwapien, RP, 1978
)
0.47
" Mestranol dosage above the ED50 reduced the tubal stay towards two days in comparison to five days in control animals."( Influence of 3-methylether of ethinylestradiol (Mestranol) on oviductal egg transport in rats.
Oettel, M; Ohme, E; Strecke, J; Tiroke, I, 1978
)
1.42
" The potency and dosage is correlated with the pathogenic effects observed."( Effects of contraceptive pills and intrauterine devices on urinary bladder.
Fayad, M; Kamel, M; Mooro, H; Osman, MI; Youssef, AF; Zahran, MM, 1976
)
0.26
" All the dose-response curves were drawn using logit-log transformation."( [Effect of oral contraceptive on the pituitary and plasma L.H. levels and on the hypothalamic LH-RH level (author's transl)].
Arai, K; Kanazawa, M; Okinaga, S; Sato, N; Yanaihara, T, 1976
)
0.26
" Animals receiving labeled steroids or labeled bile intraductally also had the duodenum fitted with a cannula connected with a dosing syringe."( Effects of neomycin on the biliary excretion and enterohepatic circulation of mestranol and 17beta-oestradiol.
Brewster, D; Jones, RS; Symons, AM, 1977
)
0.49
" The dosage most often used was a 5: to ."( Biochemical effects of treatment with oral contraceptive steroids on the dopaminergic system of the rat.
Algeri, S; Dolfini, E; Jori, A; Ponzio, F, 1976
)
0.26
" In the intermediate dosage range, both factors contributed to the decreased ratio."( Effect of 17alpha-ethinylestradiol on biliary excretion of bile acids.
Watanabe, H, 1975
)
0.25
"A comparative clinical trial of two combined oral contraceptives differing only in estrogen type and dosage was conducted at the Centro de Investigaciones Hideyo Noguchi in Merida, Yucatan, Mexico."( A comparative clinical trial of Norinyl 1 + 35 versus Norinyl 1 + 50 in Merida, Yucatan, Mexico.
de Cetina, TC; Dunson, TR; Gamboa, LV; Reyes, LP; Rowan, AJ; Waszak, CS; Weaver, MB, 1990
)
0.28
" This wide variability confounds efforts to establish tight dose-response relationships, a point rarely considered in clinical or epidemiologic studies of these compounds."( Pharmacokinetics of ethinyl estradiol and mestranol.
Brody, SA; Goldzieher, JW, 1990
)
0.54
" Since the amount of norethindrone in the two dosage groups was the same, this difference in the pharmacokinetics between the 35 micrograms EE and the 50 micrograms ME formulations remains unexplained."( Pharmacokinetics of three bioequivalent norethindrone/mestranol-50 micrograms and three norethindrone/ethinyl estradiol-35 micrograms OC formulations: are "low-dose" pills really lower?
Brody, SA; Goldzieher, JW; Turkes, A, 1989
)
0.53
" Studies of the oral contraceptives in current use show that the coagulation effects depend on the dosage of estrogen and the type of progestogen used in combination."( Coagulation effects of oral contraception.
Bonnar, J, 1987
)
0.27
" Six women with luteal insufficiency received 300 mg/d after control studies, and this dosage was effective in supplementing the circulating natural hormone so that it reached the level of that of fertile women."( The biological expression of natural progesterone.
Alonso-Uriarte, R; Cortés-Gallegos, V; González-Diddi, M; Sojo-Aranda, I, 1988
)
0.27
" There was no relationship between the dosage of estrogen and the onset of cerebrovascular disease."( [Cerebral venous thrombosis associated with the use of oral contraceptives].
Kamezaki, T; Kobayashi, E; Maki, Y; Meguro, K; Tsuboi, K, 1986
)
0.27
" Because of endogenous estrogen accumulation, such dosage levels make the total of endogenous and exogenous estrogen dangerously high."( Liver hamartomas in patients on oral contraceptives.
Elstein, M, 1974
)
0.25
" Mestranol in this dosage appeared to be relatively safe, but it is too early to evaluate the long-term hazards of such therapy."( Oestrogen replacement therapy for prevention of osteoporosis after oophorectomy.
Aitken, JM; Hart, DM; Lindsay, R, 1973
)
1.16
" Patients had been treated with 4 different dosage combinations of estrogen and progestins over periods varying from 3 months to 24 months."( Progestational agents and blood coagulation. VI. Relationship of ABO blood types to changes induced by oral contraceptives.
Lillie, MA; Mink, IB, 1974
)
0.25
" It has a distinct antifertility effect in rats but without a clearcut dose-response relationship."( Antifertility effect and some pharmacological actions of Butea frondosa seed extracts.
Bhide, NK; Kapila, K; Razdan, MK, 1969
)
0.25
" The dosage of Enovid was selected on the basis of preliminary experiments."( Reduction of carcinogen-induced breast cancer in rats by an anti-fertility drug.
Casey, AE; Griswold, DP; Weisburger, EK; Weisburger, JH, 1968
)
0.25
"19-nor steroids in high and medium dosage in continuous or cyclic combined regimens with oestrogen produce an endometrium characterized by hyperinvoluted glands, a prominent predecidual reaction, suppressed arterioles, and dilated venules."( Synthetic progestagen-oestrogen preparations and endometrial morphology.
Ober, WB, 1966
)
0.24
" In some, continuous therapy was given at the same dosage for 60-240 days."( Influence of norethynodrel and mestranol upon cervical dysplasia and carcinoma in situ.
Arsenault, J; Ayre, JE; Hillemanns, HG; Le GUERRIER, J; Leguerrier, J, 1966
)
0.53
" But again, both these extracts were capable of enhancing the mutation yield induced with an ineffective dosage of 2-acetylaminofluorene and N-nitrosopiperidine."( Enhancement of mutagenic activity in Salmonella by contraceptive steroids.
Allen, BE; Cox, JT; Epler, JL; Rao, TK, 1983
)
0.27
" The ergotropic effect of Mestranol depends on its dosage and possibly the nutrients in the ration."( [Use of mestranol as an anabolic substance in fattening bulls].
Chemnitius, KH; Freytag, HH; Hennig, A,
)
0.87
"We describe the plasma levels of FSH and LH in ten patients with gonadal dysgenesis during treatment with a low dosage sequential estrogen-progestogen preparation."( Plasma levels of FSH and LH in patients with gonadal dysgenesis during sequential estrogen and progestogen therapy.
Amann, K; Breckwoldt, M; Peters, F; Reck, G; Roll, H; Zahradnik, HP, 1980
)
0.26
" During a four year period, 14 patients were treated with an oral contraceptive preparation which combined a reduced dosage of estrogen and progesterone."( [A new method for managing epistaxis in Osler's disease (author's transl)].
Budde, R, 1981
)
0.26
" In women pituitary suppressed by a high-dose oral contraceptive, the daily administration of 150 IU rFSH for 1 week induced more and larger antral follicles than the same regimen with urinary FSH, whereas the serum immunoactive FSH concentrations measured 24 h after each dosing were similar."( Clinical profiling of recombinant follicle stimulating hormone (rFSH; Puregon): relationship between serum FSH and efficacy.
Coelingh Bennink, H; Mannaerts, BM; Out, HJ; Rombout, F,
)
0.13
" The findings of this study indicate that there is little potential for dosages as high as 30 mg/day, the maximum recommended dosing schedule, of rizatriptan to alter the plasma concentrations of oral contraceptives."( A double-blind, placebo-controlled evaluation of the effect of oral doses of rizatriptan 10 mg on oral contraceptive pharmacokinetics in healthy female volunteers.
Goldberg, MR; Liu, G; Shadle, CR, 2000
)
0.31
" An antithromboembolic effects was suggested with an increasing combined dosage of norethisterone acetate."( Thromboembolic disease and the steroidal content of oral contraceptives.
Swyer, GI, 1970
)
0.25
"The observation that estrogens in sufficient dosage given postcoitally may prevent implantation of the ovum have led to studies regarding practical clinical application."( Post-coital oral contraception.
Morris, JM; Van Wagenen, G, 1966
)
0.24
" The pill blocks the normal hypothalamo-hypophyseal secretions and prevents ovulation; high dosage pills are completely effective in doing this; minipills less effective."( [The pill].
Dellenbach, P; Schick, R,
)
0.13
"The effect on liver functions of oral contraceptives (OCs) was studied by measuring the effect low dosage (Primovlar and Ovulen) OCs on serum pseudocholine esterase, a hepatic enzyme."( Effect of low dosage contraceptive pills on serum pseudocholine esterase level.
El Khodary, M; Mikaty, N; Nagui, AR; Shaarawy, M; Shalaby, M, 1976
)
0.26
" Dosage used should be minimum, compatible with efficacy for both the estrogens and the progestogens."( Metabolic effects of contraceptive steroids IV. Liver function tests--short term observations.
Chaudhury, RR; Devi, PK; Gupta, I; Nath, R, 1972
)
0.25
" Dosage is increased only when break through bleeding occurs."( Newer synthetic progestins for the treatment of endometriosis.
Kistner, RW, 1970
)
0.25
" In general, the lowest effective dose of any drug, including contraceptives, is the best practice, but as the dosage is decreased from 50 mcg, cycle control is less effective though side effects are minimized; therefore, reliance on bleeding patterns is necessary for deciding an individual's dosage schedule."( The choice of the dose of oestrogen in a combined oral contraceptive.
Smith, M, 1978
)
0.26
" Administration and dosage of the various agents is to be specified by a doctor according to the particular method, and to the state of health of the patient."( [Pharmacological aspects of oral contraceptives (author's transl)].
Simon, P; Soubrie, C; Weil-levy, C, 1980
)
0.26
" This low dosage was also useful in the management of dysmenorrhea, menorrhagia and irregular menses."( OVULATION INHIBITORS.
CROCKER, KM; STITT, WD, 1964
)
0.24
"Serial plasma and intracellular zidovudine pharmacokinetics following oral and intravenous dosing were determined in 18 men and 20 women treated with zidovudine."( The impact of sex and contraceptive therapy on the plasma and intracellular pharmacokinetics of zidovudine.
Aberg, J; Aweeka, FT; Bardeguez, A; Coombs, RW; Lizak, P; Rosenkranz, SL; Segal, Y; Thevanayagam, L; Watts, DH, 2006
)
0.33
"Men exhibited higher area under the concentration versus time curve for intracellular zidovudine and zidovudine-monophosphate following oral and intravenous dosing and higher zidovudine triphosphate following oral dosing."( The impact of sex and contraceptive therapy on the plasma and intracellular pharmacokinetics of zidovudine.
Aberg, J; Aweeka, FT; Bardeguez, A; Coombs, RW; Lizak, P; Rosenkranz, SL; Segal, Y; Thevanayagam, L; Watts, DH, 2006
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
xenoestrogenA synthetic or semi-synthetic compound that has oestrogenic activity.
[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 (3)

ClassDescription
17beta-hydroxy steroidA 17-hydroxy steroid in which the hydroxy group at position 17 has a beta-configuration.
terminal acetylenic compoundAn acetylenic compound which a carbon of the C#C moiety is attached to a hydrogen atom.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[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 (36)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency10.59090.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency8.51640.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency2.64050.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency0.74190.000657.913322,387.1992AID1259377; AID1259394
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency19.76230.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency5.50080.000417.946075.1148AID1346784; AID1346795; AID1347036
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.12270.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency5.49410.000214.376460.0339AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency14.82600.003041.611522,387.1992AID1159552; AID1159553; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.03340.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency16.47870.005428.02631,258.9301AID1346982; AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.48910.000229.305416,493.5996AID1259383; AID743069; AID743075; AID743077; AID743078; AID743079
GVesicular stomatitis virusPotency5.58560.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency4.89750.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency0.94380.001024.504861.6448AID743215
thyroid stimulating hormone receptorHomo sapiens (human)Potency15.23990.001628.015177.1139AID1224843; AID1224895
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency24.00600.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency1.10130.039147.5451146.8240AID1224845
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency22.25960.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.02240.000627.21521,122.0200AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency7.07950.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency29.85540.004611.374133.4983AID624296
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency31.62280.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency1.25890.891312.067628.1838AID1487
Interferon betaHomo sapiens (human)Potency5.58560.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency5.58560.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency5.58560.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency5.58560.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)IC50 (µMol)0.01800.00000.723732.7000AID625258
Estrogen receptorHomo sapiens (human)Ki0.00520.00000.42297.9070AID625258
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)1.38200.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.37100.00322.28879.3160AID625207
Androgen receptorRattus norvegicus (Norway rat)IC50 (µMol)10.68200.00101.979414.1600AID625228
Androgen receptorRattus norvegicus (Norway rat)Ki7.12100.00031.21858.9270AID625228
Cannabinoid receptor 1Homo sapiens (human)IC50 (µMol)28.54000.00010.275310.0000AID625235
Cannabinoid receptor 1Homo sapiens (human)Ki22.53200.00010.50779.6000AID625235
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)1.38200.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.37100.00031.465610.0000AID625207
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)0.04100.00010.86458.7096AID625222
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.02200.00000.70488.1930AID625222
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7Homo sapiens (human)AC502.48000.039815.002550.0000AID743267
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (153)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
antral ovarian follicle growthEstrogen receptorHomo sapiens (human)
epithelial cell developmentEstrogen receptorHomo sapiens (human)
chromatin remodelingEstrogen receptorHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
signal transductionEstrogen receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEstrogen receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEstrogen receptorHomo sapiens (human)
androgen metabolic processEstrogen receptorHomo sapiens (human)
male gonad developmentEstrogen receptorHomo sapiens (human)
negative regulation of gene expressionEstrogen receptorHomo sapiens (human)
positive regulation of phospholipase C activityEstrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptorHomo sapiens (human)
response to estradiolEstrogen receptorHomo sapiens (human)
regulation of toll-like receptor signaling pathwayEstrogen receptorHomo sapiens (human)
negative regulation of smooth muscle cell apoptotic processEstrogen receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionEstrogen receptorHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
response to estrogenEstrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
fibroblast proliferationEstrogen receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEstrogen receptorHomo sapiens (human)
stem cell differentiationEstrogen receptorHomo sapiens (human)
regulation of inflammatory responseEstrogen receptorHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
RNA polymerase II preinitiation complex assemblyEstrogen receptorHomo sapiens (human)
uterus developmentEstrogen receptorHomo sapiens (human)
vagina developmentEstrogen receptorHomo sapiens (human)
prostate epithelial cord elongationEstrogen receptorHomo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesisEstrogen receptorHomo sapiens (human)
regulation of branching involved in prostate gland morphogenesisEstrogen receptorHomo sapiens (human)
mammary gland branching involved in pregnancyEstrogen receptorHomo sapiens (human)
mammary gland alveolus developmentEstrogen receptorHomo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongationEstrogen receptorHomo sapiens (human)
protein localization to chromatinEstrogen receptorHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptorHomo sapiens (human)
negative regulation of miRNA transcriptionEstrogen receptorHomo sapiens (human)
regulation of epithelial cell apoptotic processEstrogen receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptorHomo sapiens (human)
positive regulation of acute inflammatory response to antigenic stimulusCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
spermatogenesisCannabinoid receptor 1Homo sapiens (human)
axonal fasciculationCannabinoid receptor 1Homo sapiens (human)
response to nutrientCannabinoid receptor 1Homo sapiens (human)
memoryCannabinoid receptor 1Homo sapiens (human)
positive regulation of neuron projection developmentCannabinoid receptor 1Homo sapiens (human)
negative regulation of serotonin secretionCannabinoid receptor 1Homo sapiens (human)
positive regulation of fever generationCannabinoid receptor 1Homo sapiens (human)
negative regulation of fatty acid beta-oxidationCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, GABAergicCannabinoid receptor 1Homo sapiens (human)
response to lipopolysaccharideCannabinoid receptor 1Homo sapiens (human)
negative regulation of mast cell activationCannabinoid receptor 1Homo sapiens (human)
negative regulation of dopamine secretionCannabinoid receptor 1Homo sapiens (human)
response to nicotineCannabinoid receptor 1Homo sapiens (human)
cannabinoid signaling pathwayCannabinoid receptor 1Homo sapiens (human)
response to cocaineCannabinoid receptor 1Homo sapiens (human)
glucose homeostasisCannabinoid receptor 1Homo sapiens (human)
positive regulation of apoptotic processCannabinoid receptor 1Homo sapiens (human)
response to ethanolCannabinoid receptor 1Homo sapiens (human)
negative regulation of action potentialCannabinoid receptor 1Homo sapiens (human)
negative regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
positive regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
regulation of insulin secretionCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicCannabinoid receptor 1Homo sapiens (human)
maternal process involved in female pregnancyCannabinoid receptor 1Homo sapiens (human)
regulation of feeding behaviorCannabinoid receptor 1Homo sapiens (human)
regulation of penile erectionCannabinoid receptor 1Homo sapiens (human)
retrograde trans-synaptic signaling by endocannabinoidCannabinoid receptor 1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationCannabinoid receptor 1Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
regulation of metabolic processCannabinoid receptor 1Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (64)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
TFIIB-class transcription factor bindingEstrogen receptorHomo sapiens (human)
transcription coregulator bindingEstrogen receptorHomo sapiens (human)
transcription corepressor bindingEstrogen receptorHomo sapiens (human)
transcription coactivator bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
chromatin bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
nuclear receptor activityEstrogen receptorHomo sapiens (human)
steroid bindingEstrogen receptorHomo sapiens (human)
protein bindingEstrogen receptorHomo sapiens (human)
calmodulin bindingEstrogen receptorHomo sapiens (human)
beta-catenin bindingEstrogen receptorHomo sapiens (human)
zinc ion bindingEstrogen receptorHomo sapiens (human)
TBP-class protein bindingEstrogen receptorHomo sapiens (human)
enzyme bindingEstrogen receptorHomo sapiens (human)
protein kinase bindingEstrogen receptorHomo sapiens (human)
nitric-oxide synthase regulator activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor bindingEstrogen receptorHomo sapiens (human)
estrogen response element bindingEstrogen receptorHomo sapiens (human)
identical protein bindingEstrogen receptorHomo sapiens (human)
ATPase bindingEstrogen receptorHomo sapiens (human)
14-3-3 protein bindingEstrogen receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen receptorHomo sapiens (human)
cannabinoid receptor activityCannabinoid receptor 1Homo sapiens (human)
protein bindingCannabinoid receptor 1Homo sapiens (human)
identical protein bindingCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor activityCannabinoid receptor 1Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (42)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
nucleoplasmEstrogen receptorHomo sapiens (human)
transcription regulator complexEstrogen receptorHomo sapiens (human)
cytoplasmEstrogen receptorHomo sapiens (human)
Golgi apparatusEstrogen receptorHomo sapiens (human)
cytosolEstrogen receptorHomo sapiens (human)
plasma membraneEstrogen receptorHomo sapiens (human)
membraneEstrogen receptorHomo sapiens (human)
chromatinEstrogen receptorHomo sapiens (human)
euchromatinEstrogen receptorHomo sapiens (human)
protein-containing complexEstrogen receptorHomo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
mitochondrial outer membraneCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
actin cytoskeletonCannabinoid receptor 1Homo sapiens (human)
growth coneCannabinoid receptor 1Homo sapiens (human)
presynaptic membraneCannabinoid receptor 1Homo sapiens (human)
membrane raftCannabinoid receptor 1Homo sapiens (human)
glutamatergic synapseCannabinoid receptor 1Homo sapiens (human)
GABA-ergic synapseCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
cytoplasmCannabinoid receptor 1Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (86)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
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.
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.
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.
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.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1124644Induction of vaginal cornification in ovariectomized mature rat at 0.025 to 0.1 mg/kg, po administered with sesame oil by Allen-Doisy method relative to control1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis and estrogenic properties of 17-epi-ethynylestradiol and its ether derivatives epimestranol and epiquinestrol.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID188023Oral antifertility potency (A) relative to ethynylestradiol (EE) in rats.1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Analogues of [(triethylsilyl)ethynyl]estradiol as potential antifertility agents.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID678719Metabolic stability in human liver microsomes assessed as medium signal/noise ratio (S/N of 10 to 100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID197229Oral estrogenic activity in uterotropic assay in rats at 100-10000 ng dose1980Journal of medicinal chemistry, Mar, Volume: 23, Issue:3
Synthesis and biological activity of some 15-oxaestranes.
AID625295Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in Pfizer data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID1124652Displacement of 17beta-[3H]estradiol from rabbit uterine estrogen receptor after 16 to 18 hrs by liquid scintillation counting relative to ethynylestradiol1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis and estrogenic properties of 17-epi-ethynylestradiol and its ether derivatives epimestranol and epiquinestrol.
AID1124650Displacement of 17beta-[3H]estradiol from rabbit uterine estrogen receptor after 16 to 18 hrs by liquid scintillation counting1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis and estrogenic properties of 17-epi-ethynylestradiol and its ether derivatives epimestranol and epiquinestrol.
AID188024Oral estrogenic potency (E) relative to ethynylestradiol (EE) in rats1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Analogues of [(triethylsilyl)ethynyl]estradiol as potential antifertility agents.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
AID1124643Estrogenic activity in immature rat administered orally with sesame oil as three doses by uterotropic assay relative to ethynylestradiol1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis and estrogenic properties of 17-epi-ethynylestradiol and its ether derivatives epimestranol and epiquinestrol.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
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.
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.
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.
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.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,304)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902169 (94.14)18.7374
1990's66 (2.86)18.2507
2000's35 (1.52)29.6817
2010's24 (1.04)24.3611
2020's10 (0.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index44.61 (24.57)
Research Supply Index7.89 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index74.96 (26.88)
Search Engine Supply Index2.02 (0.95)

This Compound (44.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials183 (7.33%)5.53%
Reviews56 (2.24%)6.00%
Case Studies172 (6.89%)4.05%
Observational0 (0.00%)0.25%
Other2,084 (83.53%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective Comparison of Hormone Withdrawal Symptoms of a 24/4 Regimen With a 21/7 Regimen of OC [NCT00475189]51 participants (Actual)Interventional2007-06-30Completed
Deciphering the Hormonal and Nociceptive Mechanisms Underlying Bladder Pain [NCT02214550]Phase 4353 participants (Actual)Interventional2014-07-31Completed
Pharmacodynamics of NPC-01( 1mg Norethisterone and 0.02mg Ethinyl Estradiol) and IKH-01( 1mg Norethisterone and 0.035mg Ethinyl Estradiol); Effect of NPC-01 and IKH-01 on Serum Concentrations of Estradiol, Progesterone, FSH and LH. [NCT01253824]Phase 314 participants (Actual)Interventional2011-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01253824 (4) [back to overview]Comparing Estradiol AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))
NCT01253824 (4) [back to overview]Comparing FSH AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))
NCT01253824 (4) [back to overview]Comparing LH AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))
NCT01253824 (4) [back to overview]Comparing Progesterone AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))
NCT02214550 (6) [back to overview]Change in Participant Bladder Pain Sensitivity From Baseline.
NCT02214550 (6) [back to overview]Change in Participant Bladder Pain Sensitivity From Baseline.
NCT02214550 (6) [back to overview]Change in Quantitative Sensory Testing (QST) Parameters Regarding Pelvic Hyperalgesia From Baseline
NCT02214550 (6) [back to overview]Change in Quantitative Sensory Testing (QST) Parameters Regarding Pelvic Hyperalgesia From Baseline
NCT02214550 (6) [back to overview]Differences in EEG Recorded Cortical Activity Among Participants
NCT02214550 (6) [back to overview]Differences in EEG Recorded Cortical Activity Among Participants

Comparing Estradiol AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))

Estradiol was measured on day 3, 6, 9, 12, 15, 18, 21, 24 on 3 consecutive menstrual period (pre administration/Baseline(BL), study drug administration(SDA), post administration/follow up(FU)) and calculated AUC from these data (NCT01253824)
Timeframe: Day 3, 6, 9, 12, 15, 18, 21, 24 of menstrual cycles

,
Interventionpg・day/mL, (Mean)
Difference of estradiol AUC (BL-SDA)Difference of estradiol AUC(FU-SDA)
IKH-012478.02434.9
NPC-011654.71872.6

[back to top]

Comparing FSH AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))

FSH was measured on day 3, 6, 9, 12, 15, 18, 21, 24 on 3 consecutive menstrual period (pre administration/Baseline(BL), study drug administration(SDA), post administration/follow up(FU)) and calculated AUC from these data (NCT01253824)
Timeframe: Day 3, 6, 9, 12, 15, 18, 21, 24 of menstrual cycles

,
InterventionmIU・day/mL (Mean)
Differnce of FSH (BL-SDA)Difference of FSH(FP-SDA)
IKH-01-4.3800.538
NPC-01-9.609-4.404

[back to top]

Comparing LH AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))

LH was measured on day 3, 6, 9, 12, 15, 18, 21, 24 on 3 consecutive menstrual period (pre administration/Baseline(BL), study drug administration(SDA), post administration/follow up(FU)) and calculated AUC from these data (NCT01253824)
Timeframe: Day 3, 6, 9, 12, 15, 18, 21, 24 of menstrual cycles

,
InterventionmIU・day/mL (Mean)
Difference of LH(BL-SDA)Difference of LH(FU-SDA)
IKH-0157.12459.837
NPC-0160.87461.571

[back to top]

Comparing Progesterone AUC of Menstrual Period During Study Drug Administration With Pre and Post Study Drug Administration (Baseline(BL)-Study Drug Administration(SDA), Follow up(FU)-Study Drug Administration(ADA))

Progesterone was measured on day 3, 6, 9, 12, 15, 18, 21, 24 on 3 consecutive menstrual period (pre administration/Baseline(BL), study drug administration(SDA), post administration/follow up(FU)) and calculated AUC from these data (NCT01253824)
Timeframe: Day 3, 6, 9, 12, 15, 18, 21, 24 of menstrual cycles

,
Interventionng・day/mL (Mean)
Difference of progesterone(BL-SDA)Difference of progesterone(FU-SDA)
IKH-0193.14859.344
NPC-0154.17189.711

[back to top]

Change in Participant Bladder Pain Sensitivity From Baseline.

Score on a scale. Specifically, we used a Visual Analog Scale- 0 through 100 scale with 0 being no pain and 100 worst pain imaginable. Results from the visual analog scale (VAS) of the bladder filling test at the initial, 6 month and 12 month visits will be compared to determine if participants in each of the treatment groups had a reduction in pain. Bladder pain ratings at first urge will be used at the outcome measure. (NCT02214550)
Timeframe: 0 (baseline), 6 month, and 12 month visits

,,,,
Interventionscore on a scale (Mean)
Baseline
No Intervention Chronic Pain (Positive Controls)17.3
No Intervention: Dysmenorrhea (D)4.1
No Intervention: Dysmenorrhea With Cross Organ Sensitization (D+COS)33
No Intervention: Healthy Controls2.2
No Intervention: Painful Bladder Syndrome (PBS)/Interstitial Cystitis (IC)49.0

[back to top]

Change in Participant Bladder Pain Sensitivity From Baseline.

Score on a scale. Specifically, we used a Visual Analog Scale- 0 through 100 scale with 0 being no pain and 100 worst pain imaginable. Results from the visual analog scale (VAS) of the bladder filling test at the initial, 6 month and 12 month visits will be compared to determine if participants in each of the treatment groups had a reduction in pain. Bladder pain ratings at first urge will be used at the outcome measure. (NCT02214550)
Timeframe: 0 (baseline), 6 month, and 12 month visits

,,,
Interventionscore on a scale (Mean)
BaselineMonth 6Month 12
D+COS-continuous Microgestin 1/2041.218.68.6
D+COS-cyclic Microgestin 1/2037.032.034.0
D+COS-no OC38.244.547.0
PBS-continuous Microgestin 1/2047.941.438.8

[back to top]

Change in Quantitative Sensory Testing (QST) Parameters Regarding Pelvic Hyperalgesia From Baseline

Results from the QST testing performed at initial, 6 month and 12 month visits will be compared to determine if participants in each of the treatment groups had a reduction in sensitivity from baseline. Specifically, measure reported is the pressure pain threshold in newtons observed at the transition from pressure to pain transvaginally at the 12 o'clock position (anteriorly against the bladder). Lower values (pressure) indicate greater sensitivity. (NCT02214550)
Timeframe: 0 (baseline), 6 months and 12 months

,,,,
InterventionNewtons (Mean)
Baseline
No Intervention Chronic Pain (Positive Controls)6.9
No Intervention: Dysmenorrhea (D)8.9
No Intervention: Dysmenorrhea With Cross Organ Sensitization (D+COS)7.2
No Intervention: Healthy Controls11.6
No Intervention: Painful Bladder Syndrome (PBS)/Interstitial Cystitis (IC)6.9

[back to top]

Change in Quantitative Sensory Testing (QST) Parameters Regarding Pelvic Hyperalgesia From Baseline

Results from the QST testing performed at initial, 6 month and 12 month visits will be compared to determine if participants in each of the treatment groups had a reduction in sensitivity from baseline. Specifically, measure reported is the pressure pain threshold in newtons observed at the transition from pressure to pain transvaginally at the 12 o'clock position (anteriorly against the bladder). Lower values (pressure) indicate greater sensitivity. (NCT02214550)
Timeframe: 0 (baseline), 6 months and 12 months

,,,
InterventionNewtons (Mean)
BaselineMonth 6Month 12
D+COS-no OC5.955.407.36
D+COS-continuous Microgestin 1/2013.812.39.94
D+COS-cyclic Microgestin 1/209.3813.97.74
PBS-continuous Microgestin 1/208.213.395.59

[back to top]

Differences in EEG Recorded Cortical Activity Among Participants

We obtained the peak alpha frequency at the right and left parietal occipital electrodes and averages of the two sides were assessed at Baseline, 6 month, and 12 Month to determine whether differences in resting state brain activity at parieto-occipital electrode sites are affected by oral contraceptives (NCT02214550)
Timeframe: Baseline, 6 months and 12 months

,,,,
InterventionHertz (Mean)
Baseline
No Intervention Chronic Pain (Positive Controls)10.15
No Intervention: Dysmenorrhea (D)10.12
No Intervention: Dysmenorrhea With Cross Organ Sensitization (D+COS)9.96
No Intervention: Healthy Controls10.03
No Intervention: Painful Bladder Syndrome (PBS)/Interstitial Cystitis (IC)10.0

[back to top]

Differences in EEG Recorded Cortical Activity Among Participants

We obtained the peak alpha frequency at the right and left parietal occipital electrodes and averages of the two sides were assessed at Baseline, 6 month, and 12 Month to determine whether differences in resting state brain activity at parieto-occipital electrode sites are affected by oral contraceptives (NCT02214550)
Timeframe: Baseline, 6 months and 12 months

,,,
InterventionHertz (Mean)
BaselineMonth 6Month 12
D+COS-continuous Microgestin 1/2010.0510.199.75
D+COS-cyclic Microgestin 1/2010.010.019.97
D+COS-no OC10.0310.109.88
PBS-continuous Microgestin 1/2010.1310.1610.48

[back to top]