Page last updated: 2024-11-05

methoxamine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Methoxamine: An alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

methoxamine : An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group and the phenyl ring is 2- and 5-substituted with methoxy groups. It is an antihypotensive agent (pressor), an agonist acting directly at alpha-adrenoceptors with selectivity for the alpha-1 adrenoceptor subtype similar to phenylephrine . [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]

Cross-References

ID SourceID
PubMed CID6082
CHEMBL ID524
CHEBI ID6839
SCHEMBL ID34158
MeSH IDM0013598

Synonyms (72)

Synonym
gtpl483
2,5-dimethoxynorephedrine
benzenemethanol, .alpha.-(1-aminoethyl)-2,5-dimethoxy-
benzyl alcohol, .alpha.-(1-aminoethyl)-2,5-dimethoxy-
BSPBIO_000549
2-amino-1-[2,5-bis(methyloxy)phenyl]propan-1-ol
alpha-(1-aminoethyl)-2,5-dimethoxybenzyl alcohol
benzyl alcohol, alpha-(1-aminoethyl)-2,5-dimethoxy-
methoxamedrine
methoxamin
benzenemethanol, alpha-(1-aminoethyl)-2,5-dimethoxy-
SPECTRUM_001021
PRESTWICK2_000535
BSPBIO_001995
BPBIO1_000605
LOPAC0_000769
PRESTWICK3_000535
SPECTRUM5_001821
AB00053731
methoxamine
390-28-3
C07513
DB00723
pseudomethoxamine
metossamina
KBIOGR_000541
KBIO2_001501
KBIO2_004069
KBIOSS_001501
KBIO3_001495
KBIO2_006637
SPBIO_002470
SPBIO_000852
PRESTWICK1_000535
SPECTRUM2_000776
SPECTRUM3_000498
SPECTRUM4_000051
PRESTWICK0_000535
NCGC00089793-02
NCGC00015692-06
L000757
chebi:6839 ,
nrl001
nrl-001
CHEMBL524 ,
methoxamine (ban)
D08201
(1r,2s)-2-amino-1-(2,5-dimethoxyphenyl)propan-1-ol
2-amino-1-(2,5-dimethoxyphenyl)propan-1-ol
2-amino-1-(2,5-dimethoxy-phenyl)-propan-1-ol(methoxamine)
bdbm50026777
2-amino-1-(2,5-dimethoxy-phenyl)-propan-1-ol
2-amino-1-(2,5-dimethoxy-phenyl)-propan-1-ol (methoxamine)
CCG-204854
AKOS009208855
mfcd00242998
NCGC00015692-03
NCGC00015692-04
SCHEMBL34158
NCGC00015692-08
2-amino-1-(2,5-dimethoxyphenyl)-1-propanol #
(.+/-.)-.alpha.-(1-aminoethyl)-2,5-dimethoxybenzyl alcohol
AB00053731_12
AB00053731_13
DTXSID0023290
SBI-0050747.P003
Q685119
BRD-A39189014-003-14-4
SDCCGSBI-0050747.P004
NCGC00015692-13
2-(4-bromo-phenyl)-5-methyl-2h-pyrazole-3-carboxylicacid
EN300-365687

Research Excerpts

Overview

Methoxamine is an alpha-adrenergic drug. Its unique pharmacokinetics and mechanism of action on alpha-1 receptors lead to consider it as a first-choice drug for treating drug-induced or veno-occlusive priapism.

ExcerptReferenceRelevance
"Methoxamine is a blood-pressure increasing drug commonly used for maintaining intraoperative hemodynamics."( Dose-dependent effects of intravenous methoxamine infusion during hip-joint replacement surgery on postoperative cognitive dysfunction and blood TNF-α level in elderly patients: a randomized controlled trial.
Han, J; Liu, R; Sun, D; Sun, S; Wang, L; Yang, L, 2017
)
1.45
"Methoxamine is a pure alpha 1 agonist causing vasoconstriction and increased peripheral vascular resistance."( The roles of methoxamine and norepinephrine in electromechanical dissociation.
Sanders, AB, 1984
)
1.36
"Methoxamine is an alpha-adrenergic drug, its unique pharmacokinetics and mechanism of action on alpha-1 receptors lead to consider it, similarly to phenylephrine, as a first-choice drug for treating drug-induced or veno-occlusive priapism. "( Intracavernous methoxamine in the treatment of priapism.
Bueno, G; Hernandez, C; Jara, J; Moncada, I, 1998
)
2.1

Actions

Methoxamine did not inhibit the Cl- current evoked by either direct activation of adenylate cyclase with forskolin or inhibition of phosphodiesterase activity with 3-isobutyl-1-methylxanthine. Methoxamine tended to activate the cardiovascular system, but did not affect the release of ADH significantly.

ExcerptReferenceRelevance
"Methoxamine potentially promotes TNF-α expression, leading to an increased risk of POCD."( Dose-dependent effects of intravenous methoxamine infusion during hip-joint replacement surgery on postoperative cognitive dysfunction and blood TNF-α level in elderly patients: a randomized controlled trial.
Han, J; Liu, R; Sun, D; Sun, S; Wang, L; Yang, L, 2017
)
1.45
"Methoxamine did not enhance this immunological release reaction at concentrations up to 10(-6) M."( Modulation by alpha 2-adrenergic stimulation of IgE-mediated 14C-serotonin release from rat mast cells.
Ijichi, H; Kizu, A; Nakagawa, M; Shimamura, O; Yamasaki, Y, 1983
)
0.99
"Methoxamine tended to activate the cardiovascular system, but did not affect the release of ADH significantly."( The role of central alpha 1- and alpha 2-adrenoceptors in the regulation of vasopressin release and the cardiovascular system.
Iitake, K; Kimura, T; Matsui, K; Ota, K; Shoji, M; Yoshinaga, K, 1984
)
0.99
"Methoxamine did not inhibit the Cl- current evoked by either direct activation of adenylate cyclase with forskolin or inhibition of phosphodiesterase activity with 3-isobutyl-1-methylxanthine, indicating that alpha-adrenergic stimulation inhibits beta-adrenergic responses at a point upstream of adenylate cyclase activation."( Alpha 1-adrenergic inhibition of the beta-adrenergically activated Cl- current in guinea pig ventricular myocytes.
Harvey, RD; Hool, LC; Oleksa, LM, 1996
)
1.02
"Methoxamine produced an increase (0.5-2 mg/kg) or did not modify (0.01 and 3 mg/kg) spontaneous uterine motility."( Effects of methoxamine on spontaneous uterine activity and blood flow of the rat uterus 'in vivo'.
Estañ, L; Martinez-Mir, I; Morales-Olivas, FJ; Palop, V; Rubio, E; Tarazona, E, 1992
)
1.39

Treatment

Methoxamine treatment increased stroke work by 74 +/- 34%. ALOPEX predicted a 73 +/- 43% increase above control values. Methoxamine pretreatment also increased the sensitivity of alpha-oxoglutarate dehydrogenase in intact mitochondria.

ExcerptReferenceRelevance
"Methoxamine pretreatment also increased the sensitivity of alpha-oxoglutarate dehydrogenase in intact mitochondria to 10 nM--300 nM extramitochondrial Ca2+ during steady-state Ca2+ recycling across the inner membrane."( The alpha-adrenergic-mediated activation of Ca2+ influx into cardiac mitochondria. A possible mechanism for the regulation of intramitochondrial free CA2+.
Crompton, M; Kessar, P, 1981
)
0.98
"Methoxamine treatment increased stroke work by 74 +/- 34%, while ALOPEX predicted a 73 +/- 43% increase above control values."( Cardiovascular applications of the ALOPEX optimization technique.
Berger, DS; Friedrichs, GS; Micheli-Tzanakou, E, 1993
)
1.01

Toxicity

ExcerptReferenceRelevance
" Twenty-one adverse events were reported in 8 (30."( A randomised, controlled, crossover study to investigate the safety and response of 1R,2S-methoxamine hydrochloride (NRL001) on anal function in healthy volunteers.
Bush, D; Gruss, HJ; Jacobs, A; Pediconi, C; Scholefield, JH; Simpson, JA, 2014
)
0.62
" Thirty-nine adverse events were reported in 20 (76."( A randomised, controlled, crossover study to investigate the pharmacodynamics, pharmacokinetics and safety of 1R,2S-methoxamine hydrochloride (NRL001) in healthy elderly subjects.
Bell, D; Duffin, A; Gruss, HJ; Jacobs, A; Pediconi, C, 2014
)
0.61
" The most commonly reported adverse events (AEs) in the active treatment groups were paraesthesia and piloerection."( A double-blind, placebo-controlled, randomised, parallel-group, dose-escalating, repeat dose study in healthy volunteers to evaluate the safety, tolerability, pharmacodynamic effects and pharmacokinetics of the once daily rectal application of NRL001 supp
Bell, D; Duffin, A; Gruss, HJ; Jacobs, A; Pediconi, C, 2014
)
0.4
" Secondary outcomes include measures of efficacy of NRL001 compared with placebo following 8 weeks treatment; safety and tolerability; evaluation of plasma pharmacokinetics; establishment of any pharmacokinetic/pharmacodynamic relationship to adverse events; dose-response relationship; the efficacy of NRL001 therapy at 4 and 8 weeks assessed by the Vaizey score; and QoL using the Faecal Incontinence Quality of Life and the EQ-5D-5L Healthcare Questionnaires following 4 and 8 weeks NRL001 therapy."( Libertas: rationale and study design of a multicentre, Phase II, double-blind, randomised, placebo-controlled investigation to evaluate the efficacy, safety and tolerability of locally applied NRL001 in patients with faecal incontinence.
Jones, D; Scholefield, JH; Shing, RN; Siproudhis, L; Walker, D, 2014
)
0.4
" Whether pre-emptive methoxamine infusion is effective and safe to prevent spinal anesthesia-induced hypotension is still a controversial issue, to dress this knowledge lack, we performed a systemic review and meta-analysis to evaluated it."( The efficacy and safety of pre-emptive methoxamine infusion in preventing hypotension by in elderly patients receiving spinal anesthesia: A PRISMA-compliant protocol for systematic review and meta-analysis.
He, LX; Li, L; Yao, YT, 2022
)
1.31

Pharmacokinetics

This study aimed to assess the effects of a single dose of 10 mg NRL001 (the 1R,2S stereoisomer of methoxamine hydrochloride) in a 2 g suppository on pharmacodynamic and pharmacokinetic (PK) variables.

ExcerptReferenceRelevance
" In the remaining four patients, three were diagnosed by PCG alone and one by pharmacodynamic phonocardiography using methoxamine (ME-PCG)."( [Pulsed Doppler echocardiography and pharmacodynamic phonocardiography in the diagnosis of silent aortic regurgitation: a correlative study].
Amano, K; Hada, Y; Hasegawa, I; Ishimitsu, T; Sakamoto, T; Takahashi, H; Takahashi, T; Takenaka, K; Takikawa, R; Yamaguchi, T, 1985
)
0.48
" In conclusion, isolated mesenteric arteries from obese Zucker rats do not show relevant structural changes, and the pharmacodynamic behaviour of such vessels appears to be the same as that of control preparations."( Pharmacodynamic behaviour of isolated resistance vessels obtained from hypertensive-diabetic rats.
Kam, KL; Pfaffendorf, M; van Zwieten, PA, 1996
)
0.29
" This method was successfully applied to the analysis of the three drugs in rat plasma and their pharmacokinetic studies."( Pharmacokinetic study of three cardiovascular drugs by high-performance liquid chromatography using pre-column derivatization with 9,10-anthraquinone-2-sulfonyl chloride.
Cui, S; Feng, F; Liu, H; Ma, M; Xie, D; Xu, S, 2007
)
0.34
"This study aimed to assess the effects of a single dose of 10 mg NRL001 (the 1R,2S stereoisomer of methoxamine hydrochloride) in a 2 g suppository on pharmacodynamic and pharmacokinetic (PK) variables, and safety, in a healthy elderly population."( A randomised, controlled, crossover study to investigate the pharmacodynamics, pharmacokinetics and safety of 1R,2S-methoxamine hydrochloride (NRL001) in healthy elderly subjects.
Bell, D; Duffin, A; Gruss, HJ; Jacobs, A; Pediconi, C, 2014
)
0.83

Compound-Compound Interactions

ExcerptReferenceRelevance
" These data demonstrate that sequential treatment with BaP in combination with MeoA is associated with induction of highly proliferative phenotypes in GMCs characterized by differential expression of growth-related protooncogenes."( Induction of highly proliferative phenotypes in cultured glomerular mesangial cells by benzo[a]pyrene alone or in combination with methoxamine.
Bowes, RC; Ramos, KS; Weber, TJ, 1995
)
0.5

Dosage Studied

Benextramine displaced the dose-response curve to methoxamine to the right. renal alpha-adrenoceptors do not mediate renin secretion elicited by direct neural activation of the juxtaglomerular granular cells.

ExcerptRelevanceReference
" The dose-response curve for the chronotropic action of phenylephrine was parallel to that of isoprenaline, whilst the dose-response curve for the inotropic action of phenylephrine was less steep than that of isoprenaline."( Characterization of adrenoceptors mediating positive inotropic responses in the ventricular myocardium of the dog.
Endoh, M; Shimizu, T; Yanagisawa, T, 1978
)
0.26
" Values of KA and A50 were calculated from dose-response curves obtained for three alpha-adrenergic agonists (phenylephrine, methoxamine and norepinephrine) in the presence and absence of partial irreversible blockade by phenoxybenzamine."( Determination of the stimulus-response relation for three alpha-adrenergic agonists on rabbit aorta.
Gero, A; Raffa, RB; Tallarida, RJ, 1979
)
0.47
"In cumulative dose-response studies, strips from bladder neck of rabbit were significantly more sensitive to stimulation with noradrenaline, phenylephrine, and methoxamine than were strips from detrusor."( A difference in sensitivity to alpha-adrenergic agonists exhibited by detrusor and bladder neck of rabbit.
Awad, SA; Carro-Ciampi, G; Dean, DM; Downie, JW, 1975
)
0.45
" Dose-response curves for stimulant agonists were obtained in isolated vasa deferentia which were depolarized by a K-rich, Na-free solution."( The effects of denervation, cocaine, 6-hydroxydopamine and reserpine on the characteristics of drug-induced contractions of the depolarized smooth muscle of the rat and guinea-pig vas deferens.
Westfall, DP, 1977
)
0.26
" Dose-response curves to norepinephrine were shifted to the left along the log dose axis (enhanced potency) and the maximum degree of contraction that could be elicited was increased."( Influence of temperature and cocaine on responses of the isolated mouse vas deferens to adrenergic amines.
Bohuski, K; Buckner, CK; Ryan, CF, 1975
)
0.25
" Seven days after pretreatment with 6-hydroxydopamine there is a shift to the left and increase in maxima of the dose-response curves for norepinephrine and methoxamine."( The effect of pretreatment with 6-hydroxydopamine on the norepinephrine concentration and sensitivity of the rat vas deferens.
Fedan, JS; Westfall, DP,
)
0.33
" At 110 min after dosing, subjects took a slow, full inspiration with a 30 s breath-hold, and at 150 min after dosing the subjects performed one single forced expiration."( The effect of respiratory manoeuvres and pharmacological agents on the pharmacokinetics of nedocromil sodium after inhalation.
Holgate, ST; Honeywell, RG; Renwick, AG; Singh, S; Summers, QA, 1992
)
0.28
" The dose-response curves of these compounds in the former were shifted to the right and/or abolished, suggesting decreased sensitivity of LEW/N hypothalami to these neurotransmitters."( Neurotransmitter-induced hypothalamic-pituitary-adrenal axis responsiveness is defective in inflammatory disease-susceptible Lewis rats: in vivo and in vitro studies suggesting globally defective hypothalamic secretion of corticotropin-releasing hormone.
Aksentijevich, S; Bagdy, G; Bernardini, R; Calogero, AE; Chrousos, GP; Gold, PW; Smith, C; Sternberg, EM; Wilder, RL, 1992
)
0.28
" We performed dose-response curves to methoxamine, an alpha-adrenoceptor agonist, with and without N omega-nitro-L-arginine, a specific inhibitor of nitric oxide synthesis, in experimental portal hypertension."( The role of nitric oxide in the vascular hyporesponsiveness to methoxamine in portal hypertensive rats.
Albillos, A; Colombato, LA; Groszmann, RJ; Lee, FY, 1992
)
0.79
" Indices of amplification were leftward shifts of methoxamine dose-response (DR) curves produced by 5-HT (0."( Evidence for a 5-HT1-like receptor mediating the amplifying action of 5-HT in the rabbit ear artery.
de la Lande, IS, 1992
)
0.54
" Dose-response curves were constructed for methoxamine and sodium nitroprusside comparing the various dosages with systemic pressor and depressor responses, respectively."( Augmentation of baroreflex-mediated bradycardia in conscious pregnant rats.
Conrad, KP; Russ, RD, 1992
)
0.55
" Similarly, increased plasma renin activity induced by chronic salt depletion (0% NaCl) in pithed rats provoked a shift to the right of the dose-response curves to Ang II and ET-1 but not to MTX."( Cross-desensitization between angiotensin II and endothelin-1 in the pithed rat.
Auguet, M; Braquet, P; Chabrier, PE; Etiemble, E; Guillon, JM; Roubert, P, 1991
)
0.28
" Dose-response curves were obtained to bolus injections of 5-hydroxytryptamine (5-HT) in Krebs'-perfused hindquarters of male Wistar rats."( Thromboxane A2 receptor stimulation similarly potentiates pressor responses to 5-hydroxytryptamine in perfused hindquarters of non-diabetic and alloxan diabetic rats.
Hodgson, WC; King, RG; Sikorski, BW, 1991
)
0.28
" Dose-response curves for methoxamine and vasopressin were not significantly different between groups."( Does enhanced sympathetic tone contribute to angiotensin II hypertension in rats?
Chow, KY; Kline, RL; Mercer, PF, 1990
)
0.58
" Pretreatment of aortic rings with APIII (up to 3 x 10(-6) M) did not alter the normal ET-1 dose-response curve with respect to potency but did diminish the maximal contraction achieved."( Atrial natriuretic factor and endothelin interactions in control of vascular tone.
Novosad, EI; Opgenorth, TJ, 1990
)
0.28
" Cumulative forearm blood flow dose-response curves to three cumulative infusion rates (3 min each) of NE (0."( Verapamil and alpha-mediated vasoconstriction in human forearm: a comparison between norepinephrine and selective alpha 1- and alpha 2-adrenergic agonists.
Graziadei, L; Pana-Race, G; Pedrinelli, R; Salvetti, A; Taddei, S, 1987
)
0.27
" Analysis of cumulative dose-response curves showed that the two local anesthetics antagonized methoxamine and inhibited the field-stimulation response."( Effects of lidocaine and procaine on canine nasal blood vessels.
Jackson, RT; Wang, HW,
)
0.35
" The dose-response curve for methoxamine, but not for xylazine, was shifted to the left by the neuroleptic."( Increased peripheral alpha 1-adrenoceptor sensitivity following chronic thioridazine treatment in the pithed rat.
Badia, A; Cuffí, ML; Vila, E, 1989
)
0.57
" Benextramine (3, 6 and 12 mg/Kg) displaced the dose-response curve to methoxamine to the right."( Benextramine and nifedipine distinguish between sub-classes of alpha 1-adrenoceptors.
Tabrizchi, R; Triggle, CR, 1989
)
0.51
" The absence of a depression of the maximum of the dose-response curve of ST 587 and the very moderate attenuation of the maximal B-HT 920-induced increase in diastolic blood pressure (BP) confirms the lack of major calcium entry blocking properties of R 56865 for alpha-adrenoceptor-activated calcium channels in vitro."( Interaction between R 56865 and alpha-adrenoceptors in the pithed rat.
Fruh, C; Koch, P; Peters, T; Schneider, J; Wilffert, B; Wilhelm, D,
)
0.13
" Destruction of the endothelium in vitro had no effect on the responses to these 2 analogues and the log dose-response curve for [Ala1,15]endothelin-1 in the isolated mesentery was biphasic."( Vascular activities of endothelin-1 and some alanyl substituted analogues in resistance beds of the rat.
Douglas, SA; Hiley, CR; Randall, MD, 1989
)
0.28
" Methoxamine increased the tension of both normal and diabetic ventricles, but in diabetic ones, the dose-response curve to methoxamine was shifted to the left and the efficacy of the alpha-agonist was enhanced."( Alpha-adrenergic supersensitivity and decreased number of alpha-adrenoceptors in heart from acute diabetic rats.
Borda, ES; Sterin-Borda, L; Wald, M, 1988
)
1.19
" Methoxamine produced a dose-related increase in uterine activity, prazosin produced a rightward displacement of the dose-response curve of methoxamine reaching the same maximal effect."( Effect of methoxamine on spontaneous motility of the isolated rat uterus.
Esplugues, J; Estañ, L; Morales-Olivas, FJ; Rubio, E, 1985
)
1.58
" In the presence of Tris, the cumulative dose-response curve to norepinephrine was significantly shifted to the left, whereas methoxamine dose-response curves were similar in both buffers."( Tris buffer effects on melanophore aggregating responses.
Castrucci, AM; Visconti, MA, 1985
)
0.48
" Decreasing [Mg2+]0 from the optimal concentration of 1 to 0 mM caused a 20-fold parallel rightward displacement of the oxytocin dose-response curve."( Magnesium ions and oxytocin sensitivity of the male mouse anococcygeus.
Gibson, A, 1985
)
0.27
" Met (1 X 10(-6) M) increased the tension of both normal and diabetic atria, but in diabetic atria, the dose-response curve to Met was shifted to the left and the efficacy of Met was enhanced."( Hypersensitivity to methoxamine in atria isolated from streptozotocin-induced diabetic rats.
Canga, L; Sterin-Borda, L, 1986
)
0.59
" In the rat tail artery, there were no differences in the dose-response relationships to noradrenaline, methoxamine, and KCl whether the agonists were applied as single or cumulative doses."( Desensitization of the vascular contractile response to cumulative doses of alpha 2-adrenoceptor agonists.
Cheung, DW, 1986
)
0.49
" Cumulative dose-response curves to intra-arterial methoxamine or B-HT 933 were obtained during saline or two different rates of verapamil infusion (0."( Verapamil antagonizes forearm vasoconstriction mediated by selective alpha 1- and alpha 2-agonists in hypertensive patients.
Graziadei, L; Panarace, G; Pedrinelli, R; Salvetti, A; Taddei, S, 1986
)
0.52
" The dose-response curves obtained with vasopressin and methoxamine were not significantly different between control and diabetic animals."( Evidence for regionally selective changes in response to potassium chloride but not vasopressin or methoxamine in vasculature from diabetic rats.
Doroudian, A; Hebden, RA; McNeill, JH, 1988
)
0.74
" Complete dose-response curves were generated to methoxamine, phenylephrine, and norepinephrine."( Vascular catecholamine sensitivity during pregnancy in the ewe.
Cooke, R; Keve, TM; McLaughlin, MK, 1989
)
0.53
"3 mg/kg) in presence of prazosin shifted the norepinephrine pressor dose-response curves to the right whereas it was ineffective in yohimbine-pretreated animals."( Calcium entry blockade by nitrendipine and alpha adrenergic responsiveness in vivo: comparison with noncalcium entry blocker vasodilators in absence and presence of phenoxybenzamine pretreatment.
Pedrinelli, R; Tarazi, RC, 1985
)
0.27
" Dose-response studies of the effect of epinephrine on adenosine-deaminase or isoproterenol-stimulated fat-cells demonstrate an inhibitory effect of epinephrine on lipolysis promoted by stimulation of alpha 2-adrenoceptors which occurs before the commonly described beta 1-adrenergic effect which promotes stimulation of lipolysis."( Fat cell adrenoceptors: inter- and intraspecific differences and hormone regulation.
Berlan, M; Carpene, C; Lafontan, M, 1985
)
0.27
" Dose-response curves were constructed to noradrenaline (alpha 1/alpha 2), methoxamine (alpha 1-selective) and B-HT 920 (alpha 2-selective)."( Characterization of post-junctional alpha-adrenoceptors in the rat isolated perfused femoral artery.
Dyke, AC; Widdop, RE, 1987
)
0.5
" The norepinephrine- and methoxamine-induced dose-response curves were similar in both SAD and SO groups on day 3, but shifted to the left on days 7 and 15 and demonstrated a tendency to shift to the right at 30 days."( Contractile reactivity of the perfused mesenteric vascular bed from sinoaortic denervated rats to norepinephrine, methoxamine and verapamil.
Bissoli, NS; Cabral, AM; Moyses, MR; Vasquez, EC, 1988
)
0.79
" For each agent tested in this study, dose-response curves were established."( Micturition in the unanesthetized rat: spinal vs. peripheral pharmacology of the adrenergic system.
Durant, PA; Lucas, PC; Yaksh, TL, 1988
)
0.27
" Dose-response curves for methoxamine documented its positive, but different, inotropic actions in the two groups and at the four periods of the estrous cycle."( Prostaglandin output from and the spontaneous inotropism of uterine horns isolated from underfed rats at different stages of the sex cycle. Smooth muscle contractile influences of indomethacin and of methoxamine.
Gimeno, AL; Gimeno, MA; Goldraij, A; Sterin, AB, 1987
)
0.76
" The dose-response curves to methacholine reached a plateau or maximal effect after a 30 to 50% fall in FEV1 in 14 of the 16 smokers challenged."( Characteristics of bronchial hyperresponsiveness in smokers with chronic air-flow limitation.
Black, JL; Du Toit, JI; Salome, CM; Sundrum, R; Woolcock, AJ, 1986
)
0.27
" The dose-response effect of a pure alpha-adrenergic agonist, methoxamine, on regional myocardial blood flow has not been investigated in this setting."( The effect of epinephrine versus methoxamine on regional myocardial blood flow and defibrillation rates following a prolonged cardiorespiratory arrest in a swine model.
Brown, CG; Davis, EA; Hamlin, RL; Katz, SE; Luu, T; Werman, HA, 1987
)
0.79
" When dose-response curves to an alpha adrenergic agonist were obtained in the presence of a threshold concentration of the same or another alpha agonist, the curve was shifted to the left at threshold but converged with the control curve between ED10 and ED70."( Vasoconstrictor threshold synergism and potentiation in the rabbit isolated thoracic aorta.
Murray, DL; Purdy, RE; Stupecky, GL, 1986
)
0.27
" The content of high-tyrosine proteins in wool was still depressed in most sheep 70 days after dosing with methoxinine."( Effects of phenylalanine and analogues of methionine and phenylalanine on the composition of wool and mouse hair.
Gillespie, JM; Reis, PJ, 1985
)
0.27
" Nifedipine shifted the pressor dose-response curves of all three agonists to the right."( Nifedipine and alpha adrenoceptor antagonism.
Brown, MJ; Dollery, CT; Heavey, DJ; Murphy, MB; Scriven, AJ, 1984
)
0.27
" Based on the inability of phentolamine and prazosin to prevent neurally mediated renin secretion and on the dose-response relationship between methoxamine and changes in renin secretion, renal blood flow, and urinary sodium excretion, we conclude that renal alpha-adrenoceptors do not mediate renin secretion elicited by direct neural activation of the juxtaglomerular granular cells."( Role of renal alpha-adrenoceptors mediating renin secretion.
DiBona, GF; Osborn, JL; Thames, MD, 1982
)
0.46
" Cumulative dose-response curves to noradrenaline and methoxamine on the circular contraction of isolated iliac arteries showed a significant shift to the right, together with a reduction in the maximal contraction."( Vascular reactivity in perinatally undernourished rats.
Del Basso, P; Keller, EA; Orsingher, OA; Salica, C, 1983
)
0.51
" In the presence of L (8 X 10(5) ml-1) the dose-response curve to Me shifted to the left and the efficacy of Me was enhanced."( alpha-Adrenoceptor stimulated lymphocytes trigger the mechanical response of vas deferens: participation of arachidonic acid metabolites.
Borda, ES; Cangiani, S; de Bracco, MM; Finiasz, M; Sterin-Borda, L, 1984
)
0.27
" The effects of CU 32-085 and bromocriptine on dose-response curves to sympathomimetic agents (adrenaline, noradrenaline, methoxamine and clonidine), intravenously administered, were also studied."( Hypotensive action and alpha-adrenolytic properties of a new dopaminergic agonist, CU 32-085, in the rat.
Esplugues, J; Morales-Olivas, FJ; Palop, V; Rubio, E, 1984
)
0.48
" Norepinephrine ED50 values and dissociation constants (KA) were determined by analysis of dose-response data with and without partial inactivation of alpha receptors by phenoxybenzamine."( Qualitative and quantitative differences between the postsynaptic alpha adrenoceptors of rabbit ear artery and thoracic aorta.
Ashbrook, DW; Purdy, RE; Stupecky, GL; Watanabe, MY, 1983
)
0.27
" All three alpha antagonists employed produced in innervated glands parallel displacements of the dose-response curves to norepinephrine, prazosin being 30 and 100 times more potent than phentolamine and yohimbine, respectively."( Alpha-1 adrenoceptors mediate secretory responses to norepinephrine in innervated and denervated rat submaxillary glands.
Elverdin, JC; Luchelli-Fortis, MA; Perec, CJ; Stefano, FJ, 1984
)
0.27
") evoked dose-dependent shifts to the right of the dose-response curves to B-HT 933 whilst having minimal effects on the methoxamine dose-response curve."( An investigation into the selectivity of a novel series of benzoquinolizines for alpha 2-adrenoceptors in vivo.
Paciorek, PM; Pierce, V; Shepperson, NB; Waterfall, JF, 1984
)
0.48
" Cumulative dose-response curves for isoproterenol, norepinephrine and methoxamine were made for the different groups."( In vitro contractile responses of the uterus from 'restricted diet' rats to adrenoceptor agonists. Influence of cyclo-oxygenase inhibitors.
Gimeno, AL; Gimeno, MA; Goldraij, A; Sterin, AB, 1983
)
0.5
" When the dosage of dobutamine was increased to 200 micrograms ."( Effects of adrenergic agonists on electrolyte transport in perfused salivary duct of rat.
Jirakulsomchok, D; Schneyer, CA, 1984
)
0.27
" Dose-response curves obtained by infusing Ca2+ (2-8 mg X min-1 X kg-1) were identical in N and Db."( Enhanced sensitivity of diabetic hearts to alpha-adrenoceptor stimulation.
Downing, SE; Fripp, RR; Lee, JC, 1983
)
0.27
") was administered at 30 min intervals on four experimental days: no pretreatment; after prazosin 1 mg/kg and infusion; after pharmacological 'total' autonomic effector block (TAB) and with repeated three point methoxamine dose-response lines."( Haemodynamic response to ketanserin in rabbits with Page hypertension: comparison with prazosin.
Angus, JA; Wright, CE, 1983
)
0.45
"Cumulative dose-response curves were produced for the effect of different adrenergic agonists on the contractions of uterine strips from natural estrous and ovariectomized rats."( Inhibitory effects of some catecholamines on contractions of uterine strips isolated from estrous and spayed rats. Influence of endogenous and exogenous prostaglandins on the action of methoxamine.
Agostini, MC; Borda, E; Gimeno, AL; Gimeno, MF; Sterin-Borda, L, 1981
)
0.45
" Agents were compared over dosage ranges that produced maximal increases in QTc interval and monophasic action potential duration (MAPD)."( Comparative assessment of ibutilide, D-sotalol, clofilium, E-4031, and UK-68,798 in a rabbit model of proarrhythmia.
Brunden, MN; Buchanan, LV; Gibson, JK; Kabell, G, 1993
)
0.29
"As atrial natriuretic factor (ANF) is intimately involved in water and electrolyte homeostasis, dose-response studies were performed in the parotid as well as submaxillary glands of the rat with increasing doses of the atrial peptide to investigate its possible role as a sialogogic agent."( Atrial natriuretic factor enhances induced salivary secretion in the rat.
Bianciotti, LG; Colatrella, C; Elverdin, JC; Fernández, BE; Vatta, MS, 1994
)
0.29
" At all time periods under L-NAME and 2 weeks after stopping treatment, the dose-response to norepinephrine was significantly more sensitive than in controls, with a concomitant slight increase in efficacy."( Resistance artery structure and neuroeffector mechanisms in hypertension induced by inhibition of nitric oxide synthase.
Li, JS; Schiffrin, EL, 1994
)
0.29
" Nifedipine (100 micrograms/kg, 300 micrograms/kg, and 1000 micrograms/kg) inhibited in a dose-dependent manner the pressor responses to the alpha 1- and alpha 2-adrenoceptor agonists, the dose-response curves to the alpha 2-adrenoceptor agonists being shifted further to the right."( A comparison of the effects of TMB-8 and nifedipine on pressor responses to alpha 1- and alpha 2-adrenoceptor agonists in pithed rats.
Aleixandre, MA; Pintado, A; Puerro, M, 1995
)
0.29
" In each subject, dose-response curves for the effects on forced expiratory volume in one second (FEV1) of serially doubling doses of inhaled histamine were obtained on three different days, 15 min after pretreatment with either methoxamine (10 mg) or duplicated placebo."( Effects of pretreatment with inhaled methoxamine on bronchial responses to histamine in asthmatic subjects.
Dall'Ava-Santucci, J; Dinh-Xuan, AT; Lockhart, A; Monchi, M; Phan-Puibaraud, TT; Regnard, J, 1995
)
0.75
" Inclusion of cadmium (30 microM) in the physiological salt solution significantly reduced the maximum response, without significantly altering the ED50 or the Hill coefficient of the dose-response curve to methoxamine."( Role of intracellular and extracellular calcium in alpha 1-adrenoceptor-mediated vasoconstriction in the rat perfused hindquarters.
Tabrizchi, R,
)
0.32
" At 16 weeks of age more-complete dose-response curves to the alpha 1-agonist methoxamine were also constructed."( Arterial hypertrophy and pressor responsiveness during development of hypertension in spontaneously hypertensive rats.
Lee, RM; Leenen, FH; Tsoporis, J; Yuan, B, 1994
)
0.52
") produced a moderate--but significant--rightward displacement of the dose-response curves to all agonists."( [The alpha-antiadrenergic properties of spiroxatrine, a ligand of serotonergic 5-HT1A receptors].
Hong, E; Ibarra, M; Ransanz, V; Terrón, JA; Villalón, CM,
)
0.13
" The slopes of the dose-response curves for noradrenaline, phenylephrine and methoxamine and frequency-response curves for renal nerve stimulation generated at each dose level of BRL38227 could not be distinguished statistically."( Effect of BRL 38227 on the adrenergic regulation of the kidney vasculature of the rat.
Johns, EJ, 1993
)
0.51
" S(-)-propranolol 10(-5) M also inhibited vasoconstriction induced by methoxamine, shifting the dose-response curves to the right, but did not affect pressor responses to arginine-vasopressin."( Propranolol stereoselectively inhibits alpha-adrenoceptor-mediated vasoconstriction in mesenteric arterial beds of rats.
Heinemann, A; Stauber, RE, 1996
)
0.53
" In thoracic aortic strips with intact endothelium, the first and second (1 h later) dose-response curves obtained with methoxamine were almost the same."( A comparative study on the rat aorta and mesenteric arterial bed of the possible role of nitric oxide in the desensitization of the vasoconstrictor response to an alpha 1-adrenoceptor agonist.
Kamata, K; Makino, A, 1997
)
0.51
"A sensitive spectrophotometric assay has been developed for the determination of methoxamine in pure dosage form and in its pharmaceutical preparations."( Spectrophotometric determination of methoxamine using cerium(IV) in presence of sodium lauryl sulphate and rhodamine-B.
al-Obaid, AM; Alwarthan, AA, 1997
)
0.8
" Pharmacological effects on forearm blood flow (FBF) are usually expressed by means of dose-response relationships."( Calculation of plasma concentrations of intra-arterially infused compounds in forearm plethysmography.
Bruning, TA; Chang, PC; Kemme, MJ; Muizert, Y; van Zwieten, PA, 1998
)
0.3
" There was no effect of NPY on postjunctional ACh or isoprenaline agonist dose-response curves."( Exogenous NPY modulation of cardiac autonomic reflexes and its pressor effect in the conscious rabbit.
Angus, JA; Serone, AP; Wright, CE, 1998
)
0.3
" The dose-response curve for methoxamine was shifted to the right and the maximum contractile response was impaired in mesenteric arterial beds from diabetic rats."( Possible modulation by endothelin-1, nitric oxide, prostaglandin I2 and thromboxane A2 of vasoconstriction induced by an alpha-agonist in mesenteric arterial bed from diabetic rats.
Kamata, K; Makino, A, 1998
)
0.59
" Apparent rate constants for methoxamine binding and unbinding gave Kd values in agreement with EC50 values measured from dose-response relations."( Non-specific action of methoxamine on Ito, and the cloned channels hKv 1.5 and Kv 4.2.
Fedida, D; Li, Q; Parker, C, 1999
)
0.91
" Analysis of the dose-response curves of beta-adrenergic agonists yielded an EC50 of 5 x 10-9 and 1 x 10-11 M for adrenaline and isoproterenol, respectively."( Beta-adrenergic agonists regulate cell membrane fluctuations of human erythrocytes.
Gulayev, N; Korenstein, R; Levin, S; Moses, A; Tuvia, S, 1999
)
0.3
" In each session, dose-response curves to both locally infused noradrenaline acid tartrate (0."( Comparison of the effects of venlafaxine, desipramine, and paroxetine on noradrenaline- and methoxamine-evoked constriction of the dorsal hand vein.
Abdelmawla, AH; Bradshaw, CM; Langley, RW; Szabadi, E, 1999
)
0.52
"In vitro-perfused SMA vascular beds were tested for the cumulative dose-response to octreotide at baseline conditions and after preconstriction with different vasoconstrictors (alpha1-agonist methoxamine, endothelin [ET-1], phorbol ester [PdBu], and potassium chloride [KCl])."( Octreotide potentiates PKC-dependent vasoconstrictors in portal-hypertensive and control rats.
Groszmann, RJ; Tsai, MH; Wiest, R, 2001
)
0.5
" Concentration-dependent dose-response curves to acetylcholine (10(-8)-10(-5) M), sodium nitroprusside (10-6(-5) x 10(-4) M), and adenosine triphosphate (ATP) (10(-8)-10(-5) M) in the hepatic artery were constructed after the tone was raised by addition of methoxamine (3 micorM L(-1))."( Nitric oxide modulates acetylcholine-induced vasodilatation in the hepatic arterial vasculature of the dual-perfused rat liver.
Alexander, B; Benjamin, IS; Yang, W, 2001
)
0.49
" The present studies show that the inhibition of memory by high doses of noradrenaline is mimicked by the alpha1-AR agonist methoxamine, and the dose-response curve is shifted to the right by pretreatment with the alpha1-AR antagonist prazosin."( Stimulation of alpha1-adrenoceptors inhibits memory consolidation in the chick.
Gibbs, ME; Summers, RJ, 2001
)
0.52
" The dilator and constrictor dose-response curves were combined into a single relationship for MAP, cardiac output, total peripheral conductance (TPC) and heart rate; total peripheral resistance (TPR) was estimated as 1/TPC."( Structural factors increase blood pressure through the interaction of resistance vessel geometry with neurohumoral and local factors: estimates in rabbits with renal cellophane-wrap hypertension with intact effectors and during neurohumoral blockade.
Angus, JA; Korner, PI; Wright, CE, 2002
)
0.31
" A portal perfusion pressure dose-response curve to methoxamine was performed in control and cirrhotic rat livers preincubated with vehicle, the nitric oxide synthase blocker N(G)-nitro-L-arginine (L-NNA), indomethacin cyclooxygenase (COX) inhibitor, L-NNA + indomethacin, or the thromboxane (TX) A(2) receptor blocker SQ 29,548."( Cyclooxygenase-derived products modulate the increased intrahepatic resistance of cirrhotic rat livers.
Abraldes, JG; Bosch, J; Bragulat, M; Corominola, H; García-Pagán, JC; Graupera, M; Peralta, C; Rodés, J, 2003
)
0.57
" Administration of both non-selective and selective alpha-adrenoceptor agonists in doses of 1-40 microg noradrenaline kg(-1) body weight (BW), 1-100 microg clonidine kg(-1) BW, or 100-800 mg methoxamine kg(-1) BW enhanced contractions of the proximal cauda epididymidis in a dose-response manner."( Mediation of contraction in rat cauda epididymidis by alpha-adrenoceptors.
Chaturapanich, G; Maythaarttaphong, S; Pholpramool, C; Verawatnapakul, V, 2002
)
0.5
" Cumulative dose-response curve of methoxamine was constructed to determine the peroxidase secretion by glands from proestrous, estrous, metestrous and diestrous rats."( Hormonal influence on expression and functionality of alpha1-adrenoceptor in rat submandibular gland.
Anesini, C; Borda, E, 2003
)
0.6
" The dose-response curve for methoxamine was shifted to the right and the maximum contractile response was reduced in mesenteric arterial beds from beef tallow-fed rats, but the modulation of this response induced by L-arginine plus BSA was preserved."( Modulations of shear stress-induced contractile responses and agonist-induced vasodilation in hypercholesterolemic rats.
Kamata, K; Kobayashi, T; Matsumoto, T; Sato, A; Suenaga, H, 2004
)
0.61
" Drug dosage determined the degree of nasal mucosa contraction."( A new in vitro method of decongestant assay of nasal mucosa: a preliminary report.
Chu, YH; Kao, CH; Wang, HW,
)
0.13
"In this study, drug dosage determined the degree of nasal mucosa contraction."( A new in vitro method of decongestant assay of nasal mucosa: a preliminary report.
Chu, YH; Kao, CH; Wang, HW,
)
0.13
" After 21 days, rats fed casein 0% presented: (a) a significant shift to the left of the dose-response curves (DRC) to the autonomic agonists-norepinephrine (NE), methoxamine, isoproterenol (ISO) and methacholine; (b) increased food consumption (p<0."( Protein free diet feeding: effects on sympathetic activity and salivary evoked secretion in the submandibular gland of the rat.
Bianciotti, LG; Boyer, P; Chiarenza, AP; Elverdin, JC; Luchelli, MA; Vacas, MI; Vatta, M, 2006
)
0.53
" At higher concentrations, 3 x 10(-5) and 10(-4) m, of the antagonist, the agonist dose-response curve was shifted to the right with a decrease in the maximum effect."( Antagonism by imidazoline-type drugs of muscarinic and other receptors in the guinea-pig ileum.
Miller, DD; Patil, PN; Salazar-Bookaman, MM, 2006
)
0.33
" Dose-response curves to the Ca(2+) ionophore A-23187 and to the calmodulin/myosin light chain kinase inhibitor W-7 served to study Ca(2+)-dependent pathways."( Both Ca2+ -dependent and -independent pathways are involved in rat hepatic stellate cell contraction and intrahepatic hyperresponsiveness to methoxamine.
Bisschops, R; Cassiman, D; Fevery, J; Laleman, W; Nevens, F; Roskams, T; Severi, T; Van Landeghem, L; Van Pelt, J; Vander Elst, I; Zeegers, M, 2007
)
0.54
" Dose-response curves to methoxamine (alpha(1)-adrenergic agonist) were obtained in the absence or the presence of the nitric oxide synthase inhibitor N-monomethyl-L-arginine."( Decreased intrahepatic response to alpha(1)-adrenergic agonists in lipopolysaccharide-treated rats is located in the sinusoidal area and depends on Kupffer cell function.
Abraldes, JG; Groszmann, RJ; Haq, O; Iwakiri, Y; Lee, CH; Loureiro-Silva, MR, 2007
)
0.64
" Although prazosin (10 microg/kg/min) markedly shifted the phenylephrine (alpha(1)-agonist) dose-response curve to the right, it did not have any effect on clofilium-induced prolongation of QTc and MAPD(90) (43 +/- 7 and 53 +/- 9%, respectively) or the occurrence of TdP (seven of eight)."( Antitorsadogenic effects of ({+/-})-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits.
Belardinelli, L; Dhalla, AK; Robertson, C; Wang, WQ, 2008
)
0.35
" For each condition extended scaled dose (ScD)-TPC and TPR curves were derived from individual dose-response curves to two constrictors and two dilators."( A new approach to assessing the structural total peripheral resistance amplifier in renal (Page) hypertension in conscious rabbits.
Angus, JA; Korner, PI; Wright, CE, 2010
)
0.36
" Dose-response relationships for the elevation of mean arterial pressure or change in heart rate (HR) in response to intravenous injections of noradrenaline (NA), phenylephrine (PE), methoxamine (ME) and Ang II were determined."( The effect of losartan and carvedilol on vasopressor responses to adrenergic agonists and angiotensin II in the systemic circulation of Sprague Dawley rats.
Abdulla, MH; Abdullah, NA; Anand Swarup, KR; Johns, EJ; Khan, MA; Sattar, MA,
)
0.32
" Hepatic endothelial function was assessed in isolated and perfused rat livers by dose-response curves to acetylcholine (ACh) and methoxamine (Mtx)."( Chronic intermittent hypoxia aggravates intrahepatic endothelial dysfunction in cirrhotic rats.
Abrante, B; Abreu, P; de Ganzo, ZA; Felipe, V; González-Méndez, Y; Hernández-Guerra, M; Moreno, M; Quintero, E; Salido, E, 2013
)
0.59
"This was a Phase I, single-centre, randomised, double-blind, three-way crossover study during which subjects received three single doses of 1 g rectal suppositories (containing 5 or 10 mg NRL001 or matching placebo) or 2 g rectal suppositories (containing 10 or 15 mg NRL001 or matching placebo) on three separate dosing days."( A randomised, controlled, crossover study to investigate the safety and response of 1R,2S-methoxamine hydrochloride (NRL001) on anal function in healthy volunteers.
Bush, D; Gruss, HJ; Jacobs, A; Pediconi, C; Scholefield, JH; Simpson, JA, 2014
)
0.62
"Twenty-six subjects were dosed with study medication."( A randomised, controlled, crossover study to investigate the safety and response of 1R,2S-methoxamine hydrochloride (NRL001) on anal function in healthy volunteers.
Bush, D; Gruss, HJ; Jacobs, A; Pediconi, C; Scholefield, JH; Simpson, JA, 2014
)
0.62
"Twenty-six subjects were dosed with study medication."( A randomised, controlled, crossover study to investigate the pharmacodynamics, pharmacokinetics and safety of 1R,2S-methoxamine hydrochloride (NRL001) in healthy elderly subjects.
Bell, D; Duffin, A; Gruss, HJ; Jacobs, A; Pediconi, C, 2014
)
0.61
"Treatment with NRL001 was generally well tolerated over 14 days once daily dosing and plasma NRL001 did not accumulate over time."( A double-blind, placebo-controlled, randomised, parallel-group, dose-escalating, repeat dose study in healthy volunteers to evaluate the safety, tolerability, pharmacodynamic effects and pharmacokinetics of the once daily rectal application of NRL001 supp
Bell, D; Duffin, A; Gruss, HJ; Jacobs, A; Pediconi, C, 2014
)
0.4
" Secondary outcomes include measures of efficacy of NRL001 compared with placebo following 8 weeks treatment; safety and tolerability; evaluation of plasma pharmacokinetics; establishment of any pharmacokinetic/pharmacodynamic relationship to adverse events; dose-response relationship; the efficacy of NRL001 therapy at 4 and 8 weeks assessed by the Vaizey score; and QoL using the Faecal Incontinence Quality of Life and the EQ-5D-5L Healthcare Questionnaires following 4 and 8 weeks NRL001 therapy."( Libertas: rationale and study design of a multicentre, Phase II, double-blind, randomised, placebo-controlled investigation to evaluate the efficacy, safety and tolerability of locally applied NRL001 in patients with faecal incontinence.
Jones, D; Scholefield, JH; Shing, RN; Siproudhis, L; Walker, D, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antihypotensive agentA cardiovascular drug that tends to raise reduced blood pressure.
alpha-adrenergic agonistAn agent that selectively binds to and activates alpha-adrenergic receptors.
[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 (1)

ClassDescription
amphetaminesAmines that constitute a class of central nervous system stimulants based on the structure of the parent amphetamine 1-phenylpropan-2-amine.
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency8.19950.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency4.57230.100020.879379.4328AID488773; AID588453
GLS proteinHomo sapiens (human)Potency22.38720.35487.935539.8107AID624146
arylsulfatase AHomo sapiens (human)Potency0.26851.069113.955137.9330AID720538
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency14.68920.016525.307841.3999AID602332
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.75690.060110.745337.9330AID485368
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
[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)
Alpha-1D adrenergic receptorHomo sapiens (human)Kb0.01100.00000.03470.1650AID36273
Alpha-1A adrenergic receptorHomo sapiens (human)Kb0.01100.00020.05100.3380AID36273
Alpha-1B adrenergic receptorHomo sapiens (human)Kb0.01100.00000.05120.2660AID36273
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID36273Dissociation constant for Alpha-1-adrenergic receptor was determined before and after addition of phentolamine1982Journal of medicinal chemistry, Feb, Volume: 25, Issue:2
alpha-Adrenergic agents. 2. Synthesis and alpha 1-agonist activity of 2-aminotetralins.
AID33265Tested for Alpha adrenergic receptor agonistic activity on isolated rat vas deferens1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties of 1-(2,5-dimethoxyphenyl)-2-aminoethanols and their morpholine analogues.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1146005Induction of magnesium accumulation in rat adipocyte plasma membrane vesicles assessed as increase of magnesium level per gram of protein per 30 mins at 2 x 10'-4 M by fluorescence assay1977Journal of medicinal chemistry, Apr, Volume: 20, Issue:4
Evidence for separate peptide sequences related to the lipolytic and magnesium-accumulating activities of ACTH. Analogy with adrenergic receptors.
AID36658Approximate efficacy based on maximal effect produced by methoxamine was determined against the alpha-2 adrenergic receptor1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
2-Amino- and 2-guanidino-1,2,3,4-tetrahydro-1,4-epoxynaphthalenes as conformationally defined analogues of alpha-adrenergic agents.
AID33267Tested for Alpha adrenergic receptor agonistic activity on isolated rat vas deferens1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties of 1-(2,5-dimethoxyphenyl)-2-aminoethanols and their morpholine analogues.
AID36419Alpha-1 adrenergic receptor agonist activity in rabbit ear artery1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Alpha-adrenergic agents. 1. Direct-acting alpha 1 agonists related to methoxamine.
AID197169Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36715Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.4 nM) to rat isolated brain membranes by 50% was reported.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36262Alpha-1 adrenergic receptor activation causing vasoconstriction in the isolated rabbit ear artery1982Journal of medicinal chemistry, Feb, Volume: 25, Issue:2
alpha-Adrenergic agents. 2. Synthesis and alpha 1-agonist activity of 2-aminotetralins.
AID166802Phentolamine dissociation constant was evaluated in rabbit ear artery1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Alpha-adrenergic agents. 1. Direct-acting alpha 1 agonists related to methoxamine.
AID3678350% inhibition of specific [3H]clonidine binding (0.4 nM) to Alpha-2 adrenergic receptors in rat isolated brain membranes1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID35490Evaluated for alpha-2 adrenergic receptor activity in the field stimulated rat vas deferens preparation1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
2-Amino- and 2-guanidino-1,2,3,4-tetrahydro-1,4-epoxynaphthalenes as conformationally defined analogues of alpha-adrenergic agents.
AID1146004Induction of magnesium accumulation in rat adipocyte plasma membrane vesicles assessed as increase of intravesicular magnesium level per 30 mins at 2 x 10'-4 M by fluorescence assay1977Journal of medicinal chemistry, Apr, Volume: 20, Issue:4
Evidence for separate peptide sequences related to the lipolytic and magnesium-accumulating activities of ACTH. Analogy with adrenergic receptors.
AID1346000Human alpha1B-adrenoceptor (Adrenoceptors)1995Molecular pharmacology, Aug, Volume: 48, Issue:2
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
AID1345920Rat alpha1D-adrenoceptor (Adrenoceptors)1994Molecular pharmacology, Nov, Volume: 46, Issue:5
Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1999British journal of pharmacology, Jun, Volume: 127, Issue:4
Microphysiometric analysis of human alpha1a-adrenoceptor expressed in Chinese hamster ovary cells.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1995Molecular pharmacology, Aug, Volume: 48, Issue:2
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
AID1345971Human alpha1D-adrenoceptor (Adrenoceptors)1995Molecular pharmacology, Aug, Volume: 48, Issue:2
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,015)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901222 (60.65)18.7374
1990's515 (25.56)18.2507
2000's185 (9.18)29.6817
2010's78 (3.87)24.3611
2020's15 (0.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.50

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 Index44.50 (24.57)
Research Supply Index7.69 (2.92)
Research Growth Index4.12 (4.65)
Search Engine Demand Index76.15 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (44.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials57 (2.67%)5.53%
Reviews55 (2.58%)6.00%
Case Studies23 (1.08%)4.05%
Observational0 (0.00%)0.25%
Other2,000 (93.68%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Proof of Concept Study in Healthy Volunteers to Investigate the Safety and Response to a Single Dose of 10mg Methoxamine (NRL001) Applied Locally Using a Suppository to the Anal Canal or Rectum [NCT00893607]Phase 124 participants (Actual)Interventional2007-04-30Completed
A Multi-centre, Phase II, Double-blind, Randomised, Placebo-controlled, Parallel Group, Dose-ranging Study in Patients With Faecal Incontinence; to Evaluate the Efficacy, Safety and Tolerability of Locally Applied NRL001 Over an 8 Week Treatment Period [NCT01656720]Phase 2417 participants (Actual)Interventional2012-02-29Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]