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guanethidine

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Description

Guanethidine is a potent antihypertensive drug that acts as a postganglionic sympathetic neuron blocker. It was synthesized in the 1950s and became widely used in the treatment of hypertension. Guanethidine works by inhibiting the release of norepinephrine from sympathetic nerve endings, thereby reducing sympathetic nervous system activity. This leads to a decrease in blood pressure. Guanethidine is no longer widely used due to its adverse effects, such as orthostatic hypotension, diarrhea, and impotence. However, it remains an important research tool for studying the role of the sympathetic nervous system in various physiological processes. Guanethidine is also used in the treatment of certain types of pheochromocytoma, a rare tumor of the adrenal medulla that produces excessive amounts of catecholamines.'
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Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group. [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]

guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid. [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 CID3518
CHEMBL ID765
CHEBI ID5557
SCHEMBL ID34753
MeSH IDM0009675

Synonyms (120)

Synonym
octatensin
ismelin
su 5864 sulfate (1:1)
octadine
guanetidin sulfate
isobarin
octadin
nsc29863
guanethidine sulfate
oktadin
sanotensin
iporal
KBIO1_000539
DIVK1C_000539
1-(2-azocan-1-ylethyl)guanidine
SPECTRUM_000837
BSPBIO_002092
einecs 200-241-3
eutensol
guanethidinum [inn-latin]
octatensine
azocine, 1-((2-(aminoiminomethyl)amino)ethyl)octahydro-
guanethidine [inn:ban]
oktatenzin
hsdb 3092
oktatensin
abapresin
((2-hexahydro-1(2h)-azocinyl)ethyl)guanidine
guanetidina [inn-spanish]
dopam
dopom
NCGC00016272-01
cas-60-02-6
PRESTWICK2_000317
SPECTRUM5_000784
BPBIO1_000346
BSPBIO_000314
PRESTWICK3_000317
guanetidina
CHEBI:5557 ,
guanethidinum
1-[2-(azocan-1-yl)ethyl]guanidine
guanidine, n-[2-(hexahydro-1(2h)-azocinyl)ethyl]-
azocine, 1-(2-guanidinoethyl)octahydro-
.beta.-1-azacyclooctylethylguanidine
AB00053479
C07036
55-65-2
guanethidine
DB01170
guanidine, (2-(hexahydro-1(2h)-azocinyl)ethyl)-
2-(1'-azacyclooctyl)ethylguanidine
heptamethylenimine, 1-(2-guanidinoethyl)-
2-(1-n,n-heptamethyleneimino)ethylguanidine
(2-(octahydro-1-azocinyl)ethyl)guanidine
n-(2-perhydroazocin-1-ylethyl)guanidine
(2-(hexahydro-1(2h)-azocinyl)ethyl)guanidine
IDI1_000539
KBIO2_001317
KBIO2_003885
KBIO3_001312
KBIOSS_001317
KBIOGR_000976
KBIO2_006453
SPBIO_002533
NINDS_000539
PRESTWICK1_000317
PRESTWICK0_000317
SPECTRUM2_001103
SPBIO_001206
SPECTRUM4_000568
SPECTRUM3_000446
NCGC00016272-03
NCGC00016272-02
CHEMBL765
L000732
D08030
guanethidine (inn)
STK895063
2-[2-(azocan-1-yl)ethyl]guanidine
AKOS005614041
NCGC00247765-01
zti6c33q2q ,
unii-zti6c33q2q
guanethidine [inn]
guanethidine [hsdb]
guanethidine [who-dd]
guanethidine [vandf]
guanethidine [mi]
su 5864
gtpl7194
CCG-213488
SCHEMBL34753
3h-guanethidine
azocine, 1-[[2-(aminoiminomethyl)amino]ethyl]octahydro-
n-[2-(1-azocanyl)ethyl]guanidine #
iporal (salt/mix)
[2-(hexahydro-1(2h)-azocinyl)ethyl]guanidine
octatenzine
[2-(octahydro-1-azocinyl)ethyl]guanidine
guanidine, [2-(hexahydro-1(2h)-azocinyl)ethyl]-
su 5864 (salt/mix)
isobarin (salt/mix)
AB00053479_05
AB00053479_04
DTXSID5023116 ,
SBI-0051399.P003
2-(2-(azocan-1-yl)ethyl)guanidine
Q420673
Z1198152903
n-[2-(azocan-1-yl)ethyl]guanidine
EN300-123310
n''-[2-(azocan-1-yl)ethyl]guanidine
STR07524
1-(2-(azocan-1-yl)ethyl)guanidine
CS-0013044
HY-B1251
s01ex01
dtxcid203116
c02cc02

Research Excerpts

Overview

Guanethidine is a sympatholytic antihypertensive drug used for the treatment of severe or resistant hypertension.

ExcerptReferenceRelevance
"Guanethidine is a sympatholytic antihypertensive drug used for the treatment of severe or resistant hypertension. "( Effects of captopril on the development of tolerance to guanethidine.
Haas, GJ; Rankin, GO, 1984
)
1.96

Effects

Guanethidine is an alternative method of catecholamine depletion. Like guanethidine, it has been reported to produce sympathetic neuronal destruction in rats.

ExcerptReferenceRelevance
"Guanethidine, which has been used in studies of the peripheral autonomic nervous system, provides an alternative method of catecholamine depletion."( Comparison of the effects of intracranial injections of 6-OHDA and guanethidine on consummatory behavior and monoamine depletion.
Armstrong, S; Burnstock, G; Evans, B; Singer, G, 1975
)
1.21
"Like guanethidine, it has been reported to produce sympathetic neuronal destruction in rats."( Species and structural specificity of the lipopigment accumulation and neuronal destruction induced by N-(2-guanidinoethyl)-4-methyl-1,2,5,6-tetrahydropyridine (guanacline).
Johnson, EM; Manning, PT; Palmatier, MA; Rydel, RE, 1986
)
0.73

Actions

ExcerptReferenceRelevance
"Guanethidine, at a lower concentration (0.1 microM) did not modify the first (1st) phase vasoconstriction at low frequencies (1-2 Hz), but markedly inhibited the second (2nd) responses."( Dissociation of inhibitory effects of guanethidine on adrenergic and on purinergic transmission in isolated canine splenic artery.
Chiba, S; Yang, XP, 1999
)
1.3

Treatment

Guanethidine treatment or adrenal medullectomy significantly inhibited the elevation in blood pressure induced by Clostridium perfringens beta toxin. The combination of the two drastically reduced the pressure rise, to less than 19% of that in control rats.

ExcerptReferenceRelevance
"Guanethidine treatment decreased mainly the oxidative phosphorylation capacity of subsarcolemmal mitochondria in heart, irrespective of the substrate used."( Mitochondrial oxidative energy metabolism in guanethidine-induced sympathectomized ducklings.
Fechtali, T; Filali-Zegzouti, Y; Rouanet, JL; Roussel, D, 2014
)
1.38
"Guanethidine pretreatment did not block the ability of centrally administered leptin to decrease blood glucose concentrations in diabetic rats."( Guanethidine treatment does not block the ability of central leptin administration to decrease blood glucose concentrations in streptozotocin-induced diabetic rats.
Huggins, KW; Judd, RL; Wang, J; Wernette, CM; White, BD, 2008
)
2.51
"Both guanethidine treatment and phentolamine coadministration attenuated the constrictor response to nociceptin."( Involvement of sympathetic efferents but not capsaicin-sensitive afferents in nociceptin-mediated dual control of rat synovial blood flow.
McDougall, JJ, 2003
)
0.77
"Guanethidine treatment attenuated the increase in basal corticosterone in hypoxic pups but did not attenuate ACTH-stimulated corticosterone production."( Basal and adrenocorticotropin-stimulated corticosterone in the neonatal rat exposed to hypoxia from birth: modulation by chemical sympathectomy.
Engeland, WC; Lee, JJ; Oaks, MK; Raff, H; Widmaier, EP, 2004
)
1.04
"Guanethidine treatment caused a decrease in norepinephrine in skeletal muscle."( Protein metabolism in guanethidine-treated rats.
Bielavská, M; Holecek, M; Sprongl, L, 2004
)
1.36
"Guanethidine pretreatment attenuated myenteric but not DVC Fos-LI induced by CCK-8."( Chemical sympathectomy attenuates myenteric but not dorsal vagal complex Fos-like immunoreactivity induced by cholecystokinin-8 in the rat.
Billups, LH; Chan, WC; Esdaile, AR; Gulley, S; Henley, SC; Moran, TH; Raboin, SJ; Sayegh, AI; Sharma, SK; Sullivan, CN, 2005
)
1.05
"Guanethidine treatment attenuated the hypoxia-induced increase in cholesterol ester-bound arachidonic and adrenic acids."( Adrenal lipid profiles of chemically sympathectomized normoxic and hypoxic neonatal rats.
Bruder, ED; Henderson, LM; Raff, H, 2006
)
1.06
"The guanethidine pretreatment did not influence thermal hyperalgesia induced by a mild burn, but inhibited pain evoked by electrical stimulation of the skin (0.2 mA direct current for 4 min)."( Depletion of noradrenaline inhibits electrically-evoked pain in the skin of the human forearm.
Drummond, PD, 2008
)
0.83
"Guanethidine pretreatment eliminated the delay in gastric emptying at 8 h."( Effect of chronic stress on gastric emptying and plasma ghrelin levels in rats.
Arakawa, T; Fujiwara, Y; Higuchi, K; Ochi, M; Oshitani, N; Shiba, M; Tanaka, F; Tanigawa, T; Tominaga, K; Watanabe, T, 2008
)
1.07
"Guanethidine treatment or adrenal medullectomy significantly inhibited the elevation in blood pressure induced by Clostridium perfringens beta toxin, and the combination of the two drastically reduced the pressure rise, to less than 19% of that in control rats. "( Effect of Clostridium perfringens beta toxin on blood pressure of rats.
Dezaki, K; Endo, K; Fujii, Y; Sakurai, J, 1984
)
1.71
"Guanethidine treatment produced a massive sympathectomy, as synaptic vesicle development was totally arrested; the functional consequence of this treatment was confirmed by the attenuation of chronotropic responses to tyramine, a drug which acts by displacement of norepinephrine from the noradrenergic terminal."( Maturation of sympathetic neurotransmission in the rat heart. IV. Effects guanethidine-induced sympathectomy on neonatal development of synaptic vesicles, synaptic terminal function and heart growth.
Bareis, DL; Lau, C; Morgan, RE; Slotkin, TA, 1981
)
1.21
"Guanethidine pretreatment of nucleus tractus solitarius also abolished the clonidine response."( Involvement of alpha2-adrenoceptors of nucleus tractus solitarius in baroreflex mediated bradycardia.
Bhargava, KP; Gurtu, S; Sinha, JN, 1982
)
0.99
"Guanethidine treatment (15 mg/kg) decreased mean PRA by 41, 50, 70, and 73% at rest and during the three levels of exercise, respectively."( Mechanism of renin release in exercising dog.
Grassl, SM; Lakas, CS; Scanes, CG; Tucker, MS; Zambraski, EJ, 1984
)
0.99
"Guanethidine-treated rats did not develop hypertension in response to isolation whereas control rats did."( The influence of neonatal treatment with guanethidine on the development of isolation-induced hypertension in adult rats.
Bennett, T; Gardiner, SM, 1983
)
1.25
"Guanethidine pretreatment did not affect the blood pressure response to i.c.v."( Contribution of the sympathetic nervous system to the centrally-induced pressor action of angiotensin II in rats.
Boucher, R; Buu, T; Genest, J; Kuchel, O; Mann, JF; Rascher, W; Schömig, A,
)
0.85
"Guanethidine treatment did not affect body and adrenal weight or adrenal choline acetyltransferase activity, but it increased tyrosine hydroxylase activity at both ages."( Chemical sympathectomy and maternal separation affect neonatal stress responses and adrenal sensitivity to ACTH.
Walker, CD, 1995
)
1.01
"Guanethidine treatment was ineffective on hyperalgesia exhibited in arthritic rats but was able to reduce reliably and even suppress the abnormal reactions to cold stimulus in neuropathic animals."( Are mechanical and cold allodynia in mononeuropathic and arthritic rats relieved by systemic treatment with calcitonin or guanethidine?
Ardid, D; Attal, N; Guilbaud, G; Perrot, S, 1993
)
1.21
"Guanethidine treatment did not affect the arterial pressure or heart rate responses to aortic coarctation of intact rats but blunted the hypertensive response of SAD rats to the same values exhibited by intact rats."( Influence of sympathetic blockade on the acute hypertensive response to aortic constriction.
Ballejo, G; Castania, JA; Fazan Júnior, R; Salgado, HC; Salgado, MC, 1997
)
1.02
"In guanethidine pretreated hearts, ICI 118.551 failed to induce premature beats."( Effects of ICI 118.551, a selective beta-2 adrenergic blocking agent on the guinea pig cardiac excitability and ventricular fibrillation threshold.
Cuparencu, B; Cuprian, A; Gozariu, M; Tomus, C, 2000
)
0.82
"The guanethidine-treatment itself caused the following changes."( Prevention of exercise-induced cardiac hypertrophy in rats by chemical sympathectomy (guanethidine treatment).
Ostman-Smith, I, 1976
)
0.96
"Guanethidine treatment of rate (30 mg kg(-1), i.p. "( An assessment of the cardiovascular sympathectomy induced by guanethidine.
Blythe, TH; Hall, RC; Hughes, IE, 1976
)
1.94
"Guanethidine treatment left the uptake unaffected, except for the spleen."( The effect of surgical sympathectomy and of neonatal treatment with 6-hydroxydopamine and guanethidine on particle-bound noradrenaline and 35S-sulphomucopolysaccharides.
Blaschke, E; Uvnäs, B, 1979
)
1.2
"2 In guanethidine-treated dogs, tripelennamine administered in the same dose following burimamide produced a blockade of the response to histamine comparable to that in the bretylium experiments, but decreased only the sustained vasodilator response to stimulation at 1 Hz."( Influence of histamine H1- and H2-receptor blockers on sympathetic vasodilator and vasoconstrictor responses in canine paw.
Kraft, E; Zimmerman, BG, 1975
)
0.71
"The guanethidine treatment resulted in an 86% absolute reduction in cell number in the superior cervical ganglia of 15 day old rats."( Alteration of neonatal rat parotid gland acinar cell proliferation by guandethidine-induced sympathectomy.
Klein, RM, 1979
)
0.74
"Guanethidine treatment for 2 days failed to produce any significant alterations in sympathetic neuronal activity to the myocardium, resting neurogenic tone in the perfused hind limb vasculature and lumbar sympathetic neuronal transmission."( Time-course effects of oral guanethidine administration on cardiovascular and autonomic effects on dogs.
Buckley, JP; Cavero, I; Jandhyala, BS, 1976
)
1.27
"Guanethidine treatment produced a significant depression of basal cutaneous blood flow whereas alpha-adrenoceptor blockade did not."( Neurogenic cutaneous vasodilation in the cat forepaw.
Kawarai, M; Koss, MC, 1992
)
1
"Guanethidine treatment of capsaicin-injected rats reversed the loss of calcitonin gene-related peptide-immunoreactive nerves, but not that of substance P-immunoreactive neurons."( Plasticity in expression of calcitonin gene-related peptide and substance P immunoreactivity in ganglia and fibres following guanethidine and/or capsaicin denervation.
Burnstock, G; Cavanagh, JF; Kirkpatrick, KA; Mione, MC, 1992
)
1.21
"In guanethidine-treated rats, there was a marked increase of substance P levels in the SCG, where substance P was localized in fibers, but not cell bodies."( Guanethidine sympathectomy increases substance P concentration in the superior sympathetic ganglion of adult rats.
Benarroch, EE; Low, PA; Nelson, DK; Schmelzer, JD; Zollman, PJ, 1992
)
2.24
"Guanethidine pretreatment did not influence the inhibitory action of [D-Met2,Pro5] enkephalinamide."( An opioid peptide inhibits capsaicin-sensitive vasodilatation in the pig's skin.
Barthó, L; Ernst, R; Faulstroh, K; Pethö, G; Pierau, FK; Sann, H, 1992
)
1
"Guanethidine pretreatment blocked the effect of nerve stimulation on mucociliary activity, including the observed decrease after combined blockade, indicating the effect to be mediated via sympathetic nerve fibres."( Sympathetic nerve stimulation influences mucociliary activity in the rabbit maxillary sinus.
Cervin, A; Lindberg, S; Mercke, U, 1991
)
1
"Guanethidine pretreatment, vagotomy or forced ventilation did not modify the effect of i.c.v."( Intracerebroventricular administration of endothelins: effects on the supraspinal micturition reflex and blood pressure in the anaesthetized rat.
Giachetti, A; Giuliani, S; Lecci, A; Maggi, CA; Rovero, P; Santicioli, P, 1991
)
1
"In guanethidine-treated rats, cells were also decreased in number; in some segments the decrease was significantly greater than with 6-OHDA."( Effects of neonatal sympathectomy with 6-hydroxydopamine or guanethidine on survival of neurons in the intermediolateral cell column of rat spinal cord.
Fernandez, MC; Krukoff, TL; Vincent, DH, 1990
)
1.04
"Guanethidine treatment caused significant reductions in systolic arterial blood pressure and indices of left ventricular contractility and relaxation (p less than 0.05), but these effects were not different between infarct and control treatments (p = N.S.)."( Effect of chemical sympathectomy on cardiac hypertrophy and hemodynamics following myocardial infarction in the rat.
Fishbein, MC; Rubin, SA, 1990
)
1
"In guanethidine-treated animals we observed elevated NBF, reduced MR and dilated microvessels."( Guanethidine-induced adrenergic sympathectomy augments endoneurial perfusion and lowers endoneurial microvascular resistance.
Huang, ZX; Low, PA; Ward, KK; Zochodne, DW, 1990
)
2.24
"Guanethidine pretreatment (67 mumol kg-1) revealed a facilitatory effect of low doses of the two tachykinins (about 1 nmol kg-1) on gastrointestinal propulsion."( Stimulation and inhibition of gastrointestinal propulsion induced by substance P and substance K in the rat.
Holzer, P, 1985
)
0.99
"Guanethidine treatment decreased morphine analgesia exhibited by restrained rats but had no effect on morphine analgesia exhibited by unrestrained rats or on baseline pain sensitivity. "( Sympathetic control of tryptophan uptake and morphine analgesia in stressed rats.
Franklin, KB; Kelly, SJ, 1986
)
1.71
"In guanethidine-treated, capsaicin-desensitized segments of guinea-pig isolated ileum electrical stimulation of mesenteric nerves resulted in contractions reaching 10 to 30% of the maximal longitudinal spasm. "( Pharmacological evidence for the presence of cholecystokinin-containing neurones in the mesenteric nerves supplying the guinea-pig ileum.
Barthó, L, 1989
)
0.9
"Guanethidine treatment produced the largest differential in neuron loss and tyrosine hydroxylase activity between pre- and paravertebral ganglia."( Differential susceptibility of prevertebral and paravertebral sympathetic ganglia to experimental injury.
Cogswell, BE; McAtee, SJ; Parvin, CA; Plurad, DA; Roth, KA; Schmidt, RE, 1988
)
1
"Guanethidine treatment did not alter resting and maximum responses of plasma IR-ANP."( Responses of plasma atrial natriuretic polypeptide to isotonic volume expansion in conscious spontaneously hypertensive and chronically guanethidine-treated rats.
Bravo, EL; Imura, H; Kihara, M; Morii, N; Nakao, K; Sugawara, A; Yamori, Y, 1986
)
1.2
"The guanethidine-treated animals gained less weight, had ptosis, and had a lower mean arterial blood pressure in the supine and upright tilted positions."( Guanethidine adrenergic neuropathy: an animal model of selective autonomic neuropathy.
Low, PA; Ward, KK; Zochodne, DW, 1988
)
2.2
"In guanethidine-pretreated animals a series of atropine-resistant but hexamethonium-resistant rhythmic contractions could be demonstrated."( Propagated motor activity in the small intestine of urethane-anaesthetized rats: inhibitory action of sympathetic and capsaicin-sensitive nerves.
Giuliani, S; Maggi, CA; Meli, A; Santicioli, P, 1988
)
0.79
"In guanethidine-treated rats, the adrenaline content of the peripheral organs was extremely low as compared to that in the saline-treated animals, and the swimming-induced increase in adrenaline level in the organs was greatly suppressed."( Effects of adrenalectomy and chronic guanethidine treatment on tissue adrenaline concentrations in swimming-exposed rats.
Sudo, A, 1987
)
1.06
"Guanethidine treatment decreased the amount of mAChR from 102 to 87 fmoles/mg protein in the heart and from 444 to 388 fmoles/mg protein in the small intestine, but increased it from 223 to 282 fmoles/mg protein in the vas deferens, without changes in its characteristics."( Changes in density of muscarinic cholinergic receptor by adrenergic denervation with guanethidine.
Higuchi, H; Murata, M; Uchida, S; Yoshida, H, 1985
)
1.21
"Guanethidine treatment beginning at birth induced complete sympathectomy, as determined by abolition of contractile responses to electrical stimulation of preganglionic axons and tyramine."( Role of the sympathetic nervous system in functional maturation of Müller's smooth muscle in the rat.
Smith, PG, 1985
)
0.99
"Guanethidine treatment did not alter lordotic responsiveness to manual stimulation but did reduce the frequency of copulatory acts engaged in by the females in the complex environment."( Sociosexual behaviors of female rats during and after chronic treatment with the sympatholytic agent guanethidine.
Emery, DE, 1985
)
1.21
"Guanethidine treatment did not attenuate amphetamine anorexia as evidenced by comparable dose-dependent reductions in food intake to d-amphetamine sulfate (0.25, 0.50, 1.0, and 2.0 mg/kg) in sympathectomized and control rats."( Effects of guanethidine sympathectomy on feeding, drinking, weight gain and amphetamine anorexia in the rat.
Clark, DE; Freeman, PH; Wellman, PJ, 1985
)
1.38
"Guanethidine pretreatment (30 mg/kg i.v."( Centrally mediated cardiovascular effects of nicergoline in the dog compared to those of clonidine.
Faucon, G; Lakhal, M; Lièvre, M; Morin, MH, 1985
)
0.99
"Pretreatment with guanethidine (>or=3.5 h) also failed reduce PTD while neurons unresponsive to alpha(2) adrenoceptor agonists routinely exhibited PTD, implying the presence of other inhibitory neurotransmitters sharing a common presynaptic mechanism with alpha(2) agonists."( Alpha-adrenergic modulation of synaptic transmission in rabbit pancreatic ganglia.
Love, JA; Yi, E, 2005
)
0.65
"Pretreatment with guanethidine, a postganglionic sympathetic nerve blocker and antihypertensive drug (30 mg kg(-1), s.c., 24 h prior to experiments), reduced the magnitude of the decrease in SABP while the intensity- and frequency-dependent increases of the lip blood flow occurred by the lingual nerve stimulation only on the side ipsilateral to stimulation."( Occurrence of parasympathetic vasodilator fibers in the lower lip of the guinea-pig.
Ishii, H; Izumi, H; Niioka, T; Watanabe, H; Yamamuro, M, 2008
)
0.67
"Pretreatment with guanethidine sulphate (5 mg/kg i.v.) reduced but did not abolish the tachycardia elicited by i.c.v."( Leakage of catecholamines from rabbit cerebrospinal fluid following intracerebroventricular injection.
Maccarrone, C; Malta, E; Raper, C,
)
0.45
"Pretreatment by guanethidine (GUA) antagonized HGS inhibition of pelvic nerve evoked bladder contractions, but had no effect on the HGS-induced transient contractions."( Evidence against purinergic nerve fibres in the hypogastric nerves of the cat.
Theobald, RJ, 1983
)
0.6
"4 Pretreatment with guanethidine (15 mg/kg i.v."( Effects of lysine-vasopressin and oxytocin on central cardiovascular control.
Montastruc, JL; Montastruc, P; Tran, LD, 1982
)
0.58
"Pretreatment with guanethidine effectively suppressed the increase in the rate constant of glucose uptake, measured by the 2-deoxy-D-[3H]glucose method, in skeletal muscles upon VMH stimulation."( Regulatory mechanism of the ventromedial hypothalamus in enhancing glucose uptake in skeletal muscles.
Minokoshi, Y; Okano, Y; Shimazu, T, 1994
)
0.61
"Pretreatment with guanethidine decreases myocardial catecholamine level and completely reverses cardiac injury induced by stress."( [The role of peripheral and central mu-opiate receptors in the modulation of adrenergic cardiac lesions during stress].
Lishmanov, IuB; Maslov, LN; Naryzhnaia, NV; Revinskaia, IuG, 1998
)
0.62
"Treatment with guanethidine and prazosin reversed these sympathetic hyperactive responses in insulin-resistant rats."( Sympathetic hyperactivity in Wistar rats with insulin-resistance.
Chang, CJ; Cheng, JT; Chi, TC; Liu, IM; Lu, FH; Wu, JS, 1998
)
0.64
"Pretreatment with guanethidine significantly suppressed the increased glucose uptake by the tissues in response to leptin injected into the VMH, whereas bilateral adrenal demedullation had no significant effect."( Role of the sympathetic nervous system and insulin in enhancing glucose uptake in peripheral tissues after intrahypothalamic injection of leptin in rats.
Hamai, M; Haque, MS; Horiuchi, M; Iwai, M; Minokoshi, Y; Shimazu, T, 1999
)
0.63
"Pretreatment with guanethidine (15 mg/kg) decreased and even prevented this effect of morphine."( Studies on the mechanism of the action of morphine on the peristalsis of guinea pig ileum in situ.
Aldunate, J; Mardones, J; Yojay, L, 1975
)
0.58
"Pretreatment with guanethidine and reserpine almost completely abolished the pressor response to PAM."( Pressor action of pyridine-2-aldoxime in malathion poisoning.
Chang, P; Ganendran, A,
)
0.45
"Pretreatment with guanethidine produced a small reduction in the inhibitory action of nicotine."( Effects of nicotine on rebound excitation of guinea-pig small intestine.
Jackson, MH; Rose, BA; Wood, JD, 1976
)
0.58
"Pretreatment with guanethidine or propranolol increased the airway constriction induced by [beta Ala8]NKA-(4-10)."( Effect of ruthenium red on the bronchoconstriction induced by capsaicin and by selective tachykinin receptor agonists in anaesthetized guinea-pig.
Ballati, L; Evangelista, S; Maggi, CA, 1992
)
0.61
"Treatment with guanethidine diminished heat and cold sensitization considerably, but had less effect on mechanical sensitization and, if administered before surgery, rather increased the severity of self-mutilating behaviour."( Effects of guanethidine on sensitization to natural stimuli and self-mutilating behaviour in rats with a peripheral neuropathy.
Attal, N; Guilbaud, G; Neil, A, 1991
)
1.01
"Pretreatment with guanethidine (5 X 10(-6) M) did not block the action of tyramine on NA and DOPEG basal outflows."( Effects of tyramine on noradrenaline outflow and electrical responses induced by field stimulation in the perfused rabbit ear artery.
Miyahara, H; Suzuki, H, 1985
)
0.59
"Pretreatment with guanethidine depleted NA in the heart but did not influence plasma levels or tissue content of NPY-LI per se."( Reserpine-induced depletion of neuropeptide Y from cardiovascular nerves and adrenal gland due to enhanced release.
Al-Saffar, A; Lundberg, JM; Saria, A; Theodorsson-Norheim, E, 1986
)
0.59
"Pre-treatment with guanethidine effectively abolished the lipogenic response to nerve stimulation but potentiated the response to noradrenaline infusion."( Sympathetic activation of lipid synthesis in brown adipose tissue in the rat.
Minokoshi, Y; Saito, M; Shimazu, T, 1988
)
0.59
"Pretreatment with guanethidine did not affect basal output of HCO3- but markedly reduced the bleeding-induced response."( Bleeding-induced decrease in duodenal HCO3- secretion in the rat is mediated via alpha 2-adrenoceptors.
Fändriks, L; Jönson, C, 1987
)
0.6

Toxicity

ExcerptReferenceRelevance
" Therefore, large doses of guanethidine as required for the guanethidine loading regimen would seem to be safe even in patients in whom inotropic effects of released catecholamines would be contraindicated."( Safety of single large oral doses of guanethidine.
Nies, AS; Walter, IE, 1977
)
0.83
" Other reported effects are toxic confusional states and psychotic reactions."( Psychiatric side effects of antihypertensive drugs other than reserpine.
Fleminger, R; Paykel, ES; Watson, JP, 1982
)
0.26
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic variables have been determined that allow: (1) derivation of the loading dose necessary to achieve rapid control of blood pressure with propranolol hydrochloride, guanethidine, minoxidil and clonidine hydrochloride; (2) reduced frequency of dosing with methyldopa, hydralazine hydrochloride, prazosin hydrochloride, propranolol and clonidine; and (3) alteration of propranolol and hydralazine dosage based on physiologic factors (e."( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs.
Schumacher, GE, 1979
)
0.45

Compound-Compound Interactions

ExcerptReferenceRelevance
" These drugs may interact pharmacokinetically or pharmacodynamically, and most drug interactions are therapeutically useful."( [Drug interactions in cardiovascular therapy].
Koch-Weser, J, 1976
)
0.26
" Further studies are required of other well-recognized groups of patients on drugs which are known to interact to assess the relevance and clinical importance of the formidable lists of interactions which are now available to doctors who prescribe drugs."( Drug interactions in patients on long-term oral anticoagulant and antihypertensive adrenergic neuron-blocking drugs.
Petrie, JC; Starr, KJ, 1972
)
0.25

Bioavailability

ExcerptReferenceRelevance
" N-Nitro-L-arginine (NOLA) (5 x 10(-5) to 10(-4) M), an inhibitor of NO synthase, and haemoglobin (10(-5) M), which reduces bioavailability of NO, both reduced the amplitude of nerve-mediated relaxations to less than 50%, without affecting the ability of the muscle to relax."( Evidence that nitric oxide participates in non-adrenergic inhibitory transmission to intestinal muscle in the guinea-pig.
Furness, JB; Murphy, R; Shuttleworth, CW, 1991
)
0.28
" Both BW 467C60 and BW 392C60 were well absorbed from the alimentary tract."( Adrenergic neurone blockade and other acute effects caused by N-benzyl-N'N"-dimethylguanidine and its ortho-chloro derivative.
BOURA, AL; GREEN, AF, 1963
)
0.24

Dosage Studied

The dose-response relation of the coronary diameter to histamine was not influenced by pretreatment with the nerve transmitter blockers guanethidine (3 X 10(-6) M) and tetrodotoxin. Preliminary results from immunoassay indicate potential use for assessing dosage regimens and studying pharmacokinetics.

ExcerptRelevanceReference
"Pharmacokinetic methods that have been used to improve antihypertensive drug therapy, including antihypertensive dosage regimens, are reviewed."( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs.
Schumacher, GE, 1979
)
0.26
" These results lead us to believe that most patients who respond to this treatment could be put on a reduced dosage regimen, which should result in a decreased incidence and severity of side effects."( Control of glaucoma by reduced dosage guanethidine-adrenaline formulation.
Davies, DJ; Jones, DE; Norton, DA, 1979
)
0.53
" Preliminary results from immunoassay of plasma samples from patients receiving guanethidine indicate potential use for assessing dosage regimens and studying pharmacokinetics."( Development of radioimmunoassay for guanethidine.
Loeffler, LJ; Pittman, AW, 1979
)
0.76
"The changes in mean arterial blood pressure, heart rate and the respective noradrenaline dose-response curves after guanethidine sulphate (0."( Guanethidine-induced acute hypersensitivity to noradrenaline in anaesthetized rats.
Nielsen, GD, 1977
)
1.91
"Where practicable, all subjects found with onset-phase-four blood pressure of 90 mmHg or more after referral were allocated, on a random basis, to alternative antihypertensive regimes at a dosage related to response."( An approach to realistic evaluation of antihypertensive regimes.
Akinkugbe, OO; Basile, U; Carlisle, R; Solagbade, ME, 1977
)
0.26
"In long-term experiments in rats the effects of guanethidine sulphate on peripheral adrenergic neurons in the heart, the vas deferens, the superior cervical ganglion and the ganglion innervating the vas deferens were studied in relation to the dosage and route of administration of the drug by biochemical, histofluorimetric and electron-microscopic methods."( A study of long-term effects of guanethidine on peripheral noradrenergic neurones of the rat.
Bittiger, H; Hess, R; Krinke, G; Maĭtre, L; Schnider, K, 1977
)
0.8
" The excitability of the superior cervical ganglion of the rat was not diminished after a three-day treatment with L-Dopa, Benseraside (Ro 4-4602/1) and Iproniazid, at a dosage below the toxic level (table I)."( [Endogenous catecholamines and excitability of the superior cervical ganglion of the rat (author's transl)].
Burlet, DB, 1976
)
0.26
" The following considerations regarding tricyclic antidepressant therapy are discussed: dosage schedules, onset of action, anticholinergic effects, cardiac toxicity and drug interactions."( Rational use of psychotropic drugs. IV. Antidepressants.
Greenblatt, DJ; Shader, RI, 1975
)
0.25
" Six rabbits were used and the efficiencies of 5 different dosage protocols was estimated both as intensity and duration of activity."( Effect of adrenaline and guanethidine in reducing intraocular pressure in rabbits' eyes.
Davies, DJ; Harvey, J; Jones, DE; Norton, DA, 1975
)
0.56
" This specific type of pharmaceutical treatment appeared to be especially suitable for this disease owing to a combination of therapeutic efficacy and a substantial reduction in the total dosage for each patient."( Regional intravenous ketanserin and guanethidine therapy in Raynaud's phenomenon.
Caputi, CA; De Carolis, G; Tomasetti, C, 1991
)
0.56
" The dose-response relation of the coronary diameter to histamine was not influenced by pretreatment with the nerve transmitter blockers guanethidine (3 X 10(-6) M), atropine (10(-6) M), and tetrodotoxin (3 X 10(-7) M)."( Pathogenesis of coronary artery spasm in miniature swine with regional intimal thickening after balloon denudation.
Egashira, K; Kawasaki, T; Kobayashi, T; Nakamura, M; Tomoike, H; Yamamoto, Y, 1987
)
0.48
" The procedure is shown applicable to the analysis of a combination dosage form and is also useful for either drug in a single component dosage form."( Liquid chromatographic determination of guanethidine salts and hydrochlorothiazide using electrochemical detection and ion-pair techniques.
Clark, SS; Stewart, JT, 1986
)
0.54
"Sensitivity to propranolol varies widely, and dosage should be increased gradually."( Treatment of hypertension with propranolol.
Gillam, PM; Prichard, BN, 1969
)
0.25
"A low dosage combination of terbutaline plus guanethidine was applied topically to the eyes of rabbits with experimentally induced ocular hypertension, markedly lowering intraocular pressure."( Intraocular-pressure-lowering effect of low-dosage combination of guanethidine and terbutaline in rabbit.
Bellucci, R; Bonomi, L; Gamba, GC; Massa, F; Perfetti, S, 1983
)
0.76
" The recommended regime for GA therapy in patients with an IOP of less than 32 mm Hg is application of GA twice daily for 1 month followed by a decrease in the dosage to once a day."( Maintenance therapy of glaucoma patients with guanethidine (3%) and adrenaline (0.5%) once daily.
Dake, CL; Hoyng, PF, 1980
)
0.52
" On the other hand, 2-methyl-5-HT produced only a vasoconstriction, and the dose-response curve was shifted to the right in parallel by treatment with either ketanserin or bunazosin, although methysergide and granisetron had no antagonistic effect."( 2-Methyl-5-HT-induced vasoconstrictions mediated via alpha 1-adrenoceptors in rabbit common carotid arteries.
Chiba, S; Fujiwara, T, 1994
)
0.29
" Naloxone shifted to the right the dose-response curves for each opioid peptide significantly enhancing the ED50 values."( Modulation of non-adrenergic non-cholinergic inhibitory transmission in rat duodenum: role of opiates and 5-hydroxytryptamine.
Adamo, EB; Di Giovanni, G; Marini, R; Mulè, F; Postorino, A; Serio, R, 1993
)
0.29
" At the maximum dosage after 24 h of permanent contact with the cells (extreme, non-physiological conditions), cytolysis did not exceed 30%."( Action of new organometallic complexes against Leishmania donovani.
Craciunescu, D; Lazuen, J; Mesa-Valle, CM; Moraleda, V; Osuna, A, 1997
)
0.3
" The good result, considering the low dosage of sBMP, can be explained by the strong osteoinductivity and low immunogenicity of native allogeneic sBMP."( Low dosage of native allogeneic bone morphogenetic protein in repair of sheep calvarial defects.
Gao, TJ; Lindholm, TC; Lindholm, TS; Viljanen, VV, 1997
)
0.3
" In a subsequent experiment the lowest effective dosage (6."( Rat epididymal sperm quantity, quality, and transit time after guanethidine-induced sympathectomy.
Ferrell, J; Goldman, JM; Kempinas, WD; Klinefelter, GR; Roberts, NL; Strader, L; Suarez, JD, 1998
)
0.54
"These results indicate that the dosage of the sympathoinhibitory drug might be quite important for the treatment of CHF."( Long-term treatment with low-dose, but not high-dose, guanethidine improves ventricular function and survival of rats with heart failure after myocardial infarction.
Asanoi, H; Fujii, N; Igawa, A; Inoue, H; Kato, B; Nozawa, T, 2003
)
0.57
" Bretylium and guanethidine depress the slopes of the dose-response curves for the pressor and nictitating membrane contracting effects of tyramine."( Comparison of bretylium and guanethidine: tolerance, and effects on adrenergic nerve function and responses to sympathomimetic amines.
BOURA, AL; GREEN, AF, 1962
)
0.89
" Ghrelin was more potent than GHRP-6 and the dose-response relationship for ghrelin but not for GHRP-6 was bell-shaped."( Comparison of the gastroprokinetic effects of ghrelin, GHRP-6 and motilin in rats in vivo and in vitro.
De Man, J; De Winter, B; Depoortere, I; Peeters, T; Pelckmans, P; Thijs, T, 2005
)
0.33
"Addition of CGRP stimulated rhythmic contractility but only in the presence of calcium, with a dose-response to the level of calcium ions."( The role of sympathetic innervation in the developing rat gubernaculum.
Clarke, MC; Hutson, JM; Sasaki, Y, 2007
)
0.34
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" The final study determined the dose-response relationship for paclitaxel."( Chemical renal denervation in the rat.
Consigny, PM; Davalian, D; Donn, R; Hu, J; Rieser, M; Stolarik, D, 2014
)
0.4
" In contrast, hyperosmolar saline, paclitaxel and guanethidine do not seem to be appropriate for renal denervation in a pig model at the dosage used."( Renal denervation by CT-guided periarterial injection of hyperosmolar saline, vincristine, paclitaxel and guanethidine in a pig model.
Bernhardt, U; Donners, R; Freyhardt, P; Günther, RW; Hamm, B; Riemert, A; Rinnenthal, JL; Schnorr, J; Stolzenburg, N; Streitparth, F, 2017
)
0.92
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
adrenergic antagonistAn agent that binds to but does not activate adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists.
sympatholytic agentAny compound which inhibits the postganglionic functioning of the sympathetic nervous system (SNS).
[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 (2)

ClassDescription
guanidinesAny organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
azocanes
[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 (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
USP1 protein, partialHomo sapiens (human)Potency39.81070.031637.5844354.8130AID504865
lamin isoform A-delta10Homo sapiens (human)Potency1.41250.891312.067628.1838AID1487
[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)
Nitric oxide synthase, brain Rattus norvegicus (Norway rat)Activity0.10000.10000.10000.1000AID146288
Nitric oxide synthase, inducibleHomo sapiens (human)Activity0.10000.10000.10000.1000AID92306
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (53)

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)
response to hypoxiaNitric oxide synthase, inducibleHomo sapiens (human)
positive regulation of leukocyte mediated cytotoxicityNitric oxide synthase, inducibleHomo sapiens (human)
innate immune response in mucosaNitric oxide synthase, inducibleHomo sapiens (human)
arginine catabolic processNitric oxide synthase, inducibleHomo sapiens (human)
superoxide metabolic processNitric oxide synthase, inducibleHomo sapiens (human)
nitric oxide biosynthetic processNitric oxide synthase, inducibleHomo sapiens (human)
circadian rhythmNitric oxide synthase, inducibleHomo sapiens (human)
response to bacteriumNitric oxide synthase, inducibleHomo sapiens (human)
negative regulation of gene expressionNitric oxide synthase, inducibleHomo sapiens (human)
peptidyl-cysteine S-nitrosylationNitric oxide synthase, inducibleHomo sapiens (human)
prostaglandin secretionNitric oxide synthase, inducibleHomo sapiens (human)
positive regulation of interleukin-6 productionNitric oxide synthase, inducibleHomo sapiens (human)
positive regulation of interleukin-8 productionNitric oxide synthase, inducibleHomo sapiens (human)
regulation of cell population proliferationNitric oxide synthase, inducibleHomo sapiens (human)
negative regulation of protein catabolic processNitric oxide synthase, inducibleHomo sapiens (human)
defense response to bacteriumNitric oxide synthase, inducibleHomo sapiens (human)
regulation of cellular respirationNitric oxide synthase, inducibleHomo sapiens (human)
cell redox homeostasisNitric oxide synthase, inducibleHomo sapiens (human)
regulation of insulin secretionNitric oxide synthase, inducibleHomo sapiens (human)
defense response to Gram-negative bacteriumNitric oxide synthase, inducibleHomo sapiens (human)
positive regulation of killing of cells of another organismNitric oxide synthase, inducibleHomo sapiens (human)
cellular response to lipopolysaccharideNitric oxide synthase, inducibleHomo sapiens (human)
cellular response to type II interferonNitric oxide synthase, inducibleHomo sapiens (human)
cellular response to xenobiotic stimulusNitric oxide synthase, inducibleHomo sapiens (human)
regulation of cytokine production involved in inflammatory responseNitric oxide synthase, inducibleHomo sapiens (human)
negative regulation of blood pressureNitric oxide synthase, inducibleHomo sapiens (human)
response to hormoneNitric oxide synthase, inducibleHomo sapiens (human)
nitric oxide mediated signal transductionNitric oxide synthase, inducibleHomo sapiens (human)
response to lipopolysaccharideNitric oxide synthase, inducibleHomo sapiens (human)
inflammatory responseNitric oxide synthase, inducibleHomo sapiens (human)
positive regulation of guanylate cyclase activityNitric oxide synthase, inducibleHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

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)
nitric-oxide synthase activityNitric oxide synthase, inducibleHomo sapiens (human)
protein bindingNitric oxide synthase, inducibleHomo sapiens (human)
calmodulin bindingNitric oxide synthase, inducibleHomo sapiens (human)
FMN bindingNitric oxide synthase, inducibleHomo sapiens (human)
heme bindingNitric oxide synthase, inducibleHomo sapiens (human)
tetrahydrobiopterin bindingNitric oxide synthase, inducibleHomo sapiens (human)
arginine bindingNitric oxide synthase, inducibleHomo sapiens (human)
protein homodimerization activityNitric oxide synthase, inducibleHomo sapiens (human)
metal ion bindingNitric oxide synthase, inducibleHomo sapiens (human)
flavin adenine dinucleotide bindingNitric oxide synthase, inducibleHomo sapiens (human)
NADP bindingNitric oxide synthase, inducibleHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

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)
nucleusNitric oxide synthase, inducibleHomo sapiens (human)
nucleoplasmNitric oxide synthase, inducibleHomo sapiens (human)
cytoplasmNitric oxide synthase, inducibleHomo sapiens (human)
peroxisomeNitric oxide synthase, inducibleHomo sapiens (human)
peroxisomal matrixNitric oxide synthase, inducibleHomo sapiens (human)
cytosolNitric oxide synthase, inducibleHomo sapiens (human)
cortical cytoskeletonNitric oxide synthase, inducibleHomo sapiens (human)
perinuclear region of cytoplasmNitric oxide synthase, inducibleHomo sapiens (human)
plasma membraneNitric oxide synthase, inducibleHomo sapiens (human)
nucleusNitric oxide synthase, inducibleHomo sapiens (human)
cytosolNitric oxide synthase, inducibleHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (93)

Assay IDTitleYearJournalArticle
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID171308Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 25 mg/kg, p.o. after 24 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1133620Antihypertensive activity in pithed rat assessed as change in sympathetic outflow activation-induced systemic pressor response at 1 mg/kg, iv at 5 Hz frequency1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID171329Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. after 24 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID192802Maximum rate of rise of the left ventricular isovolumetric pressure administered at 25 uM/kg iv in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1133635Antihypertensive activity in pithed rat assessed as change in phenylephrine-induced systemic pressor response at 1 mg/kg, iv in presence of 2 mg/kg phenylephrine1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID193681Maximum rate of rise of the left ventricular isovolumetric pressure in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID230956Ratio of the concentration levels determined for the adrenal medulla to the liver after 72 hr; [Adrenal Medulla] / [liver]1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID172424Antihypertensive activity was measured for systolic pressure using spontaneous hypertensive rats (SHR) at 10 mg/kg after oral administration1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
Benzenesulfenamides as antihypertensive agents. Substituted piperidine and 1-arylpiperazine derivatives.
AID171655Change in diastolic blood pressure after iv administration of 25 uM/kg in anesthetized rats1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID171309Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 25 mg/kg, po after 4 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID171473Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. before predose1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1133634Antihypertensive activity in pithed rat assessed as change in phenylephrine-induced systemic pressor response at 1 mg/kg, iv in presence of 4 mg/kg phenylephrine1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1133627Antihypertensive activity in pithed rat assessed as change in sympathetic outflow activation-induced systemic pressor response at 1 mg/kg, iv at 10 Hz frequency1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID92306NO releasing ability of compound measured through formation of nitrite using iNOS (nitric oxide synthases)2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
N-hydroxyl derivatives of guanidine based drugs as enzymatic NO donors.
AID171469Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. after 4 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID171307Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 25 mg/kg, p.o. after 24 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID171468Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. after 24 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1133618Antihypertensive activity in pithed rat assessed as change in sympathetic outflow activation-induced systemic pressor response at 5 mg/kg, iv at 5 Hz frequency1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID61002The maximum dopamine release induced by perfusion with the test compound with basal striatal DA (%of basal x10E-3)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
In vivo intracerebral microdialysis studies in rats of MPP+ analogues and related charged species.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID170836Tested for the change in systolic blood pressure administered at 25 ug/kg intravenously in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID170668Tested for the change in diastolic blood pressure administered at 25 ug/kg intravenously in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID171470Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. after 4 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID193687Percent change in diastolic blood pressure (mmHg)in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID171328Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. after 24 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID15566Distribution in dog adrenal medulla 72 hours after administration.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID171813Change in systolic blood pressure after iv administration of 25 uM/kg in anesthetized rats1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID15565Distribution in dog adrenal medulla 30 min after administration.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID197297Changes in systolic Blood pressure following iv administration at (25 umol/kg) anesthetized rats2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N(1)-agmatine and synthetic analogues.
AID192754Maximum rate of rise of the left ventricular isovolumetric pressure was measured after iv administration of 25 uM/kg in anesthetized rats; ratio given for dP/dt1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID1133640Antihypertensive activity in pithed rat assessed as change in phenylephrine-induced systemic pressor response at 5 mg/kg, iv in presence of 4 mg/kg phenylephrine1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1133611Antihypertensive activity in pithed rat assessed as change in sympathetic outflow activation-induced systemic pressor response at 5 mg/kg, iv at 2.5 Hz frequency1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
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.
AID180651Change in heart rate after iv administration of 25 uM/kg in anesthetized rats1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Novel hypotensive agents from Verbesina caracasana. 6. Synthesis and pharmacology of caracasandiamide.
AID61001The maximal DA release induced by perfusion with 10 mM MPP+ (15 min) 1 day after perfusion with the test compound with basal striatal DA (%of basal x10E-3)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
In vivo intracerebral microdialysis studies in rats of MPP+ analogues and related charged species.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1133632Antihypertensive activity in pithed rat assessed as change in phenylephrine-induced systemic pressor response at 5 mg/kg, iv in presence of 2 mg/kg phenylephrine1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID1137255Antihypertensive activity in spontaneous hypertensive rat assessed as drop in systolic blood pressure at 10 mg/kg, po administered at 0 hrs on days 1, 2 and 3 measured at 2 hrs after drug dose on day 3 by indirect tail-cuff method1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Spiro[isobenzofuran-1(3H),4'-piperidines]. 3. Diuretic and antihypertensive properties of compounds containing a sulfur attached to nitrogen.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625278FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of no concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID193688Percent change in heart rate expressed in beats / min in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID197288Changes in diastolic Blood pressure following iv administration at (25 umol/kg) anesthetized rats2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N(1)-agmatine and synthetic analogues.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID171471Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. after 4 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID171474Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. before predose1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID186699Blood pressure change in rats after oral administration of 50 mg/kg dose after 24 hours1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Pyrimidinones. 3. N-substituted 6-phenylpyrimidinones and pyrimidinediones with diuretic/hypotensive and antiinflammatory activity.
AID171312Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 25 mg/kg, p.o. before predose1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID193699Percent change in systolic blood pressure (mmHg)in anesthetized rats by i.v. administration1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Further hypotensive metabolites from Verbesina caracasana.
AID171311Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 25 mg/kg, p.o. after 4 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID171472Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, po after 4 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID171330Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 50 mg/kg, p.o. after 24 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID146288NO releasing ability of compound measured through formation of nitrite using nNOS (nitric oxide synthases)2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
N-hydroxyl derivatives of guanidine based drugs as enzymatic NO donors.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID180831Tested for change in heart rate administered at 25 uM/kg iv in anesthetized rats1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide.
AID171486Antihypertensive activity was evaluated in spontaneously hypertensive rat model with base line systolic pressure of 174 mmHg by the indirect tail-cuff method at an oral screening dose of 50 mg/Kg1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
(+/-)-4-Aryl-4,5-dihydro-3H-1,3-benzodiazepines. 3. 2-Phenyl and 2-amino analogues as potential antihypertensive agents.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1133625Antihypertensive activity in pithed rat assessed as change in sympathetic outflow activation-induced systemic pressor response at 5 mg/kg, iv at 10 Hz frequency1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1133613Antihypertensive activity in pithed rat assessed as change in sympathetic outflow activation-induced systemic pressor response at 1 mg/kg, iv at 2.5 Hz frequency1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Derivatives of tetrahydro-1,4-benzodiazepines as potential antihypertensive agents.
AID186701Blood pressure change in rats after oral administration of 50 mg/kg dose after 4 hours1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Pyrimidinones. 3. N-substituted 6-phenylpyrimidinones and pyrimidinediones with diuretic/hypotensive and antiinflammatory activity.
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.
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 (3,565)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902954 (82.86)18.7374
1990's394 (11.05)18.2507
2000's153 (4.29)29.6817
2010's58 (1.63)24.3611
2020's6 (0.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 55.23

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index55.23 (24.57)
Research Supply Index8.27 (2.92)
Research Growth Index4.02 (4.65)
Search Engine Demand Index97.11 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (55.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials117 (3.08%)5.53%
Reviews165 (4.34%)6.00%
Case Studies72 (1.89%)4.05%
Observational0 (0.00%)0.25%
Other3,449 (90.69%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]