Compounds > pinacidil pyridine n-oxide
Page last updated: 2024-12-06

pinacidil pyridine n-oxide

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

Description

Pinacidil pyridine N-oxide is a potent and selective activator of the ATP-sensitive potassium (KATP) channel. It has been shown to have antihypertensive, anti-ischemic, and anti-diabetic effects in preclinical studies. The compound was synthesized by a team at the University of California, San Francisco, in the 1980s. It is studied for its potential therapeutic benefits in various diseases, including hypertension, diabetes, and stroke. The compound has shown promising results in clinical trials for the treatment of hypertension. Its selective activation of KATP channels makes it a potential therapeutic target for various diseases, including diabetes, stroke, and heart disease. The exact mechanism of action of pinacidil pyridine N-oxide is not fully understood, but it is believed to work by opening KATP channels in smooth muscle cells, leading to vasodilation and a decrease in blood pressure.'

pinacidil pyridine N-oxide: metabolite of pinacidil [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID64775
CHEMBL ID1053
MeSH IDM0130835

Synonyms (13)

Synonym
CHEMBL1053
einecs 280-367-3
n-cyano-n'-(pyridin-4-yl)-n''-(1,2,2-trimethylpropyl)guanidine n-oxide
guanidine, n-cyano-n-4-pyridinyl-n''-(1,2,2-trimethylpropyl)-, n-oxide
pinacidil pyridine n-oxide
(+-)-n''-cyano-n-(1-oxido-4-pyridyl)-n'-(1,2,2-trimethylpropyl)guanidine
1-cyano-2-(3,3-dimethylbutan-2-yl)-3-(1-hydroxypyridin-4-ylidene)guanidine
pinacidil n-oxide
83285-82-9
n-cyano-n'-4-pyridinyl-n-oxide-n''-(1,2,2-trimethylpropyl)guanidine
p 1368
n''-cyano-n-(3,3-dimethylbutan-2-yl)-n'-(1-hydroxypyridin-4(1h)-ylidene)guanidine
DTXSID601003259

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The peak concentration of pinacidil and N-oxide and the area under the concentration-time curve (AUC) were proportional to the dose of pinacidil, with an average pinacidil concentration of 268 micrograms/L (1."( Clinical pharmacokinetics of pinacidil, a potassium channel opener, in hypertension.
DeSante, KA; Goldberg, MR; Rockhold, FW; Thompson, WL, 1989)		0.28

Bioavailability

ExcerptReferenceRelevance
" Mean bioavailability of pinacidil was 57."( Serum concentrations and urinary excretion of pinacidil and its major metabolite, pinacidil pyridine-N-oxide following i.v. and oral administration in healthy volunteers.
Ainsworth, S; Farrow, PR; McBurney, A; Ward, JW, 1985)		0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID193411Maximum percent fall in Systolic blood pressure (SBP) was measured in anesthetized normotensive rat for 30 mins after intravenous (iv) injection at 0.3 mg/kg dose1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
Novel potassium channel openers: synthesis and pharmacological evaluation of new N-(substituted-3-pyridyl)-N'-alkylthioureas and related compounds.
AID197345Negative logarithm of the concentration causing a 100% inhibition of spontaneous mechanical activity in rat portal vein is determined in vitro1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
Novel potassium channel openers: synthesis and pharmacological evaluation of new N-(substituted-3-pyridyl)-N'-alkylthioureas and related compounds.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (80.00)18.7374
1990's2 (20.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.82

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.82 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (10.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
trimethylamine
[no description available]		1.9710methylamines;
tertiary amine		Escherichia coli metabolite;
human xenobiotic metabolite
debrisoquin
Debrisoquin: An adrenergic neuron-blocking drug similar in effects to GUANETHIDINE. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism.		2.3720carboxamidine;
isoquinolines		adrenergic agent;
antihypertensive agent;
human metabolite;
sympatholytic agent
pinacidil
Pinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)		5.06101pyridines
n'-cyano-n-(3-pyridyl)-n''-(t-butyl)guanidine
N'-cyano-N-(3-pyridyl)-N''-(t-butyl)guanidine: structure given in first source		1.9710
3-pyridyl pinacidil
3-pyridyl pinacidil: RN refers to cpd without isomeric designation		1.9810
ConditionIndicatedRelationship StrengthStudiesTrials
Blood Pressure, High
[description not available]		02.3820
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		02.3820
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		01.9710
Cirrhosis, Liver
[description not available]		01.9610
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		01.9610