Page last updated: 2024-12-10

aprikalim

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

Cross-References

ID SourceID
PubMed CID3034038
SCHEMBL ID4259442
MeSH IDM0169342

Synonyms (21)

Synonym
aprikalim
2h-thiopyran-2-carbothioamide, tetrahydro-n-methyl-2-(3-pyridinyl)-, 1-oxide
rp 52891
n-methyl-2-(3-pyridyl)tetrahydrothiopyran-2-carbothioamide-1-oxide
rp 49356
(2r)-n-methyl-1-oxo-2-pyridin-3-ylthiane-2-carbothioamide
rp -52891
aprikalim [inn]
(-)-(1r,2r)-tetrahydro-n-methyl-2-(3-pyridyl)thio-2h-thiopyran-2-carboxamide 1-oxide
aprikalimum [inn-latin]
aprikalimum
2h-thiopyran-2-carbothioamide, tetrahydro-n-methyl-2-(3-pyridinyl)-, 1-oxide, (1r,2r)-rel
unii-374bh4kvrg
374bh4kvrg ,
132562-26-6
SCHEMBL4259442
2125831-34-5
(1r,2r)-n-methyl-2-(pyridin-3-yl)tetrahydro-2h-thiopyran-2-carbothioamide 1-oxide
(2r)-n-methyl-2-(pyridin-3-yl)tetrahydro-2h-thiopyran-2-carbothioamide 1-oxide
rel-(1r,2r)-n-methyl-2-(pyridin-3-yl)tetrahydro-2h-thiopyran-2-carbothioamide 1-oxide
AKOS040746584

Research Excerpts

Overview

Aprikalim is a potent, specific, and selective opener of ATP-sensitive K+ (KATP) channels.

ExcerptReferenceRelevance
"Aprikalim is a potent, specific, and selective opener of ATP-sensitive K+ (KATP) channels. "( The myocardial lesions produced by the potassium channel opener aprikalim in monkeys and rats are prevented by blockade of cardiac beta-adrenoceptors.
Algate, C; Belin, V; Cavero, I; Gosselin, S; Hodge, T; Jordan, R; Nohynek, G; Picaut, P, 1996
)
1.98

Actions

Aprikalim was able to produce sustained and reproducible electromechanical arrest that was reversible by reperfusion.

ExcerptReferenceRelevance
"Aprikalim was able to produce sustained and reproducible electromechanical arrest that was reversible by reperfusion."( Is there an alternative to potassium arrest?
Cohen, NM; Damiano, RJ; Wechsler, AS, 1995
)
1.01
"Aprikalim was able to produce sustained and reproducible electromechanical arrest that was reversible by reperfusion."( Hyperpolarized arrest attenuates myocardial stunning following global surgical ischemia: an alternative to traditional hyperkalemic cardioplegia?
Cohen, NM; Damiano, RJ, 1994
)
1.01

Treatment

Pretreatment with aprikalim depressed the contraction by phenylephrine from 140.6 +/- 27.6% to 49.3 +/- 14.1% (P=0.002) and shifted the EC50 11.0-fold higher in rings treated with 1 microM aprikale. At 30 microM it also significantly depressed the maximal contraction for 5-HT (35.70 +/- 4.9% versus 103.30 +/- 9.8%, p < 0.001) and NE (90.60 +/- 15.6%.

ExcerptReferenceRelevance
"Pretreatment with aprikalim depressed the contraction by phenylephrine from 140.6 +/- 27.6% to 49.3 +/- 14.1% (P=0.002) and shifted the EC50 11.0-fold higher in rings treated with 1 microM aprikalim (P=0.007)."( Inhibition of vasoconstriction by potassium channel opener aprikalim in human conduit arteries used as bypass grafts.
He, GW; Yang, CQ, 1997
)
0.86
"Pretreatment with aprikalim at 1 microM depressed AII-induced contraction (33.20 +/- 7.5% versus 59.70 +/- 7.3%, p < 0.01) but only shifted the curves rightward for 5-HT or NE (EC50 3.1 or 4.3-folds higher, p < 0.05), whereas at 30 microM it also significantly depressed the maximal contraction for 5-HT (35.70 +/- 4.9% versus 103.30 +/- 9.8%, p < 0.001) and NE (90.60 +/- 15.6% versus 125.60 +/- 7.9%, p < 0.05)."( Effects of potassium channel opener aprikalim on the receptor-mediated vasoconstriction in the human internal mammary artery.
Floten, HS; Furnary, AP; He, GW; Liu, MH; Yim, AP, 2001
)
0.91

Bioavailability

ExcerptReferenceRelevance
" A slow-release oral formulation produced a significant delay in the rate of absorption, a 4-fold decrease in the peak plasma level, and a 2-fold decrease in apparent oral bioavailability relative to that observed for an oral solution."( Aprikalim: radioimmunoassay and pharmacokinetic studies in mouse, monkey, and dog.
Chevalier, P; Frydman, A; Montay, G; Rouillard, C, 1994
)
1.73

Dosage Studied

ExcerptRelevanceReference
"Arterial depressor dose-response curves to nitroprusside (a nitric oxide donor, 5-60 micrograms."( Vascular hyporesponsiveness to vasodilators in rats with cirrhosis.
Gadano, A; Lebrec, D; Moreau, R; Safka, V, 1997
)
0.3
" Incubation with CGRP8-37 (10(-6) M) specifically during the 90-minute desensitization period with nitroglycerin resulted in even greater impairment in the response to nitroglycerin in tolerant rings, even though the calcitonin gene-related peptide antagonist had been washed out before completion of the nitroglycerin dose-response curve."( Nitroglycerin-induced release of calcitonin gene-related peptide from sensory nerves attenuates the development of nitrate tolerance.
Ghatta, S; O'Rourke, ST, 2006
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (116)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (6.03)18.7374
1990's94 (81.03)18.2507
2000's13 (11.21)29.6817
2010's2 (1.72)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: 18.38

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

MetricThis Compound (vs All)
Research Demand Index18.38 (24.57)
Research Supply Index4.77 (2.92)
Research Growth Index5.52 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews6 (5.13%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other111 (94.87%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]