Gary L Stump
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Explore the profile of Gary L Stump including associated specialties, affiliations and a list of published articles.
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18
Citations
133
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Recent Articles
1.
Wolkenberg S, Nolt M, Bilodeau M, Trotter B, Manley P, Kett N, et al.
Bioorg Med Chem Lett
. 2017 Jan;
27(4):1062-1069.
PMID: 28131713
Selective inhibition of Kv1.5, which underlies the ultra-rapid delayed rectifier current, I, has been pursued as a treatment for atrial fibrillation. Here we describe the discovery of MK-1832, a Kv1.5...
2.
Regan C, Stump G, Detwiler T, Chen L, Regan H, Gilberto D, et al.
J Pharmacol Toxicol Methods
. 2016 May;
81:107-14.
PMID: 27166580
Introduction: There has been an increasing need to conduct investigative safety pharmacology studies to complement regulatory-required studies, particularly as it applies to a comprehensive assessment of cardiovascular (CV) risk. Methods:...
3.
Lynch Jr J, Stump G, Kane S, Regan C
J Cardiovasc Pharmacol
. 2009 May;
53(6):474-9.
PMID: 19430309
The triptans, serotonin 5-HT 1B/1D agonists exemplified by sumatriptan, are an effective class of migraine therapy but have class labeling contraindicating their use in patients with coronary artery disease. Triptans...
4.
Regan C, Stump G, Kane S, Lynch Jr J
J Pharmacol Exp Ther
. 2008 Nov;
328(2):571-8.
PMID: 18997059
Calcitonin gene-related peptide (CGRP) is a sensory neuropeptide that also has potent vasodilator activity. There are conflicting preclinical reports regarding the effect of CGRP receptor antagonism in the setting of...
5.
Regan C, Kiss L, Stump G, McIntyre C, Beshore D, Liverton N, et al.
J Pharmacol Exp Ther
. 2007 Oct;
324(1):322-30.
PMID: 17967939
Drug discovery efforts have focused recently on atrial-selective targets, including the Kv1.5 channel, which underlies the ultrarapid delayed rectifier current, I(Kur), to develop novel treatments for atrial fibrillation (AF). Two...
6.
Nguyen K, Claiborne C, McCauley J, Libby B, Claremon D, Bednar R, et al.
Bioorg Med Chem Lett
. 2007 May;
17(14):3997-4000.
PMID: 17498948
A novel series of cyclic benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 29 is orally active in a carrageenan-induced rat hyperalgesia model of pain.
7.
Regan C, Stump G, Wallace A, Anderson K, McIntyre C, Liverton N, et al.
J Cardiovasc Pharmacol
. 2007 Apr;
49(4):236-45.
PMID: 17438409
The cardiac electrophysiologic effects of ISQ-1, an isoquinolinone I(Kur) blocker, were characterized in vivo. In rat, ISQ-1 elicited maximal 33% to 36% increases in atrial and ventricular refractoriness at a...
8.
Liverton N, Bednar R, Bednar B, Butcher J, Claiborne C, Claremon D, et al.
J Med Chem
. 2007 Jan;
50(4):807-19.
PMID: 17249648
The discovery of a novel series of NR2B subtype selective N-methyl-d-aspartate (NMDA) antagonists is reported. Initial optimization of a high-throughput screening lead afforded an aminopyridine derivative 13 with significant NR2B...
9.
Trotter B, Nanda K, Kett N, Regan C, Lynch J, Stump G, et al.
J Med Chem
. 2006 Nov;
49(24):6954-7.
PMID: 17125248
Novel 3-cyanoisoquinoline Kv1.5 antagonists have been prepared and evaluated in in vitro and in vivo assays for inhibition of the Kv1.5 potassium channel and its associated cardiac potassium current, IKur....
10.
Nanda K, Nolt M, Cato M, Kane S, Kiss L, Spencer R, et al.
Bioorg Med Chem Lett
. 2006 Sep;
16(22):5897-901.
PMID: 16949818
This letter describes the discovery of a novel series of potent Kv1.5 ion channel antagonists based on a diisopropyl amide scaffold. Structure-activity relationships of functionalized analogs are discussed. Key compound...