Search Results - "Gaul, S L"
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Pyridinone Derivatives: Specific Human Immunodeficiency Virus Type 1 Reverse Transcriptase Inhibitors with Antiviral Activity
Published in Proceedings of the National Academy of Sciences - PNAS (01-08-1991)“…Derivatives of pyridinones were found to inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) activity and prevent the spread of…”
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Non-Peptide GPIIb/IIIa Inhibitors. 20. Centrally Constrained Thienothiophene α-Sulfonamides Are Potent, Long Acting in Vivo Inhibitors of Platelet Aggregation
Published in Journal of medicinal chemistry (01-07-1999)“…The synthesis and pharmacology of 4, a potent thienothiophene non-peptide fibrinogen receptor antagonist, are reported. Compound 4 inhibited the aggregation of…”
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Non-Peptide Glycoprotein IIb/IIIa Inhibitors. 17. Design and Synthesis of Orally Active, Long-Acting Non-Peptide Fibrinogen Receptor Antagonists
Published in Journal of medicinal chemistry (06-06-1997)“…The synthesis and pharmacological evaluation of 5 (L-738,167), a potent, selective non-peptide fibrinogen receptor antagonist is reported. Compound 5 inhibited…”
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Identification and characterization of endothelin converting activity from EAHY 926 cells: evidence for the physiologically relevant human enzyme
Published in Archives of biochemistry and biophysics (01-01-1994)“…A neutral proteolytic activity that converts human Big endothelin-1 (Big Et-1) to endothelin-1 has been identified from a human endothelial hybrid cell line,…”
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Enhancement of the Humoral Response of T Cell-Depleted Murine Spleens by a Factor Derived from Human Monocytes in Vitro
Published in The Journal of immunology (1950) (01-09-1974)“…Abstract The humoral response of thymus-derived (T) cell-depleted murine spleen cultures was stimulated by the addition of human leukocytes. The stimulatory…”
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Transglutaminase Inhibition by 2-[(2-Oxopropyl)thio]imidazolium Derivatives: Mechanism of Factor XIIIa Inactivation
Published in Biochemistry (Easton) (01-08-1994)“…The physiologic role of several transglutaminases could be more precisely defined with the development of specific inhibitors for these enzymes. In addition,…”
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Identification of low molecular weight GP IIb/IIIa antagonists that bind preferentially to activated platelets
Published in The Journal of pharmacology and experimental therapeutics (01-06-1998)“…A critical function of fibrinogen in hemostasis and thrombosis is to mediate platelet aggregation by binding selectively to an activated form of glycoprotein…”
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Discovery and initial structure–Activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists
Published in Bioorganic & medicinal chemistry letters (22-10-2001)“…Thrombin is the most potent agonist of platelet activation, and its effects are predominantly mediated by platelet thrombin receptors. Therefore, antagonists…”
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Beta adrenoceptor blocking properties of MK-761
Published in The Journal of pharmacology and experimental therapeutics (01-10-1979)“…MK-761 is a new class of compound which has beta adrenoceptor antagonist and vasodilating properties in a single molecule. The compound has in vitro beta…”
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Central antihypertensive effects of inhibitors of the renin-angiotensin system in rats
Published in The American journal of physiology (01-12-1976)“…The possibility that mean arterial pressure (MA) might be maintained by an effect of angiotensin II or its precursors on the central nervous system in rats…”
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Nonpeptide GPIIb/IIIa inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation
Published in Bioorganic & medicinal chemistry letters (05-11-1996)“…Potency enhancing features of two series of fibrinogen receptor antagonists were combined to give analogs with improved potency and oral activity. Antagonists…”
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Comparative effects of verapamil, diltiazem and felodipine during experimental digitalis-induced arrhythmias
Published in Pharmacology (1987)“…We compared the abilities of three different calcium (Ca2+) entry blockers, verapamil, diltiazem and felodipine to abolish ouabain-induced ventricular ectopy…”
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Comparative effects of enalapril, enalaprilic acid and captopril in blocking angiotensin I-induced pressor and dipsogenic responses in spontaneously hypertensive rats
Published in Clinical and experimental hypertension. Part A, Theory and practice (1984)“…The role of central angiotensin converting enzyme (ACE), in the maintenance of high blood pressure, was examined in unanesthetized spontaneously hypertensive…”
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Antagonism of conditioned salivation in conscious dogs by antihypertensive drugs
Published in Canadian journal of physiology and pharmacology (01-08-1977)“…Methyldopate (methyldopa (ethyl ester)), carbidopa, clonidine, and ST-91 were evaluated for their effects on conditioned salivation in unanesthetized dogs…”
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Nonpeptide GPIIB/IIIA inhibitors. 16. Thieno[2,3- b]thiophene α-sulfonamides are potent inhibitors of platelet aggregation
Published in Bioorganic & medicinal chemistry letters (08-04-1997)“…Centrally constrained thieno[2,3- b]thiophene sulfonamides have provided a potent, selective, orally active series of platelet aggregation inhibitors. Compound…”
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3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters
Published in Journal of medicinal chemistry (01-06-1984)“…The (5-methyl-2-oxo-1,3- dioxol -4-yl)methyl and (5-tert-butyl-2-oxo-1, 3- dioxol -4-yl)methyl esters of 3-hydroxy-alpha-methyltyrosine (methyldopa) were…”
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Relationship between angiotensin I blockade and antihypertensive properties of single doses of MK-421 and captopril in spontaneous and renal hypertensive rats
Published in European journal of pharmacology (03-12-1981)“…The exact mechanism of action of angiotensin converting enzyme (ACE) inhibitors in reducing blood pressure is not known, although inhibition of angiotensin II…”
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Attenuation of hydrochlorothiazide-induced hypokalemia in dogs by a beta-adrenergic blocking drug, timolol
Published in European journal of pharmacology (01-06-1975)“…Hydrochlorothiazide, administered at 1, 3 and 9 mg/kg/day p.o. for 4 days, produced a dose-dependent lowering of plasma potassium and an elevation in plasma…”
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NR2B-Selective N-Methyl-d-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted Benzimidazoles
Published in Journal of medicinal chemistry (08-04-2004)“…Two classes of 5-substituted benzimidazoles were identified as potent antagonists of the NR2B subtype of the N-methyl-d-aspartate (NMDA) receptor. Selected…”
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