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J R Regan

Publications and source records attributed to J R Regan.

5 recordsLinked to original sources
PubMed1990

Angiotensin-converting enzyme inhibitors. 9. Novel [[N-(1-carboxy-3-phenylpropyl)amino]acyl]glycine derivatives with diuretic activity.

A series of molecules 1 having sulfonamide diuretic moieties covalently linked to non-sulfhydryl angiotensin-converting enzyme inhibitors (ACEI) were prepared and tested for both activities. IC50 values for ACEI as low as 7 nM were observed. Discernable diuretic activity was seen for several hydrochlorothiazide-based molecules. Effects of the ACEI and diuretic structures on the respective potencies are discussed.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed1990

Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.

Compounds 1a-g consisting of enalaprilat covalently bonded to aryl sulfonamides, including several known thiazide diuretics, were synthesized and tested for ACE inhibitory and diuretic and overall antihypertensive effects. All compounds were potent ACE inhibitors in vitro, with IC50 = 6.5-85 nM. At 10 mg/kg iv or ip in the rat, 1a-g inhibited the AI pressor response by 76-100%; inhibition declined significantly upon oral dosing. Compounds 1a and 1f at 100 mg/kg ip in the sodium-depleted, spontaneously hypertensive rats reduced blood pressure 28-35% and 41-42%, respectively. Compounds 1a and 1f elicited natriuresis and kaliuresis without accompanying volume increases in the rat; 1c at 25 mg/kg iv induced delayed diuresis. Compound 1f has been chosen for further development.

Angiotensin-Converting Enzyme Inhibitors↗
PubMedDate not supplied

Spontaneous splenic rupture associated with thrombolytic therapy and/or concomitant heparin anticoagulation.

Two cases of spontaneous splenic rupture in connection with thrombolytic therapy and concomitant heparin anticoagulation are reported. One patient was being treated for peripheral arterial graft occlusion using intraarterial urokinase, the other received intravenous infusion of streptokinase for acute myocardial infarction. Neither patient had a condition predisposing to splenic rupture. Although rare, previous reports of spontaneous splenic rupture associated with thrombolytic therapy and/or anticoagulation have been reported. Splenic rupture as a complication of thrombolytic therapy and/or anticoagulation should be considered when unexplained abdominal symptoms, hypotension, or blood loss is encountered.

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