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Topical ocular hypotensive effects of the novel angiotensin converting enzyme inhibitor SCH 33861 in conscious rabbits.
Findings suggest that inhibition of ocular ACE may represent an effective means of reducing intraocular pressure and indicate that SCH 33861 is 500-fold more potent on a weight basis than is timolol in lowering IOP. Expand
Antihypertensive and hemodynamic actions of SCH 19927, the R,R-isomer and labetalol.
It is concluded that vasodilatation is largely responsible for the antihypertensive response to labetalol and particularly to SCH 19927, a potentially useful agent which would be expected to reduce pressure in humans by two complementary mechanisms, beta blockade and vasodILatation. Expand
Muscarinic agonists and antagonists in the treatment of Alzheimer's disease.
Exploration of a series of piperidinylpiperidines has yielded the potent and selective M2 antagonist SCH-217443, which has excellent bioavailability in rats and dogs and shows activity in a rat model of cognition. Expand
Inhibition of endothelial derived relaxing factor (EDRF) aggravates ischemic acute renal failure in anesthetized rats
The results of the present study suggest that the function of the ischemic kidney is sustained by EDRF/NO and is thus more sensitive to NO synthase inhibition. Expand
The synergistic hypocholesterolemic activity of the potent cholesterol absorption inhibitor, ezetimibe, in combination with 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitors in dogs.
The combination of this class of cholesterol absorption inhibitors with an HMG CoA reductase inhibitor should be very effective clinically at reducing plasma cholesterol levels, even with reduced dietary intake of cholesterol. Expand
SCH 39370, a neutral metalloendopeptidase inhibitor, potentiates biological responses to atrial natriuretic factor and lowers blood pressure in desoxycorticosterone acetate-sodium hypertensive rats.
The results suggest that NEP can play a role in ANF disposition in vivo and that potentiation of the biological activities of high doses of ANF by SCH 39370 may be consequent to its inhibitory effect on ANF degradation. Expand
Atrial Natriuretic Factor‐Potentiating and Antihypertensive Activity of SCH 34826: An Orally Active Neutral Metalloendopeptidase Inhibitor
The effects of SCH 34826 on responses to atrial natriuretic factor and on blood pressure were evaluated in rats and suggest that neutral endopeptidase inhibition may represent a new approach to treatment of some forms of hypertension. Expand
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]-
The nature and the size of the benzylic substituent are shown to be the key to controlling receptor selectivity (CCR5 vs M1, M2) and potency in the title compounds. Optimization of the lead benzylicExpand
HPLC-API/MS/MS : a powerful tool for integrating drug metabolism into the drug discovery process
Abstract HPLC combined with atmospheric pressure ionization (API) mass spectrometry (MS) has become a very useful tool in the pharmaceutical industry. The technique of HPLC-API/MS/MS is becoming veryExpand
SCH 57790, a selective muscarinic M(2) receptor antagonist, releases acetylcholine and produces cognitive enhancement in laboratory animals.
The effects observed with SCH 57790 in behavioral studies were qualitatively similar to the effects produced by the clinically used cholinesterase inhibitor donepezil, suggesting that blockade of muscarinic M(2) receptors is a viable approach to enhancing cognitive performance. Expand