491 Result(s)
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Article
L-Tryptophane and sleep
L-Tryptophane, an essential amino acid and a precursor of serotonin, is shown to have definite effects on human sleep. In normal subjects it reduces sleep latency and slightly increases sleep length without alt....
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Article
Doxepin and amitriptyline-perphenazine in mixed anxious-depressed neurotic outpatients: A collaborative controlled study
Doxepin was compared to the combination of amitriptyline-perphenazine in a double-blind controlled study conducted with 100 clinic, general practice, and private psychiatric practice outpatients diagnosed as s...
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Article
Clomipramine and amitriptyline in depressed outpatients
Clomipramine (75–125 mg/day), a relatively new tricyclic anti-depressant, was compared to amitriptyline (75–125 mg/day) in a double-blind 6 week trial carried out with 93 psychiatric and 75 non-psychiatric dep...
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Article
Strategies for the synthesis of kallikrein substrates useful for radioassay
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Chapter
Preparation of Intrinsically-Labelled Kinins
As part of a program to prepare bradykinin (H-Arg-Pro-ProGly-Phe-Ser-Pro-Phe-Arg-OH) labelled at high specific radioactivities, we have synthesized three analogs for dehalogenation in tritium gas: [4-Br-Phe5]-bra...
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Chapter
A Simple Radioassay for Human Urinary Kallikrein
We have developed a sensitive, highly selective assay for human urinary kallikrein (HUK) that uses Pro-Phe-Arg-[3H]benzylamide as substrate. The substrate was prepared from Pro-Phe-Arg-3-iodo-benzylamide by dehal...
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Article
Pharmacokinetic study of sisomicin in humans
Detailed analyses of the pharmacokinetics of sisomicin administered at doses of 25, 50, and 100 mg intravenously and intramuscularly to healthy volunteers established that the drug is handled by a two-compartm.....
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Article
The upper and lower bounds of rate constants for general mammillary compartment systems
The upper and lower bounds of rate constants for general mammillary three and four compartment systems have been derived. It is further proposed that the midpoints of the bounds can be used as initial estimate.....
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Chapter
Intestinal Drug Metabolism — Presystemic and Systemic Mechanisms and Implications
The purpose of this communication is to briefly review a series of studies, initiated with Sid Riegelman and carried on by a second generation of graduate students, on mechanisms involved in the intestinal con...
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Article
Comparison of central gastric antisecretory effects of desmethylimipramine, doxepin and pirenzepine in rats
Certain tricyclic drugs, some of which are primarily used clinically as antidepressants, have been shown to act as gastric antisecretory agents. The anatomical site(s) and mechanism(s) of action of these agent...
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Article
Analgesic effect of histamine induced by intracerebral injection into mice
Three methods were used to study the analgesic effect of intracerebral injection of histamine (Hi) on mice: the writhing test (acetic acid and phenylquinone), the electrical stimulation of the tail and the hot...
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Article
Degradation of articular cartilage by copper and hydrogen peroxide
When porcine articular cartilage particles were incubated in the presence of Cu2+ and H2O2 at pH 7.4, solubilization of collagen and proteoglycan was observed. Both agents were necessary and the rate of solubiliz...
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Article
Concentration andpH dependent steady-state volume of distribution of methotrexate estimated by a simple physiologically based method
The effects of plasma concentration and pH on the steady-state volume of distribution, Vss,of methotrexate (MTX) were studied in five conditioned male beagle-mongrel dogs. Steady-state plasma MTX concentrations ...
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Article
UrinarypH and urine flow independent renal clearance of methotrexate in dogs
The effects of urine flow and pH on methotrexate renal clearance were studied in seven conditioned male Beagle-Mongrel dogs. Steady-state plasma methotrexate and inulin concentrations were achieved by i.v. infus...
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Chapter
Synthetic Inhibitors of Carboxypeptidase N
Further to explore the functions of carboxypeptidase N (CPN) in vivo, we undertook two studies to find CPN inhibitors of high potency and relatively long duration of action. In each study we exami...
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Chapter
Slow Tight Binding Inhibitors of Angiotensin Converting Enzyme
We have found that apparent Ki values of some, but not all, carboxyalkyl-dipeptide inhibitors of angiotensin converting enzyme decrease as a function of incubation time. The most potent of the ACE inhibitors t...
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Chapter
Carboxyalkyl Peptide Inhibitors of Kininase II: Chiral Synthesis
Heretofore, carboxyalkyl peptide inhibitors of kininase II (e. g. N-[l-carboxy-3-phenylpropyl]-Ala-Pro, “enalaprilic acid”) have been synthesized by means that yield racemic product. Typically, the secondary a...
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Chapter
Radiolabelled Substrates for Angiotensin Converting Enzyme
Six [3H]benzoyl-tripeptides were prepared and tested as substrates for angiotensin converting enzyme. Each was prepared first as its [4-iodo]- benzoyl-analog, and an atom of 3H per molecule was introduced by cata...
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Chapter
Copper Status and Cadmium Administration: Effects on Zinc Distribution, Metallothionein, and Superoxide Dismutase Activity in Liver
In part, this work focuses on the extent to which cadmium intoxication can modulate SOD and MT levels when dietary copper is limiting. Although the ability of cadmium to stimulate SOD activity directly or caus...
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Article
Excitatory effect of histamine on EEGs of the cortex and thalamus in rats
When low frequency electrical stimulations were repeatedly applied to the rat midbrain reticular formation, the EEG spectral power recorded at the cortex and thalamus increased markedly, especially in the low ...
