Potent, low molecular weight thrombin receptor antagonists.
Several benzimidazole derivatives have been identified as potent thrombin receptor (PAR-1) antagonists as represented by compound 1h, which showed an IC(50) of 33 nM.
Molecular Weight↗
Biomedical subjects
K Eagen
Publications and source records attributed to K Eagen.
4-Aminosalicylic acid retention enemas in treatment of distal colitis.
Forty-five of 47 patients with distal ulcerative colitis completed a two-week double-blind, randomized, controlled trial to determine if 4-aminosalicylic acid (4-ASA) enemas, 1 g bid or 2 g bid, were therapeutically effective compared to placebo. Forty-one patients enrolled because they were refractory to or had side effects during conventional therapy with sulfasalazine or corticosteroids. Proctoscopic examination was done before and after two weeks of treatment. Patients kept daily diaries assessing: blood in stools, mucus in stools, tenesmus, abdominal pain, loss of appetite, fatigue, weight loss, and malaise. Severity of each symptom ranged from 0 (absent) to 3 (severe). A total severity score was calculated from the above for each patient. At the end of the two-week study, 35 patients elected to take 4-ASA in an open-label trial for one year. 4-ASA enemas in the 1-g bid but not the 2-g bid dosage were significantly more effective in improving symptoms than placebo: P less than or equal to 0.05. Neither dose of 4-ASA enema was better than placebo in improving the sigmoidoscopic appearance at the end of two-weeks. Forty-six percent of patients had complete resolution of all signs and symptoms in the open-label trial and 31% were better but still had sigmoidoscopic evidence of disease, a total response rate of 77%. Side effects were similar in the placebo and 4-ASA groups. We conclude that 4-ASA enemas in a dose of 1 g bid are safe and effective in the treatment of distal ulcerative colitis.
Adult↗
Self-administered nitrous oxide: an adjunct analgesic.
In a pilot study of 26 patients, a mixture of 50% nitrous oxide and 50% oxygen (N2O-O2) appeared to be an effective and safe analgesic for the incision and drainage of closed-space infections. The analgesic effect of N2O-O2, as measured by a Mean Analgesic Index, is augmented by both amnesic and dissociative effects, ie, patients remembered experiencing significantly less pain than they complained of during the procedure (p less than .01) and reported significantly more pain than they appeared to be having, as recorded by an observer (p less than .01). The patient's recollected pain, however, correlated well (r = .68) with the observer's assessment. Forty-two percent of patients had undergone a similar or identical procedure in the past without the benefit of N2O-O2 and made uniformly favorable comparative statement concerning the analgesic effect of the gas.
Abscess↗
Vestibular and medullary brain stem afferents to the abducens nucleus in the cat.
Brain stem neurons that project to the abducens nucleus (nVI) were labeled by the technique of retrograde transport of horseradish peroxidase (HRP). Following iontophoresis of HRP into nVI a large number of labeled cells are found in the ipsilateral vestibular nuclear complex, extending from the rostral medial vestibular nucleus into the ventral lateral vestibular nucleus. A smaller number of HRP-positive cells are also found in the contralateral medial vestibular nucleus. In addition, labeled cells are localized to the contralateral dorsomedial gigantocellular tegmental field as well as the nucleus praepositus hypoglossi of both sides, evidence that these neuronal groups may also be involved in eye movement control.
Abducens Nerve↗