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Biomedical subjects

K Nishida

Publications and source records attributed to K Nishida.

At least 433 records · Page 24Linked to original sources

Receptor binding properties of the new calcium antagonist benidipine hydrochloride.

The in vitro receptor binding affinity of (+/-)-(R*)-2,6-dimethyl-4-(m-nitrophenyl)-1,4-diyhydropyridine-3, 5-dicarboxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049) to 3H-nitrendipine, alpha 1-adrenergic, alpha 2-adrenergic, beta-adrenergic, muscarinic cholinergic, H1-histaminergic, D2-dopaminergic, S2-serotonergic, A1 adenosine and A2 adenosine receptors was compared with that of nifedipine, nitrendipine and nicardipine. KW-3049 bound stereospecifically to 3H-nitrendipine binding sites of rat myocardium with high affinity (Ki = 0.13 nmol/l) and to the rat brain alpha 1-receptor (Ki = 1.2 mumol/l). KW-3049 exhibited no remarkable binding affinity to alpha 2, beta-, D2-, H1-, S2-, A1-, A2- and muscarinic cholinergic receptors at 100 mumol/l. KW-3049 showed competitive inhibition against 3H-nitrendipine binding when it was added simultaneously with the ligand and rat heart membranes. KW-3049 did not affect the dissociation of 3H-nitrendipine from the receptor sites. The inhibitory activity of various isomers of KW-3049 at the 3H-nitrendipine binding sites was shown in the order of S-S-(+) greater than KW-3049 (racemate, S-S-(+), R-R-(-] greater than R-R-(-) greater than S-R-(-) greater than racemate (R-S-(+), S-R-(-] greater than R-S-(+). S-S-(+)isomer was 12 times more potent than R-R-(-)isomer on Ki basis, whereas alpha 1-adrenoceptors followed the order of S-S-(+), R-S-(+), KW-3049, racemate (R-S-(+), S-R-(-], S-R-(-) and R-R-(-).

Animals↗

Slow dissociation of the new slow-onset and long-acting calcium antagonist benidipine hydrochloride from 3H-nitrendipine binding sites.

The dissociation rates of (+/-)-(R*)-2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarb oxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049) and some calcium antagonists from 3H-nitrendipine binding sites were studied by a centrifugation technique and a filter-absorbed tissue method. KW-3049 dissociated from 3H-nitrendipine binding sites more slowly than other calcium antagonist, namely nifedipine, nitrendipine, nilvadipine, nicardipine and nisoldipine. The slow dissociation of KW-3049 from 3H-nitrendipine binding sites was supported by the equilibrium binding studies. When KW-3049 was preincubated with rat cardiac membrane, its inhibitory potency was enhanced 2.6-fold, whereas nifedipine did not alter its potency. In ex vivo binding, following administration of KW-3049 to rat, 3H-nitrendipine binding site was occupied in a dose-dependent manner and this occupation returned to a control level after 24 h. These results of receptor binding studies are in agreement with the pharmacological characteristics of KW-3049.

Animals↗

Sensitive radioreceptor assay of the calcium antagonist benidipine hydrochloride in plasma and urine.

Plasma and urinary concentrations of (+/-)-(R*)-2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarb oxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049) were measured by the radioreceptor assay using 3H-nitrendipine and rat cardiac membrane receptor. After methanol deproteinization and ethyl ether extraction under alkaline conditions as pretreatment, the detection limit for KW-3049 in plasma was 0.2 ng/ml using 0.5 ml of sample. For the urine, 0.05 ml of urine sample was directly added to the assay system, and detection limit of drug was 1 ng/ml. The cross-reactivity of the presumable metabolites was 1% or less of the unchanged drug. This radioreceptor technique was applied to pharmacokinetic studies and useful for monitoring the drug after therapeutic dosing.

Animals↗

[Examination of 400 cases of early gastric cancer--appropriate operation in view of follow-up observations].

Four hundred surgical cases of early gastric cancer in the Department of Surgery, National Tochigi Hospital, during these 15 years were reviewed to examine the influence of histopathological features and the degree of lymph node involvement on their prognosis. Although a decreasing trend of the accumulated survival rate was observed in Ro cases which died due of other diseases were frequently encountered as compared to more than R1 cases with regard to the degree of lymph node dissection no significant difference was found among various operative modes dissection. No significant difference was also observed macroscopic absolute and relative dissection. Recently, we have adopted R0 for cancer and R1 for Group 1 lymph node involvement in sm cancer. The great omentum, lesser omentum and cecal pouch are preserved as a rule. In the cases of N(+), dissection of affected lymph nodes including No. 7, 8 and 9 should be performed because of high incidence of metastasis. We conclude these surgical policies are appropriate against early gastric cancers because of good prognosis and no serious postoperative complications.

Adult↗

[A case of quadrigeminal cistern arachnoid cyst associated with hydrocephalus].

A case of quadrigeminal cistern arachnoid cyst associated with hydrocephalus is reported. A 1-year-old girl was admitted to our service on July 31, 1984, because of mental retardation and an enlarged head. She was born of a full-term pregnancy and normal vaginal delivery without prenatal complications. Progressive increase in her head circumference was noticed at the age of 6 months by her family physician. On admission she was found to be a well-nourished infant with a head circumference of 56 cm, bulging anterior fontanelle and mental retardation. Marked dilatation of the lateral ventricles and a large cyst in the quadrigeminal cistern were demonstrated on plain CT. There were no findings of communication between the ventricular system and the cyst on metrizamide CT ventriculography. The extension of the cyst from the quadrigeminal cistern to the right cerebello-pontine angle was demonstrated on reconstructed coronal CT. Reconstructed sagittal section revealed huge hydrocephalus caused by aqueductal stenosis. A vertebral angiography demonstrated opening of the para-mesencephalic segments of the bilateral posterior cerebral arteries and downward displacement of the right superior cerebellar artery. Accordingly, a large quadrigeminal cistern arachnoid cyst with hydrocephalus caused by aqueductal stenosis was suspected. Following V-P shunt operation for hydrocephalus, right temporo-parietal craniotomy was performed. The inner wall of the lateral ventricle was thin and an expanding cyst was observed through it. A partial resection of the cyst wall with the ventricular wall was performed to obtain communication between the cyst and lateral ventricle. The content of the cyst was watery clear fluid like CSF.(ABSTRACT TRUNCATED AT 250 WORDS)

Arachnoid↗

Estimation of carbohydrate antigen (CA) 19-9 levels in pure pancreatic juice of patients with pancreatic cancer.

Carbohydrate antigen (CA) 19-9 levels in pure pancreatic juice from patients with pancreatic cancer, chronic pancreatitis, and other diseases were determined, and their clinical value was assessed. CA 19-9 levels in pancreatic juice were generally very high, compared with those in serum. In addition, the pancreatic juice CA 19-9 levels in patients with pancreatic cancer were significantly higher than those in patients with chronic pancreatitis and other various diseases used as controls. The assay of pancreatic juice CA 19-9 seemed to be valuable in the diagnosis of pancreatic cancer, showing a diagnostic value approximately similar to that of the serum CA 19-9 assay and clearly superior to that of the serum or pancreatic juice carcinoembryonic antigen assay.

Antigens, Neoplasm↗

[Primary intracranial malignant germ cell tumor associated with abnormal high value of alpha-fetoprotein and human chorionic gonadotropin].

A case of primary suprasellar germ cell tumor that produced alpha-fetoprotein (AFP) and human chorionic gonadotropin (HCG) in a 8-year-old boy is reported. Partial removal of tumor and combination chemotherapy using cisplatin, vincristine, and bleomycin (modified PVB therapy) resulted in an almost definite regression of the tumor and improvement from clinical symptoms in this case. After the chemotherapy the concentrations of both serum AFP and serum HCG decreased to normal levels as well. Moreover by the immunoperoxidase method AFP, HCG, and placental alkaline phosphatase were found in this particular tumor tissue. In reviewing previous reports the immunohistochemical demonstration of three tumor markers in a single germ cell tumor is seemed to be extremely rare.

Antineoplastic Combined Chemotherapy Protocols↗