Pharmacological properties of 4-[2-(1, 2-benzisoxazol-3-yl)-2-(hexahydro-1H-azepin-1-yl)acetoxy]-1- ethyl-1- methylpiperidinium iodide (SX-810) were investigated and the following results were obtained. 1. In isolated guinea-pig ileum, SX-810 showed a competitive antagonistic effect against acetylcholine with a pA2 value of 7.93. 2. SX-810 (10-50 mg/kg p.o. or 10-50 micrograms/kg i.v.) inhibited the gastroduodenal contractions induced by bethanechol and carbachol in anaesthetized rats. 3. SX-810 (10-100 mg/kg p.o.) inhibited spontaneous gastric motility in conscious rats and rabbits. 4. SX-810 (10-100 mg/kg p.o.) inhibited gastric secretion in pylorus-ligated rats. 5. SX-810 (20-200 mg/kg p.o. or 1-10 mg/kg s.c.) inhibited the ulceration induced by pylorus ligation or by exposure to restrained and water-immersed stress in rats. 6. When administered orally to rats, SX-810 had no mydriatic effect even at 3000 mg/kg, but subcutaneously administered SX-810 (0.5-10 mg/kg) exhibited such action. 7. When administered orally to rats, SX-810 (100-500 mg/kg) caused no significant inhibition of the salivation induced by pilocarpine, but subcutaneously administered SX-810 (0.5-10 mg/kg) exhibited an inhibition of the salivation. In rabbits, SX-810 (200-500 mg/kg p.o.) also caused no significant inhibition of the salivation except at an extremely high dose of 1000 mg/kg p.o. 8. SX-810 (100-500 mg/kg p.o.) caused no significant effect on urine and electrolyte excretion in rats. These results indicate that oral use of SX-810 exhibits marked spasmolytic and antiulcerative activities without exerting systemic antimuscarinic side effects.

Animals↗

PubMed1986

A lower molecular weight gamma-chain variant in a congenital abnormal fibrinogen (Kyoto).

A gamma-chain variant with a lower molecular weight than the normal gamma chain was detected in a new congenital abnormal fibrinogen with impaired polymerization of the fibrin monomer and with normal release of fibrinopeptides A and B in a 45-year-old male. Purified fibrinogen analyzed on SDS-polyacrylamide gel electrophoresis under the reduced condition contained an abnormal protein band with an apparent molecular weight of 48,000 compared with the gamma chain with a molecular weight of 50,000. This abnormal protein band was found to be a gamma-chain variant from the molar ratio of A alpha chain:B beta chain:gamma chain:abnormal protein (about 2:2:1:1), with positive staining for carbohydrate and crosslinking ability. Crosslinked fibrin contained three types of gamma-gamma dimers with apparent molecular weights of 94,000 (the same as normal major gamma-gamma dimer), 92,000 and 90,000, and the plasmic digests of crosslinked fibrin in the presence of calcium retained three types of gamma-gamma dimer remnants. This suggests that the abnormal gamma-chain variant has a shorter polypeptide chain not in the NH2-terminal but in the COOH-terminal portion, probably at or near the polymerization site. This patient's two daughters had the same abnormal fibrinogen. This unique inherited abnormal fibrinogen was designated as fibrinogen Kyoto, and the gamma-chain variant as gamma Kyoto.

Blood Coagulation Disorders↗

PubMed1986

[Grading and operative indication for hypertensive cerebellar hemorrhage].

Fifty six patients with hypertensive cerebellar hemorrhage diagnosed by CT scan were hospitalized from November 1976 up to June 1984. The 35 male and 21 female patients ranged in age from 24 to 84 years, and 39 of them were operated on. The important factors related to prognosis of cerebellar hemorrhage were level of consciousness, size of hematoma on CT scan, and massive ventricular hemorrhage resulting in obstruction of the ventricular system. We classified the patient with cerebellar hemorrhage into 5 grades, according to the severity of these factors. Grade I indicates cerebellar signs without disturbance of consciousness and size of hematoma less than 25 mm measured by CT scan. Grade II indicates disturbance of consciousness (stupor), or progressive neurological deficits, and size of hematoma less than 50 mm without acute hydrocephalus. Grade III reveals disturbance of consciousness (stupor-semicoma), and size of hematoma less than 50 mm with acute hydrocephalus. Grade IV reveals severe disturbance of consciousness (semicoma), and size of hematoma less than 50 mm with massive ventricular hemorrhage. Grade V exhibits deep coma, and more than 50 mm diameter of hematoma. The prognosis of all of 9 patients in Grade I was good, Eleven out of 13 patients (85%) in Grade II and all of 9 patients in Grade III were alive. Fourteen out of 19 patients (74%) in Grade IV and all of 6 patients in Grade V expired in spite of operation. The patients of Grade I should be treated by conservative therapy. The patients of Grade II, Grade III, and Grade IV should be managed surgically. Surgical treatment for Grade V is not advisable.

Adult↗

PubMed1986

Purpura fulminans in a Chinese boy with congenital protein C deficiency.

Severe and recurrent purpura fulminans developed in a Chinese boy at one day of age. Results of coagulation studies performed on the patient during attacks were compatible with the diagnosis of disseminated intravascular coagulation. Subsequent investigations have revealed that the patient is homozygous and that his parents are heterozygous for protein C deficiency. Cryoprecipitate and fresh frozen plasma induced a remission, and administration of warfarin has been successful in preventing recurrence of attacks for as long as 8 months without infusion of any plasma components. None of the family members who are heterozygous for protein C deficiency have had thrombotic episodes.

Combined Modality Therapy↗

PubMed1986

[Role of lipid peroxidation in the formation of acute gastric mucosal lesions after burn stress].

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Animals↗

PubMed1986

Chronic ethylene oxide poisoning in a factory manufacturing medical appliances.

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Adult↗

PubMed1985

Purification and complete amino acid sequence of canine pancreatic secretory trypsin inhibitor.

Pancreatic secretory trypsin inhibitor (PSTI) was purified from canine pancreatic juice by HPLC. Canine PSTI inhibited bovine trypsin activity stoichiometrically and strongly with a dissociation constant of below 10(-9) M. The amino acid sequence of canine PSTI was determined by conventional methods. It had one more amino acid residue at the amino-terminus than other mammalian PSTIs, i.e. human, porcine, bovine and ovine.

Amino Acid Sequence↗

PubMed1985

High doses of gamma globulin and methylprednisolone therapy for idiopathic thrombocytopenic purpura in children.

In four children with chronic idiopathic thrombocytopenic purpura (ITP), high doses of gamma globulin or methylprednisolone were effective in increasing platelet counts transiently, yet there was no quantitative relationship between the platelet responses to these two therapies. This finding suggests a qualitative difference in the mechanisms of increasing platelets by the two drugs. High doses of gamma globulin and methylprednisolone showed a synergistic effect on the initial and maximal platelet responses, suggesting an intensification of the effect of gamma globulin by methylprednisolone. This combination therapy should be clinically useful, particularly in the control of acute haemorrhage or in preparations for emergency surgery.

Child↗

PubMed1985

The multiplicity of human pancreatic secretory trypsin inhibitor.

Four forms of pancreatic secretory trypsin inhibitor (PSTI; A1, A2, B, and C) were purified from human pancreatic juice. According to sequence results, the primary structure of B was different from that reported earlier (Greene, L.J., et al. (1976) Method Enzymol. 45, 813-825) at two positions, i.e. Asn21----Asp21, Asp29----Asn29. A1 and A2 were deamidated forms of B judging from peptide mappings with Staphylococcus aureus V8 protease. Gln45 in B was replaced by Glu in A1 and Gln51 in B was replaced by Glu in A2. C was an inhibitor lacking five amino acid residues from the amino terminal of B. B and C inhibited human cationic trypsin activity stoichiometrically with similar dissociation constants, but A1 and A2 showed poorer trypsin inhibitory activity than B and C.

Amino Acid Sequence↗

PubMed1985