摘要:

SUMMARY1. Omeprazole, a substituted benzimidazole and a potent gastric antisecretory drug has been tested for inhibition of microsomal drug oxidative function in the rat.2. A single dose of 40 mg/kg prolonged pentobarbitone sleeping times from 118 (range 73–168) min to 195 (159–222) min (P<0.01), pentobarbitone half‐lives from 89 (63–114) to 112 (54–146) min (P<0.05) and aminopyrine breath14CO2half‐lives from 43 (37–51) to 56 (49–79) min (P<0.05). Omeprazole in doses of 20 mg/kg or less had no significant effect.3. In prolonging pentobarbitone sleeping times omeprazole 40 mg/kg and an equimolar (30 mg/kg) dose of cimetidine were approximately equipotent.4. These results contrast with studies in man in which much smaller doses of omeprazole have been shown to produce clinically significant inhibition of

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00916.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

SUMMARY1. The circulatory responses to different intravenous doses of naloxone were studied in conscious rabbits before and after haemorrhage, under different conditions including prior ganglion blockade.2. Unless there had been blood loss, naloxone elicited no pressor response, even in high dose. After bleeding so that arterial pressure fell to 40 mmHg, the dose‐response relationship for naloxone had two components. Over a low‐dose range (threshold 0.3 mg/kg) naloxone had a modest pressor effect but did not affect heart rate. Over a much higher dose range (threshold 0.6 mg/kg) naloxone caused a marked rise in arterial pressure and a profound bradycardia. The highest dose of naloxone examined (25 mg/kg) caused a rise in arterial pressure of 70 mmHg and a reduction in heart rate of 160 beats/min.3. The pressor and bradycardic effects of naloxone were the same whether post‐haemorrhagic hypotension lasted 5, 10, 20 or 30 min.4. The responses to naloxone in low or high dose depended much more closely on the volume of blood removed than on the level to which arterial pressure fell. Even after non‐hypotensive haemorrhage a high dose of naloxone had marked pressor and bradycardic effects.5. Ganglion blockade prior to haemorrhage abolished the pressor response to a low, but not to a high, dose of naloxone.6. It was concluded that prolonged and severe hypotension are not necessary to ‘prime’ the cardiovascular system to respond to naloxone after haemorrhage. In a high dose its pressor effects appear to be mediated post‐ganglionically, but in a low dose it may act within the central n

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00917.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

SUMMARY1. This paper describes an investigation of the time course of changes in noradrenaline levels in epididymal and prostatic segments of rat vasa deferentia, for up to 91 days following unilateral vasectomy by medial transection, together with an investigation of the responses of isolated preparations of these segments to field stimulation of sympathetic terminals.2. No atrophy of testes or seminal vesicles, or of the prostatic and epididymal segments of operated vasa deferentia, was evident at 2, 4, 7, 28 and 91 days after unilateral vasectomy.3. Spectrophotofluorometric assay revealed that noradrenaline levels in epididymal segments of operated vasa deferentia declined rapidly (within 2 days) after unilateral vasectomy and remained below 10% of those in unoperated epididymal segments at days 4, 7, 28 and 91 post‐vasectomy. Noradrenaline levels in prostatic segments of operated vasa deferentia were unaffected by vasectomy.4. Histochemical studies revealed that catecholamine fluorescence in epididymal segments of operated vasa deferentia declined in parallel with the decline in tissue noradrenaline levels; no comparable changes occurred in prostatic segments.5. Field stimulation (10 pulses, 60 V, 1 ms, applied at 0.1–50 Hz) evoked frequency‐dependent contractions of unoperated epididymal segments and of operated and unoperated prostatic segments at 2, 4, 7, 28 and 91 days post‐vasectomy. At day 2 and 4 responses of prostatic segments of operated tissues, to frequencies below 5 Hz, exceeded those of corresponding unoperated segments, however, by day 91, there was a small but significant decline in responses. Responses of epididymal segments of operated vasa deferentia to all frequencies of stimulation declined by day 2 post‐vasectomy and were absent thereafter except in three of the 18 preparations studied at day 91.6. These results, taken together, confirm that there is a rapid decline in catecholamine levels in the epididymal segment of medially transected vasa deferentia following unilateral vasectomy. Minimal, if any, reinnervation of this segment occurs during the 3 month period following unilateral

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00918.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

SUMMARY1. One hundred and twenty‐one patients with hyperthyroidism of Graves' disease were treated with antithyroid drugs for 3 years and thyroidal response to an increase or decrease of TSH and the serum thyroid stimulating immunoglobulin (TSI) activity were studied in relation to the presence or absence of TSH binding inhibiting immunoglobulin (TBII).2. TBII activity was positive in 83% of untreated patients but decreased gradually with time during antithyroid drug therapy. Thyroidal radioactive iodine uptake (RAIU) was suppressed by T3in 86 of 121 treated patients but 16% of suppressible patients had TBII activity. Thyroidal RAIU was not suppressed by T3in 35 treated patients, and 19 of 35 unsuppressible patients had TBII activity but other 16 patients did not. When suppressible and unsuppressible patients were combined, suppression of serum T4and thyroidal RAIU by T3tended to be less in the presence of TBII activity.3. TSI activity was detected in the sera of untreated patients but did not correlate with TBII activity. TSI activity was undetectable after treatment for 3 years irrespective of presence or absence of TBII activity and T3‐suppressibility.4. TSH, T4and T3elevation in response to 500 μg thyrotropin releasing hormone (TRH) was normal in all treated patients irrespective of presence or absence of TBII activity and T3‐suppressibility.5. It is suggested thatin vivothyroidal responsiveness to an increase or decrease of endogenous TSH did not correlate with the presence or absence of TBII activity after long‐term therapy with antithyro

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00919.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

SUMMARY1. Hypotensive and natriuretic effects of chronically administered α‐human atrial natriuretic polypeptide (α‐hANP) were investigated in conscious spontaneously hypertensive rats (SHR) and Wistar‐Kyoto rats (WKY) in both sodium depletion and repletion.2. Systolic blood pressure was significantly reduced in SHR and WKY in both sodium deplete and replete states.3. Urinary sodium excretion was significantly increased in SHR and tended to be increased in WKY on sodium repletion, but remained unchanged on sodium depletion.4. It is suggested that extracellular fluid volume may be an important determinant factor of the natriuretic action of ANP but may not affect the hypotensive

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00920.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

SUMMARY1. The effects of adenosine, adenosine 5′‐triphosphate (ATP) and inosine on pancreatic exocrine secretion were investigated in the vascularly isolated and self‐hacmoperfused dog pancreas. Drugs were injected close‐arterially (i.a.) in a single bolus.2. These three purine‐related compoundsper sedid not affect resting rate of pancreatic secretion and the concentrations of protein and bicarbonate in the resting juice.3. Graded doses of adenosine (0.1–1.0 mg, i.a.) and ATP (0.1–1.0 mg, i.a.) administered 1 min prior to secretin (0.025 clinical units, i.a.) increased a secretin‐stimulated secretory volume dose‐dependently, and the effects of adenosine and ATP were reversed by pretreatments with theophylline (0.3 mg, i.a.).4. Insoine (1.0 mg, i.a.) affected neither secretin‐ nor dopamine‐stimulated (3 μg, i.a.) pancreatic secretion. Adenosine and ATP did not affect dopamine‐stimulated pancreatic secretion.5. These results suggest that adenosine and ATP (or terminal phosphate hydrolyzed derivatives) enhance secretin‐stimulated pancreatic exocrine secretion through ‘P1’ purine receptors in the exocrine cells,

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00921.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

SUMMARY1.d‐Tubocurarine (dTC) at an intravenous dose of 250 μg/kg, or at an intra‐arterial dose of 25 μg/kg, produced about a 50% block on the twitch tension of the indirectly stimulated tibialis anterior muscle of anaesthetized cats.2. ThedTC‐induced neuromuscular block was abolished if it was given intravenously but not intra‐arterially, 30 min after the commencement of sodium nitroprusside (SNP) infusion (5 μg/kg per min) when there was a maximum decrease in blood pressure.3. The results indicate that the biophase concentration ofdTC at the neuromuscular junction may be decreased as a consequence of the vasodilation induced by SNP leading to a reduced transport of the blocker to the site

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00922.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

SUMMARY1. Neuropeptide Y (NPY) is colocalised with noradrenaline in post‐ganglionic sympathetic neurons. In order to examine the possibility that activation of the sympathetic nervous system might cause release of NPY into the plasma NPY levels were measured in 16 patients undergoing exercise tests for investigation of chest pain.2. Plasma NPY concentrations rose in 14 out of the 16 patients, and the mean level of plasma NPY increased from 335 (s.e.m. = 37) to 455 (s.e.m. = 41) pg/ml.3. Plasma noradrenaline and adrenaline levels increased four‐ and two‐fold respectively.4. The increase in NPY correlated with the increase in noradrenaline, suggesting that NPY may be released with noradrenaline when sympathetic noradrenergic nerves are acti

ISSN:0305-1870    

DOI:10.1111/j.1440-1681.1986.tb00923.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY