Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C1323099 (sympathomimetic)
 2,957 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Non-nucleated red blood cells from rats contain adenyl cyclase, the activity of which is predominantly localized in the reticulocytes. Basal enzyme activities in membrane preparations from reticulocyte-rich blood (pretreatment of rats with acetyl-phenylhydrazide: about 60% reticuloytes) are about 5 times higher than in preparations from reticulocyte-poor blood (untreated animals: 2-3% reticulocytes). The enzyme activities are stimulated 10-fold by sodium fluoride (10(-2)M) and 6 to 8-fold by isoprenaline (10(-4)M). Adenyl cyclase activities in membrane preparations from reticulocyte-rich and reticulocyte-poor blood can be ascribed to identical enzymes since identical apparent Km (ATP; 3 times 10(-4)M, Ka (isoprenaline; 3 times 10(-6)M) and Ki (propranolol vs. isoprenaline; 3 times 10(-7)M) values were obtained in both preparations. Besides NaF, only phenylethanolamine derivatives with beta-adrenergic receptor stimulant properties were effective as stimulators of adenyl cyclase activity. The affinities (apparent Ka values) of the investigated compounds decreased in the order isoprenaline--hexoprenaline--fenoterol--salbutamol--adrenaline--terbutalin--noradrenaline--phenylephrine. For maximal intrinsic activity, the catechol structure was essential; the relative intrinsic activities of resorcinol derivatives did not exceed 0.6. The isoprenaline-stimulated adenyl cyclase activities in erythrocyte membrane preparations were competitively inhibited by beta-adrenergic blocking drugs, the affinities (apparent Ki values) decreasing in the order prindolol--penbutolol--propranolol--practolol. The dextrorotatory enantiomers of penbutolol and propranolol were 1/100 to 1/200 as active as the resp. levorotatory enantiomers. From experiments with alpha-adrenergic agonists (e.g. phenylephrine) and antagonists (e.g. phentolamine), it is concluded that alpha-adrenergic receptors do not interfere with the beta-adrenergically-mediated cAMP formation in these particular membranes. A variety of hormones and drugs known to stimulate denyl cyclase activities in various tissues, e. g. ACTH, glucagon, STH, erythropoietin, prostaglandin E1 etc. did not affect adenyl cyclase activity in reticulocyte-rich erythrocyte membrane preparations. In contrast to adenyl cyclase activity, phosphodiesterase activities in erythrocyte membrane and cytoplasmic fractions were only twice as high in reticulocyte-rich as in reticulocyte-poor preparations. From the experiments described, it is obvious that the adenyl cyclase of the rat reticulocyte is subject to monovalent-hormonal, i.e. beta-sympathomimetic stimulation. Moreover, the premature red blood cell provides a useful model for quantitative studies of the interaction of drugs with the beta-adrenergic receptor.
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PMID:The beta-adrenergic receptor-adenyl-cyclase system of rat reticulocytes: effects of adrenergic stimulants and inhibitors. 24 Jan 35

The renin-angiotensin system consists of two main enzymes, renin and angiotensin-converting enzyme, which lead to the formation of angiotensin-II. Angiotensin-II is a potent vasoconstrictor and stimulates the production of aldosterone. In this study we examined the effect of ACTH, potassium, (Bu)2cAMP (dbcAMP), and catecholamines on the adrenal renin-angiotensin system. To study the production of renin and aldosterone in vitro, we developed a monolayer culture of bovine zona glomerulosa cells in serum-free medium. Collagenase-dispersed zona glomerulosa cells were incubated in Pasadena Foundation for Medical Research-4 medium containing 10% fetal calf serum for 72 h, and the medium was replaced with serum-free medium for the next 24 h of the experimental period. The cells during this 24 h were exposed to various doses of ACTH, potassium, dbcAMP, and sympathomimetic agents. ACTH and dbcAMP stimulated aldosterone secretion, and this secretion was associated with an increase in renin activity in cells and medium. Aldosterone was also stimulated by high doses of potassium, and potassium had a stimulatory effect on the secretion of renin in medium. Catecholamines had a weak stimulating effect on aldosterone secretion and were potent stimulators of adrenal renin activity in cells and medium. Dopamine had no significant effect on basal aldosterone secretion or renin activity in cells and medium. In conclusion, these data indicate that adrenal renin is synthesized in bovine zona glomerulosa cells in vitro, and that ACTH and dbcAMP stimulate adrenal renin and aldosterone production. Furthermore, adrenal renin, like renal renin, may be under the control of the sympathetic nervous system.
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PMID:Regulation of the adrenal renin angiotensin system in cultured bovine zona glomerulosa cells: effect of catecholamines. 131 45

1 The effects of oral doses of pindolol (15 mg), metoprolol (200 mg) and propranolol (160 mg) on the response to insulin-induced hypoglycaemia and an oral glucose load were investigated. 2 Serum insulin and serum C-peptide secretion in response to a glucose load were inhibited (2P less than 0.01) by metoprolol and propranolol but not by pindolol. 3 During hypoglycaemia metoprolol and propranolol inhibited the clearance of insulin (2P less than 0.01) and caused a delay of glucose nadirs. 4 Adrenaline secretion during hypoglycaemia was markedly increased by metoprolol and propranolol but not by pindolol. 5 The counterregulatory response of growth hormone, ACTH and cortisol was increased following metoprolol and propranolol but not after pindolol. 6 The hypoglycaemic symptoms and signs showed a prevalence of sweating and prolonged changes in skin conductivity whereas palpitations were not observed during beta-adrenoceptor blockade. Asymptomatic hypoglycaemia did not occur. 7 The absence of unphysiological rises in adrenaline, growth hormone, ACTH and cortisol supports the use of a beta-adrenoceptor blocker with intrinsic sympathomimetic activity.
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PMID:The influence of beta-adrenoceptor blocking drugs with and without intrinsic sympathomimetic activity on the hormonal responses to hypo- and hyperglycaemia. 612 93

In 28 children undergoing adenoidectomy, plasma concentrations of catecholamines, ACTH and cortisol were measured. Fourteen children were anaesthetized with halothane (seven non-intubated, seven intubated) and 14 with enflurane (seven non-intubated, seven intubated). During undisturbed anaesthesia, plasma catecholamines were significantly higher with halothane than with enflurane (P less than 0.05). Immediately after surgery, catecholamines were increased up to 300% in the halothane groups. In the enflurane groups, however, the catecholamine concentrations remained unchanged. This difference between the two agents, after surgery, was statistically significant (P less than 0.01 for intubated and P less than 0.001 for non-intubated children). Fifteen minutes postoperatively no difference was found in plasma concentrations between the groups. In all four groups, plasma concentrations of ACTH and cortisol increased similarly during the procedure. It was concluded that plasma catecholamines were higher during halothane than during enflurane anaesthesia in children undergoing adenoidectomy. This difference may be caused by a stimulating effect of halothane on the endogenous catecholamine release. This increased sympathomimetic response during halothane anaesthesia was correlated to the incidence of ventricular arrhythmias previously found with this agent during adenoidectomy.
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PMID:Catecholamine and endocrine response in children during halothane and enflurane anaesthesia for adenoidectomy. 632 22

In this prospective, randomized study, two regimens of total intravenous anaesthesia (TIVA), with propofol and S(+)-ketamine (S-ketamine) and with propofol and alfentanil, were compared with reference to endocrine stress response, circulatory effects and recovery. METHODS. The investigation was conducted in two groups of 20 ASA I-III patients over 60 years of age who were scheduled for endoprothetic orthopaedic surgery. After oral premedication with midazolam, patients received a TIVA with body-weight-adjusted doses of propofol, and S-ketamine or alfentanil as the analgesic component. For CPPV (PEEP 5 mbar), air and oxygen (FiO2 33%) were used. For muscle relaxation, patients of both groups received vecuronium in body-weight-adjusted doses. Blood samples were taken through a central venous line at seven time points before induction of anaesthesia and on the first morning after the operation also for analysis of epinephrine, norepinephrine (by HPLC/ECD), and ADH, ACTH and cortisol (by RIA). In addition, SAP, HR, arterial oxygen saturation, recovery from anaesthesia and side effects were observed. RESULTS. The two groups had comparable group mean values for age (S-ketamine group 71 years, alfentanil-group 70 years), other biometric data, and duration of anaesthesia and operation (Table 1). Plasma levels of epinephrine, norepinephrine (Table 2, Fig. 1), ADH (Table 2, Fig. 2) ACTH and cortisol (Table 2, Fig. 3) were higher in the S-ketamine-group (P < 0.05) owing to the intraoperative course of these endocrine parameters. Before induction, and on the first morning after the operation, levels were comparable between the groups. 5 min after the induction of anaesthesia, SAP and HR (Table 3) were significantly lower in the alfentanilgroup (P = 0.001). Recovery from anaesthesia (orientation with respect to person and location) was faster in the alfentanilgroup (16 vs 39 min, P = 0.001). An arterial oxygen saturation below 90% was observed in 7 patients in the S-ketamine- and 13 patients in the alfentanilgroup (P = 0.03). Four patients with S-ketamine reported dreams, and 1 dream was judged negative. Postoperative emesis was found in 6 patients in the S-ketaminegroup and 12 patients in the alfentanilgroup (P = 0.03). All patients said they would agree to undergo the same anaesthetic technique again. CONCLUSIONS. Considerable differences were found in the endocrine stress response of the two groups. With respect to endocrine response and circulation, TIVA with propofol and S-ketamine had sympathomimetic properties with positive circulatory effects and led to moderate endocrine stimulation. This should be kept in mind in patients with hypotension, hypothyrosis, or adrenocortical insufficiency; because "eustress" might be beneficial in this group of patients. On the other hand, TIVA with propofol and alfentanil showed sympatholytic properties, with negative circulatory effects and a remarkable reduction of endocrine stress response. This might be beneficial in patients with hypertension and states of endocrine hyperfunction. Both regimens were accompanied by such typical side effects as dreams, delayed recovery, reduced ventilation, and emesis, which should also be considered.
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PMID:[Total intravenous anesthesia (TIVA) in geriatric surgery. S-(+)-ketamine versus alfentanil]. 859 65