Drugs online research references
Br J Pharmacol. 1993 Oct;110(2):603-8.
Competitive inhibition by procaine of carbachol-induced stimulus-secretion coupling in rat pancreatic acini.
Ikei N, Busik J, Habara Y, Kanno T.
Otsuka Assay Laboratories, Otsuka Pharmaceutical Co., Tokushima, Japan.
1. Procaine (0.03-10 mM) inhibited carbachol (CCh)-induced amylase release from rat isolated pancreatic acini in a competitive manner. Kinetic analysis of the relation between CCh concentrations and the amount of amylase released in the presence of various procaine concentrations indicated that procaine caused competitive inhibition with the affinity constant (pA2) value of 5.00 +/- 0.08. 2. Receptor binding assay confirmed that procaine (0.01-10 mM) competitively inhibited [N-methyl-3H]-scopolamine chloride ([3H]-NMS) binding to its receptor with binding affinity (pKi) of 4.63 +/- 0.10. 3. Procaine transformed CCh-evoked [Ca2+]i dynamics: the initial rise in [Ca2+]i followed by a gradual decay during continuous stimulation with 3 microM CCh was transformed by 0.3 mM procaine to the oscillatory [Ca2+]i dynamics, which resembled the response to 0.3 microM CCh in the absence of procaine. The initial phase of [Ca2+]i oscillation corresponded to the initial phase of CCh-induced amylase release in isolated perfused acini. 4. Procaine (0.3-3 mM) did not inhibit the secretory response to cholecystokinin octapeptide (CCK-8) in isolated incubated acini. A higher concentration of procaine (10 mM) caused weak but significant inhibition of the response to only limited concentrations of CCK-8, 30 and 100 pM. Procaine lower than 10 mM was ineffective on [125I]-BH-CCK-8 binding, although procaine (10 mM) caused weak but significant inhibition of the binding.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7694753&dopt=Abstract
Eur J Pharmacol. 1988 Mar 29;148(2):269-72.
Scopolamine modulates apomorphine-induced behavior in rats treated with haloperidol or SCH 23390.
Butkerait P, Friedman E.
Department of Psychiatry, Medical College of Pennsylvania/EPPI, Philadelphia 19129.
In acute experiments, scopolamine (1.0 mg/kg) potentiated apomorphine stereotypy and inhibited the antistereotypic effect of both haloperidol (0.5 mg/kg) and SCH 23390 (0.2 mg/kg). Daily administration of either haloperidol (0.5 mg/kg) or SCH 23390 (0.2 mg/kg) for 3 weeks produced enhanced stereotypic responses to apomorphine. Co-administration of scopolamine (1.0 mg/kg) with haloperidol or SCH 23390 significantly reduced the behavioral supersensitivity produced by haloperidol or SCH 23390 alone. It is suggested that both D-1 and D-2 dopamine receptors are linked to a cholinergic mechanism.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2897925&dopt=Abstract
Minerva Anestesiol. 1991 Jul-Aug;57(7-8):399-412.
[Hemodynamic effects of propofol in patients undergoing pulmonary excision and in patients undergoing closed heart mitral valve surgery]
[Article in Italian]
Merli M, Amari B, Ferrante M, Gagliardone MP, Milazzo F, Oppizzi M, Paino R, Cattani C.
Centro A. De Gasperis, III Servizio di Anestesia e Rianimazione, Ospedale Maggiore Niguarda Ca' Granda, Milano.
The effects of propofol on cardiovascular dynamics were studied, by means of SO2 Swan-Ganz catheter, in 12 patients scheduled for elective pulmonary resection and in 10 patients undergoing closed heart mitral valve commissurotomy. Myocardial contractility was also investigated in 10 patients (5 pulmonary and 5 mitral valve patients) by means of transthoracic echocardiography. The patients were premedicated with morphine (0.1 mg/kg i.m.), scopolamine (0.005 mg/kg i.m.) and diazepam (0.1 mg/kg p.o.). Anaesthesia was induced with propofol (2 mg/kg i.v.) and fentanyl (0.005 mg/kg i.v.) and maintained with propofol (6 mg/kg/h) plus fentanyl (0.005 mg/kg/h) infusion. Muscle relaxation was assured by pancuronium bromide (0.1 mg/kg). Ventilation (O2-N2O 50%) was controlled to maintain ETCO2 between 30 and 40 mmHg. All the patients undergoing pulmonary resection were intubated with double lumen endotracheal tube. Measurements were performed with the patients awake, after induction, during steady state anaesthesia, before and after thoracotomy. Propofol together with fentanyl significantly decreased arterial pressure (more than 35%) and cardiac index (more than 40%) in both groups of patients; heart rate showed no significant changes even after intubation. Right atrial pressure didn't change meanwhile wedge pressure showed a reduction, with statistical significance only in pulmonary patients. Total systemic resistances didn't show any variation in both groups of patients. The echocardiographic data revealed an important impairment of myocardial contractility after bolus of propofol, mainly in cardiac patients, as evidenced by decrease of ejection fraction values (20%) and by increase of left ventricle end systolic volume index (10%) from baseline. SVO2 and DO2/VO2 ratio values were stable, according with deep anaesthesia level and adequate metabolic balance. In pulmonary patients, during one lung ventilation, the intrapulmonary shunt values did not differed either during or without propofol infusion, thus suggesting that propofol doesn't interfere with pulmonary hypoxic vasoconstrictor response. In conclusion an aware use of propofol and a careful haemodynamic monitoring would be advisable primarily in patients with a well known or supposed cardiovascular disease.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1944963&dopt=Abstract
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