Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.4.16.2 (PCP)
 3,761 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

To characterize the relation between clinical and hemodynamic state in acute myocardial infarction, 200 patients with acute infarction were evaluated with clinical and hemodynamic criteria. Patients were classified clinically on the basis of peripheral hypoperfusion (hypotension, tachycardia, confusion, cyanosis, oliguria) and pulmonary congestion (rales, abnormal chest roentgenogram). Four clinical subsets were defined that correlated with cardiac index (Cl, liters/min per m2) and pulmonary capillary pressure (PCP, mm Hg): (see article). Parallel hemodynamic subsets were developed independently on the basis of depressed cardiac index (2.2 liters/min per m2 or less) and elevated pulmonary capillary pressure (greater than 18 mm Hg). The rate of accuracy of clinical examination in predicting hemodynamic abnormalities was 83 percent. Mortality rates were similar in the clinical and hemodynamic subset calssifications, averaging 2.2 percent in subset I, 10.1 percent in subset II, 22.4 percent in subset III and 55.5 percent in subset IV. Drug interventions in the course of hospitalization resulted in a 38 percent increase in depressed cardiac index and 34 percent decrease in elevated pulmonary capillary pressure. Resolution of clinical abnormalities paralleled this hemodynamic improvement in 70 percent of patients. These data suggest that clinical performance and both clinical and hemodynamic subsets are directly relevant to establishing prognosis and the selection of therapy in patients with acute myocardial infarction.
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PMID:Correlative classification of clinical and hemodynamic function after acute myocardial infarction. 83 73

Intravenous nitroglycerin therapy during acute myocardial infarction has beneficial effects on infarct size, infarct complications, and mortality. Numerous dosage formulas for the continuous administration of nitrates are currently used, although several studies have demonstrated the rapid development of tolerance during long-term treatment in patients with ischemic heart disease. The dose and dosage of a continuous nitrate application in the clinical setting of acute myocardial infarction has thus yet to be resolved. This study investigated the hemodynamic effects of a 60-h, low- (33 micrograms/min) vs high- (133 micrograms/min) dose intravenous nitroglycerin (NTG) infusion in 16 patients with uncomplicated acute myocardial infarction. In group I (33 micrograms/min NTG; n = 8) the initial nitrate effect on the pulmonary capillary pressure (PCP-control: 14 +/- 1.5; 4 h: 7 +/- 0.9; 60 h: 7 +/- 0.8; mean +/- SEM; all values in mm Hg) and mean pulmonary artery pressure (PAPM-control: 23 +/- 2.3; 4 h: 15 +/- 1.3; 60 h: 14 +/- 1.3) remained unchanged for 60 h. In group II (133 micrograms/min NTG; n = 8) an almost complete loss of the initial effect on PCP (control: 15 +/- 1.6; 4 h: 5 +/- 1.4; 60 h: 12 +/- 1.3) and PAPM (control: 25 +/- 2.0; 4 h: 14 +/- 1.8; 60 h: 20 +/- 1.3) was observed. In contrast to high-dose application the low-dose NTG-infusion induced comparable acute hemodynamic effects that were not attenuated by tolerance development.
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PMID:[Dose and time dependence of hemodynamic tolerance development during intravenous nitrate therapy in acute myocardial infarct]. 190 22

The synthesis and in vitro sigma receptor activity of the two diastereomers of U50,488 [(+/-)-2], namely, (1R,2S)-(+)- cis-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacet ami de [(+)-1] and (1S,2R)-(-)-cis-3,4-dichloro- N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide [(-)-1], are described. (+)-1 and (-)-1 were synthesized from (+/-)-trans-N-methyl-2-aminocyclohexanol [(+/-)-3]. Pyridinium chlorochromate (PCC) oxidation of the N-t-Boc-protected derivative of (+/-)-3 afforded (+/-)-2-[N- [(tert-butyloxy)carbonyl]-N-methylamino]cyclohexanone [(+/-)-5]. The sequence of enamine formation with pyrrolidine, catalytic reduction, N-deprotection, and optical resolution afforded (1R,2S)-(-)-cis-2-pyrrolidinyl-N-methylcyclohexylamine [(-)-10] and (1S,2R)-(+)-cis-2-pyrrolidinyl-N-methylcyclohexylamine [(+)-10]. The optical purity (greater than 99.5%) of (-)-10 and (+)-10 was determined by HPLC analysis of the diastereomeric ureas formed by reaction with optically pure (R)-alpha-methylbenzyl isocyanate. The absolute configuration of (-)-10 and (+)-10 was determined by single-crystal X-ray diffractometry of the bis-(R)-mandelate salt. Condensation of optically pure (-)-10 and (+)-10 with 3,4-dichlorophenylacetic acid furnished (+)-1 and (-)-1, respectively. Compounds (+)-1, (-)-1, (-)-2, and (+)-2 were compared for their binding affinities at kappa opioid, sigma, D2-dopamine, and phencyclidine (PCP) receptors in competitive binding assays using [3H]bremazocine ([3H]BREM) or [3H]U69,593, [3H]-(+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine [[3H]-(+)-3-PPP], or [3H]-1,3-di(o-tolyl)guanidine ([3H]DTG), [3H]-(-)-sulpiride [[3H]-(-)SULP], and [3H]-1- [1-(2-thienyl)cyclohexyl]piperidine ([3H]TCP), respectively. In the systems examined, (-)-2 exhibited the highest affinity for kappa receptors, with a Ki of 44 +/- 8 nM. However, (-)-2 also showed moderate affinity for sigma receptors, with a Ki of 594 +/- 3 nM [[3H]-(+)-3-PPP]. The (1R,2R)-(+)-enantiomer, (+)-2, had low affinity for both kappa and sigma receptors, exhibiting Ki values of 1298 +/- 49 nM at kappa ([3H]BREM) and 1270 +/- 168 nM at sigma [[3H]-(+)-3-PPP]. In contrast, the chiral cis compounds (+)-1 and (-)-1 showed high affinity for sigma receptors and negligible affinity for kappa opioid receptors in the [3H]BREM assay. Compound (-)-1 exhibited a Ki of 81 +/- 13 nM at sigma receptors [[3H]-(+)-3-PPP] and 250 +/- 8 nM ([3H]DTG).(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. 254 74

Haemodynamic monitoring, using a Swan-Ganz balloon catheter, was done in 14 patients with pump failure associated with acute myocardial infarction, before and for 8 h after single 6 mg oral dose of molsidomine. The following changes effects were found: HR fell by 1.6 to 4.7% (significant at 4th hour; p less than 0.05); SBP was 8.4% lower after 1 h (p less than 0.05); PCP was decreased by approximately 30%, a significant effect that lasted for 8 hours (p less than 0.002). CI did not change significantly, although individual analysis showed it to have increased in 6 out of 12 cases. Stroke volume index was increased by about 6% (significant after 1 h, p less than 0.025). The left ventricular stroke work index also increased from 9.8 to 24.5% (significant after 1 and 4 h, p less than 0.01 and 0.025). These findings show the beneficial haemodynamic effects of molsidomine in pump failure complicating acute myocardial infarction.
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PMID:Haemodynamic effects of oral molsidomine in pump failure complicating myocardial infarction. 654 66

The unloading mechanisms and side of peripheral action of the new antianginal drug molsidomine was compared with isosorbide dinitrate (ISDN) in 14 patients with acute myocardial infarction using a Swan-Ganz catheter and venous occlusion plethysmography. Sublingual molsidomine (2-4 mg) increased calf venous capacitance (CVC) (0.42 +/- 0.18 to 0.64 +/- 0.09 ml/100 ml, p less than 0.05) from 30 to 240 minutes, while simultaneously lowering of PCWP (25.9 +/- 4.9 to 15.8 +/- 7.3 mmHg, p less than 0.05) and CVP (9.3 +/- 3.7 to 5.8 +/- 3.5 cmH2O, p less than 0.05). Calf blood flow (CBF), calf vascular resistance (CVR), CI, TSPR and SWI were not affected significantly. Molsidomine reduced preload more than 240 minutes after its administration. Sublingual ISDN increased CBF into the initial 15 minutes (1.19 +/- 0.49 to 1.83 +/- 0.98 ml/100ml/min, p less than 0.05) and CVC from 5 to 60 minutes (0.42 +/- 0.19 to 0.68 +/- 0.24 ml/100ml p less than 0.01) while simultaneously lowering PCWP (24.3 +/- 2.2 to 14.6 +/- 4.5 mmHg, p less than 0.01) and CVP (9.0 +/- 2.8 to 5.5 +/- 3.5 cmH2O, p less than 0.05). Neither drug affected cardiac index, blood pressure or systemic vascular resistance. These data suggest that molsidomine significantly lowered elevated preload (PCWP/PCP) by dilating venous capacitance vessels. Its length of action was 240 minutes compared with 60 minutes obtained with ISDN, which suggests this new agent may be of marked benefit in the AMI patients suffering from backward failure uncomplicated by forward failure in whom continued preload reduction is necessary. (Results are expressed as the mean +/- standard deviation).
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PMID:Unloading effects of molsidomine on peripheral circulation and cardiac hemodynamics in patients with acute myocardial infarction. 668 6

The rise in serum myoglobin (MGB), total CPK (CKT) and its MB isoenzyme (CK - MB) was studied and compared over the first three days of acute myocardial infarction (AMI) and correlations were sought between the peak values of these three parameters and haemodynamic and biological indices of left ventricular function. Blood was taken from MGB (radio immunological technique), CKT and CK - MB (spectrophotometry) estimation every 2 hours for 24 hours and then every 6 hours up to the 72nd hour in 36 patients with AMI less than 12 hours old. On admission, this protocol was completed by a haemodynamic study (right heart pressures, systemic blood pressure, cardiac output measurement by thermodilution), arterial gases and ECG recordings. The average delays before the pathological rise, the maximal peak value and the return to normal were significantly shorter (p less than 0.001) for MGB (2, 6 and 25 hours) than for CK - MB (5,16 and 34 hours) or CKT (5,21 and 57 hours). The sensitivity of the diagnosis of myocardial infarction was not significantly higher with MGB than CKT or CK - MB either in the whole group (sensitivity of 91.6 p. 100 for MGB and 86.1 p. 100 for CKT and CK - MB) or in a subgroup of ten patients without transmural infarction (70 p. 100 for MGB compared with 60 p. 100 for CKT and CK - MB). A significant correlation was found between the peak values of MGB (p less than 0.02) and CK- MB (p less than 0.02) and the indices of left ventricular function (PCP, PAO2 and LVSWI). This was not observed with CKT. In conclusion, apart form technical problems which remain unresolved time-consuming investigation), serum MGB gives a much earlier and as sensitive a biochemical diagnosis of AMI as CKT and CK - MB. MGB and CK - MB are much better prognostic indicators than CKT as judged by the indices of left ventricular function. Finally, MGB estimation should be of particular value in the diagnosis of secondary extension of infarction.
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PMID:[Value of serum myoglobin in acute myocardial infarction. Kinetic study]. 679 24

Haemodynamic and echocardiographic studies of isosorbide dinitrate were conducted in 12 patients (8 men and 4 women) with left ventricular failure consecutive to recent myocardial infarction. The groups: group I received 5 mg/h and group II 10 mg/h Risordan intravenously. After one hour treatment, group I patients showed a significant fall in both PAP (from 32.3 +/- 5.3 to 26.7 +/- 6.9 mmHg; p less than 0.01) and PCP (from 21.8 +/- 4.7 to 17.3 +/- 7.7 mmHg; p less than 0.05). These haemodynamic changes were amplified after a second hour of treatment: PAP fell to 24 +/- 7.9 mmHg (p less than 0.01) and PCP to 14.2 +/- 4.4 mmHg (p less than 0.001). RAP decreased from 7.2 +/- 5.1 to 3.5 +/- 5 (p less than 0.05). There were no changes in heart rate, systemic arterial pressure, peripheral resistance, cardiac index, forward stroke work nor, on echocardiography, in ventricular diameters, shortening fraction and VCF. After one hour treatment, group II patients showed a fall in PAP (from 30.5 +/- 4.7 to 21.7 +/- 3.5 mmHg; p less than 0.01), PCP (from 21.7 +/- 4.8 to 14.8 +/- 4.9 mmHg: p less than 0.001) and RAP (from 10.3 +/- 2.9 to 7.2 +/- 2; p less than 0.01). The systolic diameter of the left ventricle was reduced from 66.3 +/- 10.6 to 64.3 +/- 11.3 (p less than 0.01). After 4 hours, improvement in PAP and PCP was maintained; the other values remained stable. The effectiveness of Risordan i.v. in left ventricular failure consecutive to acute myocardial infarction is due to reduction of filling pressures in the left ventricule. With the 10 mg/h dose, as opposed to the 5 mg/h dose, the systemic arterial pressure and the double and triple products tend to be reduced, which suggests greater effectiveness.
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PMID:[Use of isosorbide dinitrate (Risordan) injection in left ventricular failure following acute myocardial infarction (author's transl)]. 711 Sep 69

To test the sensitivity and specificity of hemodynamic criteria for acute right ventricular infarction (RVI), two groups of patients with anatomically proved acute myocardial infarction and hemodynamic monitoring were studied. Group A included 22 patients acute RVI and group B, 38 with infarction confined to the left ventricle. In both groups, the closest relation between right atrial and pulmonary capillary pressures (RAP and PCP), as well as the presence of a severe noncompliant pattern (SNCP), were studied. A SNCP was defined as a y descent deeper than the x descent in RAP. RAP was equal to or higher than PCP in 10 patients from group A and in none from group B. In group B, a significant relation was found between RAP and PCP (r = 0.777, y = 0.43x + 0.18) (p less than 0.05), and the 95% confidence limits could be calculated. Above these limits, a closer relation between RAP and PCP was only found in patients with RVI. However, six patients with RVI showed an RAP/PCP relation within 95% confidence limits of group B (sensitivity 72.7%, specificity 100%). A SNCP was present in 12 patients with RVI and only in one without RVI (p less than 0.01) (sensitivity 54.5% and specificity 97.4%). When either criterion is present (close relation between RAP and PCP or SNCP), a high sensitivity (81.8%) and specificity (97.4%) can be achieved in the diagnosis of acute RVI.
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PMID:Sensitivity and specificity of hemodynamic criteria in the diagnosis of acute right ventricular infarction. 726 Dec 84