Abstract:
:The binding of [3H]ketanserin and [125I]BE 2254 [( beta-(4-hydroxyphenyl)ethylaminomethyl]tetralone) was characterized in human brain cortex membranes. As observed in saturation experiments, [3H]ketanserin (a reportedly selective serotonin 5-HT2 ligand) and [125I]BE 2254 (a selective alpha 1-adrenergic antagonists) labeled, apparently, a homogeneous class of high-affinity recognition sites. Competition experiments performed with [125I]BE 2254 and a series of 20 structurally different compounds resulted in steep and monophasic competition curves. In contrast, competition curves of these compounds for [3H]ketanserin binding were often shallow or biphasic, suggesting a heterogeneity of the sites labeled by [3H]ketanserin. In particular, alpha-adrenoceptor-selective ligands (e.g., prazosin, BE 2254, WB 4101, phentolamine) showed clearly biphasic curves displacing about 20% of [3H]ketanserin binding with nanomolar affinity. On the other hand, cinanserin, a selective 5-HT2 antagonist, showed nanomolar affinity for 80% of the sites labeled by [3H]ketanserin, and micromolar affinity for the other 20%. There was a highly significant correlation between [125I]BE 2254 binding and the minor component of [3H]ketanserin in human brain cortex membranes (r = 0.910, p less than 0.0001, n = 20). The data show that [3H]ketanserin binds in the nanomolar concentration range (1.5-1.8 nM) to both 5-HT2 and alpha 1-adrenergic receptors. Similar results were obtained in rat and pig brain membranes. The data suggest that ketanserin possesses a rather limited degree of selectivity in human tissue.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Hoyer D,Vos P,Closse A,Palacios JM,Engel G,Davies Hsubject
Has Abstractpub_date
1987-01-01 00:00:00pages
S48-50eissn
0160-2446issn
1533-4023journal_volume
10 Suppl 3pub_type
杂志文章abstract::Carvedilol (20 mg/kg, bid) or vehicle was given to rats surviving a myocardial infarction (MI) 24 h (n = 409). In rats with large MI, carvedilol partially preserved left ventricular (LV) function and intrinsic myocardial contractility and reactivity to beta-adrenergic stimulation. Carvedilol led to scar thickening, in...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200201000-00009
更新日期:2002-01-01 00:00:00
abstract::In this study, we examined glyceryl trinitrate (GTN) biotransformation and cyclic GMP elevation in vascular smooth muscle before onset of GTN-induced relaxation. Isolated rabbit aortic strips (RAS) and strips of bovine pulmonary artery (BPA) and bovine pulmonary vein (BPV) were contracted submaximally and incubated wi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199005000-00005
更新日期:1990-05-01 00:00:00
abstract::Angiopeptin (AP: BIM23014C), a cyclic analogue of the peptide hormone somatostatin, inhibits intimal hyperplasia after balloon angioplasty. This inhibition has been attributed to a direct inhibitory effect on smooth muscle cell (SMC) proliferation. However, the SMC that proliferate in the intima and contribute to inti...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199504000-00015
更新日期:1995-04-01 00:00:00
abstract::The renin-angiotensin system affects blood pressure and regional blood flow through endocrine, paracrine, and autocrine influences. The circulating endocrine renin-angiotensin system (RAS) is activated for acute cardiovascular homeostasis. The recent demonstration of a local renin-angiotensin system in the blood vesse...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:
更新日期:1987-01-01 00:00:00
abstract::Reperfusion of ischemic myocardium is accompanied by intracellular Ca overload, leading to cardiac dysfunction. However, the mechanisms underlying intracellular Ca overload have yet to be fully elucidated. The mechanism may involve the activation of store-operated Ca entry, which is primarily mediated through the tran...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000566
更新日期:2018-04-01 00:00:00
abstract::Sixteen hypertensive patients received pindolol (10-45 mg/day); mean +/- SD, 28.75 +/- 15.22) for 3-8 weeks in a placebo-controlled, single-blind, crossover study. Supine and standing blood pressures (BP) were lowered, whereas effective renal plasma flow and glomerular filtration rates (estimated from the clearances o...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-198105000-00018
更新日期:1981-05-01 00:00:00
abstract::Heart failure after myocardial infarction (MI) is associated with endothelial dysfunction. There is conflicting evidence on the exact nature of this endothelial dysfunction and how endothelium-dependent vasodilation is affected by angiotensin-converting enzyme inhibitor (ACE-I) therapy. Furthermore, consequences of ac...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000187175.05780.e2
更新日期:2005-12-01 00:00:00
abstract::Several reports suggest the presence of sodium-potassium pump inhibitor in plasma and various tissues, particularly during volume-expanded state and low-renin hypertension. It has been hypothesized that by inhibiting the cardiovascular muscle-cell Na(+)-K+ pump, this inhibitor can constrict blood vessels, enhance vaso...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199322002-00005
更新日期:1993-01-01 00:00:00
abstract::Isolated Langendorff-perfused rat hearts set up to allow measurement of mechanical myocardial function (according to Bardenheuer and Schrader) were subjected to 60 min of global ischemia (gI). The hearts were perfused with a modified Krebs-Henseleit solution (KHS; control group) or KHS with desipramine (DMI group) 100...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198806121-00003
更新日期:1988-01-01 00:00:00
abstract::We compared the effect of verapamil slow-release (VSR) and the combination of nifedipine plus propranolol on transient myocardial ischemia in a double-blind study comprising 20 patients with proven coronary artery disease and chronic stable angina. According to the results of 24-h Holter-monitoring recording, patients...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00005344-199204000-00024
更新日期:1992-04-01 00:00:00
abstract::Vascular smooth muscle cells (SMCs) play a key role in the development of atherosclerotic lesions. Vascular smooth muscle, however, does not represent a homogeneous tissue. Using myosin as a marker of the differentiation processes in development and in vascular disease, we have been able to demonstrate the existence o...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-199219002-00004
更新日期:1992-01-01 00:00:00
abstract::Dihydropyridine calcium antagonists play an important role in the treatment of arterial hypertension. In many centers, they are used as first-line treatment. Since impaired renal function can be a complication of long-standing blood pressure elevation, the usefulness of dihydropyridine calcium antagonists in hypertens...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:
更新日期:1989-01-01 00:00:00
abstract::The calcium channel blocker nifedipine and the new phosphodiesterase (PDE) inhibitor enoximone are used in the treatment of cardiovascular diseases. Since both substances are acting on slow calcium channels and because systemic elimination of these two agents is dependent on oxidative drug metabolizing enzyme activity...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:
更新日期:1990-01-01 00:00:00
abstract::In view of recent findings on the anatomic heterogeneity of rapid vasodilation via estrogen receptor (ER)-dependent mechanisms, it is obvious that with regard to human physiology and disease much of it is still unknown, and research in this area is urgently needed. This is also important because chronic drug therapy w...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/FJC.0b013e31829709d4
更新日期:2013-07-01 00:00:00
abstract::Several mechanisms have been suggested for the absence of reflex tachycardia in response to the hypotensive effect of the selective alpha 1-adrenoceptor antagonist indoramin, including, in animals, membrane-stabilising activity, prolongation of repolarisation time, and reduction in baroreflex sensitivity. The present ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00005344-198803000-00004
更新日期:1988-03-01 00:00:00
abstract::Bromocriptine, a dopamine (DA) receptor agonist, has been reported to have hypotensive effects in anesthetized and conscious normotensive rats but its mechanism of action is still not fully understood. Therefore, we studied the changes in mean arterial blood pressure (MAP) and heart rate (HR) elicited by an intravenou...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199109000-00003
更新日期:1991-09-01 00:00:00
abstract::The effects of bufuralol and its carbinol metabolite have been compared with those of propranolol in the anaesthetised and conscious cat and dog. Bufuralol and its carbinol metabolite are nonselective beta-adrenoceptor antagonists; the former has equivalent potency to propranolol, whereas the latter is six times more ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1984-01-01 00:00:00
abstract::At present, endothelin (ET) receptor classification remains controversial. We investigated the presence of atypical ETA receptors in human saphenous veins (SV). Human SV was obtained from 24 patients undergoing coronary artery bypass grafting. Vessels were set up in organ baths, stretched to a tension of 6 g, and left...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199800001-00049
更新日期:1998-01-01 00:00:00
abstract::The effect of two calcium antagonists on left ventricular (LV) relaxation and diastolic filling was evaluated in 16 randomized patients. Isradipine and nifedipine were administered intravenously in a maximum dose of 60 micrograms/min for isradipine and 63 micrograms/min for nifedipine. Heart rate was increased signifi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:
更新日期:1990-01-01 00:00:00
abstract::We studied the hemodynamic effects of four doses of milrinone, administered by intravenous (i.v.) infusion alone and after autonomic blockade with prazosin, propranolol, atropine, and clonidine. Plasma concentrations of milrinone (50-600 ng/ml) were similar to those used for the treatment of cardiac failure and were u...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198705000-00002
更新日期:1987-05-01 00:00:00
abstract::The effect of atrial natriuretic peptide (ANP) on cytosolic free calcium ([Ca2+]i) was studied in monolayers of cultured vascular smooth muscle (VSM) cells loaded with a fluorescent calcium indicator, fura-2. ANP (atriopeptin III, 10(-8) M) decreased the resting level of [Ca2+]i and sustained rises in [Ca2+]i followin...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1989-01-01 00:00:00
abstract::An attempt was made to study possible interaction between neuromodulation by adenosine and nicotine stimulatory effects. Dose-effect curves were made double blind in 7 nonsmoking, nonsnuffing healthy volunteers (25-49 years) before and during exposition to nicotine roughly corresponding to the nicotine of one cigarett...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199012000-00015
更新日期:1990-12-01 00:00:00
abstract::The effects of olprinone (0.2 microg/kg per minute, i.v.) on cerebral blood flow were examined using technetium-99m-ethyl cysteinate dimer (99mTc-ECD) brain single-photon emission computed tomography in 14 stroke patients (69.0 +/- 5.6 years) and 12 normal subjects (68.1 +/- 6.2 years). The regional cerebral blood flo...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00005344-200104000-00004
更新日期:2001-04-01 00:00:00
abstract::Sinoaortic deafferentation (SAD) is characterized by arterial pressure lability, without sustained hypertension. Although SAD rats did not become hypertensive, their isolated aortas exhibit RCs. We have investigated whether these RCs are influenced by endothelium. Aortic rings were placed in an organ chamber, and the ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e31813c112f
更新日期:2007-11-01 00:00:00
abstract::Effects of FK409 were investigated in perfused guinea-pig Langendorff hearts subjected to ischemia and reperfusion. Nitric oxide electrode, fluorometry, and 31P nuclear magnetic resonance imaging were used to monitor changes in cellular high-phosphorous energy and nitric oxide and Ca2+ content in the heart together wi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200110000-00012
更新日期:2001-10-01 00:00:00
abstract::Hypertension, atherosclerosis, arteriosclerosis, and cardiomyopathy account for 80% of all diabetic deaths. A paucity of data exists concerning reactivity of the diabetic vasculature to vasopressor substances. The purpose of this investigation was to determine the influence of short-term (4-5 weeks) diabetes on the re...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198303000-00016
更新日期:1983-03-01 00:00:00
abstract::Endothelin-1 (ET-1) in the central nervous system has been suggested to produce suppressive effects on pain transmission. We investigated the manner by which ET-1 exerts this action. ET-1 administered intracerebroventricularly produced a dose-dependent antinociceptive effect in a thermal pain test that utilized a spin...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000166271.40044.0c
更新日期:2004-11-01 00:00:00
abstract::The antiarrhythmic efficacy and proarrhythmic potential of the class IC antiarrhythmic agent encainide were assessed in subacute and chronic postinfarction canine models, respectively. In conscious dogs with spontaneous premature ventricular complexes (PVCs) at 48 h after anterior myocardial infarction (MI), cumulativ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199303000-00008
更新日期:1993-03-01 00:00:00
abstract::Late sodium channel current (late INa) is considered to be an antiarrhythmic target. The prime antiarrhythmic mechanisms of late INa inhibition have been suggested to be (1) suppression of intracellular calcium [Cai]-mediated rhythmic activity (through reduction in Cai secondary to the decrease in intracellular sodium...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/FJC.0000000000000510
更新日期:2017-09-01 00:00:00
abstract::To investigate the effects of ramipril, a new angiotensin converting enzyme inhibitor, on autonomic function, autonomic function tests were performed in eight healthy male subjects, aged 22-26 years, after single oral administration of 5 mg of ramipril or placebo, in a randomized, double-blind, crossover design. Measu...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-198900133-00010
更新日期:1989-01-01 00:00:00