Pharmacological characterization of PABSA, an orally active and highly potent endothelin-receptor antagonist.

abstract：:The clinical activity of metformin (N,N-dimethyl biguanide), a widely used antidiabetic agent, on arterial blood flow was evaluated in 15 patients with peripheral atherosclerosis. Flow was determined by quantitative strain-gauge plethysmography; plasma lipid, lipoprotein, and apoprotein levels were repeatedly tested d...

journal_title：Journal of cardiovascular pharmacology

authors： Sirtori CR,Franceschini G,Gianfranceschi G,Sirtori M,Montanari G,Bosisio E,Mantero E,Bondioli A

更新日期：1984-09-01 00:00:00

abstract：:To investigate the role of endothelin (ET) in severe hypertension, endothelial dysfunction hypercholesterolemic stroke-prone spontaneously hypertensive rats (SHRSP on a 5% cholesterol diet) were additionally fed with 1% NaCl and 0.023% nitro-L-arginine. Under these conditions, all untreated rats died within 30 days (m...

journal_title：Journal of cardiovascular pharmacology

authors： Münter K,Hergenröder S,Kirchengast M

更新日期：1998-01-01 00:00:00

abstract：:Development of tolerance to nicorandil (NCR), N-(2-hydroxyethyl)nicotinamide nitrate (ester), was compared with that to nitroglycerin (NTG) or isosorbide dinitrate (ISDN) in dogs. An intracoronary arterial (i.a.) injection of NCR (20 micrograms), ISDN (30 micrograms), or NTG (1 microgram) caused coronary vasodilation....

journal_title：Journal of cardiovascular pharmacology

authors： Sakai K,Kuromaru O

更新日期：1987-01-01 00:00:00

abstract：:Intracellular [Ca2+]i overloading in cardiomyocytes is a fundamental pathogenic event associated with chronic aldosterone/salt treatment (ALDOST) and accounts for an induction of oxidative stress that leads to necrotic cell death and consequent myocardial scarring. This prooxidant response to Ca2+ overloading in cardi...

journal_title：Journal of cardiovascular pharmacology

authors： Kamalov G,Ahokas RA,Zhao W,Zhao T,Shahbaz AU,Johnson PL,Bhattacharya SK,Sun Y,Gerling IC,Weber KT

更新日期：2010-03-01 00:00:00

abstract：:The complementary antihypertensive effects of the beta-blocker/calcium antagonist combination has to be weighed against their additive and potentially detrimental negative inotropic, chronotropic, and dromotropic effects inherent in both classes of drugs. We reviewed the main adversity, particularly electrophysiologic...

journal_title：Journal of cardiovascular pharmacology

authors： Brouwer RM,Follath F,Bühler FR

更新日期：1985-01-01 00:00:00

abstract：:The antihypertensive efficacy of the calcium entry blocker nitrendipine administered as monotherapy (20-80 mg; mean, 36/day) on the average for 144 days to 46 patients with essential hypertension (WHO I and II) was investigated in relation to age, pretreatment blood pressure, and plasma renin activity. In addition, we...

journal_title：Journal of cardiovascular pharmacology

authors： Müller FB,Bolli P,Erne P,Block LH,Kiowski W,Bühler FR

更新日期：1984-01-01 00:00:00

abstract：:No single pathophysiologic mechanism explains adequately cold-induced vasospasm in all forms of Raynaud's phenomenon. Local serotonin release from activated platelets is a contributory element in those disorders typified by structural arterial change, e.g., systemic sclerosis (scleroderma). Selective antagonism of S2-...

journal_title：Journal of cardiovascular pharmacology

authors： Seibold JR

更新日期：1985-01-01 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

authors： Blaber LC,Burden DT,Eigenmann R,Gerold M

更新日期：1984-01-01 00:00:00

abstract：:Using selective endothelin (ET) receptor antagonists, we investigated which ET receptor subtypes mediate the changes in blood pressure and hematocrit produced by intraarterial injection of ET-1 in the anesthetized rabbit. In addition, the receptor through which ET-1 stimulates the release of prostacyclin (PGI2) and, h...

journal_title：Journal of cardiovascular pharmacology

authors： McMurdo L,Lidbury PS,Corder R,Thiemermann C,Vane JR

更新日期：1993-01-01 00:00:00

abstract：:The effects of the calcium channel blocker, diltiazem hydrochloride (DZ), on conscious, resting spontaneously hypertensive rats (SHR) were evaluated and compared with results from parallel studies on Wistar-Kyoto (WKY) controls. DZ was administered as a continuous, cumulative infusion at rates equal to 0.40, 2.00, and...

journal_title：Journal of cardiovascular pharmacology

authors： Flaim SF,Newman ED,Annibali JA

更新日期：1986-03-01 00:00:00

abstract：:Kinins locally synthesized in the cardiovascular tissue are believed to contribute to the regulation of cardiovascular homeostasis by stimulating the endothelial cells to release nitric oxide, prostacyclin, or a hyperpolarizing factor via autocrine-paracrine mechanisms. This study was designed to investigate the actio...

journal_title：Journal of cardiovascular pharmacology

authors： Kanna T,Akata T,Izumi K,Nakashima M,Yonemitsu Y,Hashizume M,Takahashi S

更新日期：2002-11-01 00:00:00

abstract：:Calcium-entry blockers were administered in an attempt to protect myocardium during cardiac arrest due to ventricular fibrillation in mechanically ventilated dogs. An intravenous injection of verapamil, nifedipine, or lidoflazine was administered prior to successively prolonged episodes of ventricular fibrillation, du...

journal_title：Journal of cardiovascular pharmacology

authors： Vincent JL,Goldstein J,Dufaye P,Domb M

更新日期：1984-11-01 00:00:00

abstract：:Early studies in experimental animals and in humans indicated the need to examine the feasibility of infarct size reduction by the early treatment of patients recruited to well-designed clinical trials. The extensive experience with beta-adrenoceptor blockers and the comparatively recent data generated with the use of...

journal_title：Journal of cardiovascular pharmacology

authors： Fitzsimons TJ

更新日期：1989-01-01 00:00:00

abstract：:Endogenous as well as synthetic cannabinoids have potent vasodilatory actions in a variety of vascular preparations. Their precise mechanism of action is as yet unclear, but several studies point to the activation of type 1 vanilloid (TRPV1) receptors on primary afferent perivascular nerves, stimulating the release of...

journal_title：Journal of cardiovascular pharmacology

authors： Breyne J,Vanheel B

更新日期：2006-02-01 00:00:00

abstract：:Hyperhomocysteinemia is a risk factor for atherosclerosis, and is found in the heterozygous form in approximately one-third of all individuals with coronary artery disease. The sulfhydryl group of homocysteine has been viewed as contributing to the atherogenic effects of this low-molecular-weight thiol, largely as a c...

journal_title：Journal of cardiovascular pharmacology

authors： Stamler JS,Loscalzo J

更新日期：1992-01-01 00:00:00

abstract：:The effects of bPTH-(1-34), a synthetic preparation of bovine parathyroid hormone containing the first 34 amino acids, on electromechanical activity of isolated rabbit sinus node cells and guinea pig papillary muscles were examined by microelectrode techniques. In sinus node cells, bPTH-(1-34) (10(-7) M) decreased the...

journal_title：Journal of cardiovascular pharmacology

authors： Kondo N,Shibata S,Tenner TE Jr,Pang PK

更新日期：1988-05-01 00:00:00

abstract：:Hibernating myocardium is characterized by chronic reduction of myocardial blood flow due to obstructive coronary artery disease, causing reversible left ventricular dysfunction and flow-metabolism mismatch. The condition is unstable and increasing demand may lead to further left ventricular dysfunction or necrosis ca...

journal_title：Journal of cardiovascular pharmacology

authors： Lahiri A,Senior R,Khattar R

更新日期：1999-06-01 00:00:00

abstract：:To clarify the characteristics of KC-399, a newly synthesized potassium channel opener, we investigated the effects of KC-399 and lemakalim on the contractions induced by norepinephrine (NE 1 microM) and K+ (30 and 90 mM) and on 86Rb efflux in rat thoracic aorta. KC-399 (0.01-10 nM) and lemakalim (0.001-10 microM) ind...

journal_title：Journal of cardiovascular pharmacology

authors： Tamura K,Suzuki Y,Yoshida S,Nabata H

更新日期：1994-02-01 00:00:00

abstract：:Artemisinin is an endoperoxide sesquiterpene lactone from Artemisia annua L with multiple beneficial effects, including anti-inflammation, antioxidant, and vascular protection. Recent studies have found that inflammation along with autophagy deficiency in macrophages is the possible reason for foam cell accumulation i...

journal_title：Journal of cardiovascular pharmacology

authors： Cao Q,Du H,Fu X,Duan N,Liu C,Li X

更新日期：2020-04-01 00:00:00

abstract：:KATP channels are a complex of regulatory sulfonylurea receptor subunits and the pore-forming inward rectifiers such as Kir6.1. Using the whole-cell patch-clamp technique, we investigated the interaction of nicotine with the Kir6.1 subunit as well as the underlying mechanism. Stable expression of Kir6.1 in HEK-293 cel...

journal_title：Journal of cardiovascular pharmacology

authors： Hanna ST,Cao K,Sun X,Wang R

更新日期：2005-05-01 00:00:00

abstract：:Previously we showed that blocking the endothelin (ET)A receptor subtype with BQ-153 inhibited the vasoconstrictor effects of intravenously administered ET-1. In the presence of the ET(A) antagonist, ET-1 produced marked reductions in myocardial contractility and renal blood flow. We postulated that either the ET(B) r...

journal_title：Journal of cardiovascular pharmacology

authors： Cirino M,Martin E,Yano M,Rodger IW

更新日期：1997-06-01 00:00:00

abstract：:Kinins elicit prostaglandin and inositol phosphate production in 3T3 fibroblasts through stimulation of B2 receptors. Prostaglandin synthesis is maximum by 5 min, whereas inositol phosphate production continues for longer than 30 min. Prostaglandin synthesis is stimulated by phospholipase A2, which releases arachidona...

journal_title：Journal of cardiovascular pharmacology

authors： Burch RM

更新日期：1990-01-01 00:00:00

abstract：:Spontaneously hypertensive stroke-prone rats suffer spontaneous strokes partly as a result of abnormal cerebrovascular development. This model exhibits prehypertensive, typical hypertensive and malignant hypertensive stages. We had observed that vascular endothelial growth factor and its receptors, kinase domain regio...

journal_title：Journal of cardiovascular pharmacology

authors： Jesmin S,Sakuma I,Togashi H,Yoshioka M,Hattori Y,Kitabatake A,Miyauchi T

更新日期：2004-11-01 00:00:00

abstract：:Several mechanisms of action for Ca2+ antagonists are possible at the vascular muscle cell membrane and at subsequent steps. In rat caudal artery, nitrendipine hyperpolarizes the resting vascular muscle cell, an action different from that of verapamil. Hyperpolarization might be expected to explain the relaxant action...

journal_title：Journal of cardiovascular pharmacology

authors： Hermsmeyer K,Kuthe C

更新日期：1984-01-01 00:00:00

abstract：:Endothelin-1 reduces the chronotropic and inotropic effects of the beta-adrenoceptor agonist isoproterenol in rabbit isolated atria. Vascular interactions between endothelin-1 and isoproterenol have not been reported. Rings of the rabbit aorta without endothelium were mounted on myographs to measure isometric tension....

journal_title：Journal of cardiovascular pharmacology

authors： Gilbert P,Thorin E

更新日期：2003-10-01 00:00:00

abstract：BACKGROUND:S-equol is known as an estrogenic substance, but its ability to restore vascular endothelial function is unknown. The aim of this study was to investigate the impact of S-equol on endothelial function and intimal thickening under isoflavone- and estrogen-deficient circumstances. METHODS:Twelve-week-old fema...

journal_title：Journal of cardiovascular pharmacology

authors： Ohkura Y,Obayashi S,Yamada K,Yamada M,Kubota T

更新日期：2015-05-01 00:00:00

abstract：:The relationships between the effects on blood pressure and vascular responsiveness, and the whole blood concentration of the antihypertensive drug trimazosin and its major metabolite were investigated in six normotensive male volunteers following 100 mg i.v. and 200 mg p.o. administration. Pressor responses to intrav...

journal_title：Journal of cardiovascular pharmacology

authors： Vincent J,Elliott HL,Meredith PA,Reid JL

更新日期：1985-09-01 00:00:00

abstract：:We produced transgenic mice overexpressing Na+/ H+ exchanger as a model of salt-sensitive hypertension and reported that dietary salt loading elevates blood pressure in these transgenic mice. We speculate that this blood pressure elevation may be attributed to the elevation of intraarterial smooth muscle Ca2+ concentr...

journal_title：Journal of cardiovascular pharmacology

authors： Kiraku J,Sugiyama T,Ashida T,Takahashi N,Fujii J,Kuro-o M,Nagai R

更新日期：2000-03-01 00:00:00

abstract：:Beside its antiarrhythmic properties, which in particular are used for the treatment of atrial fibrillation, quinidine is known to have alpha-adrenoceptor blocking properties. On the other hand, atrial fibrillation is reported to cause activation of the sympathetic nervous system which, in turn, reduces coronary blood...

journal_title：Journal of cardiovascular pharmacology

authors： Schipke J,Schulz R,Tölle T,Heusch G,Thämer V

更新日期：1987-12-01 00:00:00

abstract：:One of the earliest structural changes in the heart adapting to hypertension is left ventricular hypertrophy, which can now be exactly measured by echocardiography. Left ventricular hypertrophy increases the incidence of coronary artery disease, heart failure, and sudden death severalfold, independent of the blood pre...

journal_title：Journal of cardiovascular pharmacology

authors： Schmieder RE

更新日期：1992-01-01 00:00:00