Quantitative analysis of the interaction of [3H]spiroperidol with serotonin and dopamine receptors.


:Many radioligands used to study neurotransmitter receptors label multiple subtypes or multiple classes of receptors. Frequently, two subtypes or classes of receptors coexist in the same tissue and exhibit only slightly different affinities for a radioligand. A new analytical method has been developed to quantitate the interaction of a slightly selective radioligand with two distinct classes of binding sites. This new approach requires that a series of inhibition experiments with a selective unlabeled ligand be performed in the presence of increasing concentrations of the radioligand. Analysis of the resulting inhibition curves, utilizing simultaneous nonlinear regression analysis techniques, yields estimates of the density of each class of receptor as well as the affinity of each receptor for the labeled and unlabeled ligands. This approach was used to characterize the interaction of [3H]spiroperidol with serotonin 5-HT2 and dopamine D2 receptors. A series of inhibition curves were generated with the 5-HT2 selective antagonist ketanserin using membranes prepared from rat striatum. [3H]Spiroperidol was found to be 23-fold more selective for D2 receptors and 27% of the sites labeled by [3H]spiroperidol exhibited a high affinity for ketanserin and were presumed to be 5-HT2 receptors. Since all of the radioligands commonly used to label 5-HT2 receptors also label other receptors, this method of analysis should be particularly useful in the study of these receptors.


J Cardiovasc Pharmacol


McGonigle P


Has Abstract


1988-01-01 00:00:00








11 Suppl 1


  • 3H-digoxin distribution in the nervous system in ventricular tachycardia.

    abstract::The distribution of 3H-digoxin has been measured in a large number of tissues from the central, autonomic, and peripheral nervous system after the induction of ventricular tachycardia by infusing digoxin into anesthetized dogs. In most parts of the nervous system the tissue digoxin concentration was close to that in t...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Frazer G,Binnion P

    更新日期:1981-11-01 00:00:00

  • Pentoxifylline Ameliorates Cardiac Fibrosis, Pathological Hypertrophy, and Cardiac Dysfunction in Angiotensin II-induced Hypertensive Rats.

    abstract::Inflammation induces cardiac fibrosis and hypertrophy in multiple cardiovascular diseases, contributing to cardiac dysfunction. We tested the hypothesis that pentoxifylline (PTX), a phosphodiesterase inhibitor with anti-inflammatory property, would attenuate cardiac fibrosis and hypertrophy, and prevent cardiac dysfun...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Zhang X,Meng F,Song J,Zhang L,Wang J,Li D,Li L,Dong P,Yang B,Chen Y

    更新日期:2016-01-01 00:00:00

  • Chronic treatment in vivo with dimethylthiourea, a hydroxyl radical scavenger, prevents diabetes-induced endothelial dysfunction.

    abstract::Oxidative stress is believed to play a role in diabetes-induced vascular complications. In this study, we tested whether chronic treatment with a known hydroxyl radical scavenger, dimethylthiourea (DMTU), could prevent endothelial dysfunction in diabetes. Lewis strain rats were made diabetic by an intravenous injectio...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Pieper GM,Siebeneich W,Roza AM,Jordan M,Adams MB

    更新日期:1996-12-01 00:00:00

  • Congestive heart failure: where homeostasis begets dyshomeostasis.

    abstract::Despite today's standard of care, aimed at preventing homeostatic neurohormonal activation, one in every five patients recently hospitalized with congestive heart failure (CHF) will be readmitted within 30 days of discharge because of a recurrence of their symptoms and signs. In light of recent pathophysiological insi...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Kamalov G,Bhattacharya SK,Weber KT

    更新日期:2010-09-01 00:00:00

  • Role of Caspase 1 in Ischemia/Reperfusion Injury of the Myocardium.

    abstract::Acute occlusion of a coronary artery can result in myocardial infarction-a leading cause of premature death. Prompt restoration of blood flow to the myocardium can prevent excessive death of cardiomyocytes and improve clinical outcome. Although the major mechanism of cell death after reperfusion is necrosis, it is now...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审


    authors: Rauf A,Shah M,Yellon DM,Davidson SM

    更新日期:2019-09-01 00:00:00

  • Effects of nitrendipine (BAY e 5009), nifedipine, verapamil, phentolamine, papaverine, and minoxidil on contractions of isolated rabbit aortic smooth muscle.

    abstract::The effects of nitrendipine, a new antihypertensive agent, have been examined using the isolated rabbit aortic strip stimulated with either noradrenaline (1.7 X 10(-8) - 1.7 X 10(-5) mol/L) or potassium (22.7-52.7 mmol/L). Nifedipine, verapamil, phentolamine, papaverine, and minoxidil were used as reference compounds....

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Towart R

    更新日期:1982-11-01 00:00:00

  • The impact of respiratory syncytial virus infection on endothelin receptor function and release in sheep bronchial explants.

    abstract::We investigated the impact of respiratory syncytial virus (RSV) infection, an important asthma precipitant, on endothelin receptor function and release in sheep bronchial explants. RSV infection was confirmed using polymerase chain reaction and immunohistochemistry. Since sheep airway smooth muscle contains only endot...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Fernandes LB,D'Aprile AC,Self GJ,Harnett GB,Goldie RG

    更新日期:2004-11-01 00:00:00

  • Hypertension and the development of heart failure.

    abstract::Hypertension is a well-known risk factor that predisposes to the development of left ventricular hypertrophy, coronary flow abnormalities, and systolic and diastolic dysfunction. This complex of abnormalities is known as hypertensive heart disease and eventually leads to heart failure. Structural lesions underlying th...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审


    authors: de Leeuw PW,Kroon AA

    更新日期:1998-01-01 00:00:00

  • Analysis of the electrophysiologic effects of short-term oxybutynin on guinea pig and rabbit ventricular cells.

    abstract::The objective of this study was to investigate the cardioactive properties of oxybutynin, a drug that is widely prescribed for management of voiding dysfunction. Membrane currents were recorded from whole-cell-configured guinea pig ventricular myocytes, and action potentials were recorded from guinea pig and rabbit pa...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Jones SE,Kasamaki Y,Shuba LM,Ogura T,McCullough JR,McDonald TF

    更新日期:2000-02-01 00:00:00

  • Amlodipine inhibition of serum-, thrombin-, or fibroblast growth factor-induced vascular smooth-muscle cell proliferation.

    abstract::Atherosclerosis, like several other vascular diseases, exhibits structural and functional abnormalities resulting partially from an exaggerated proliferation of vascular smooth-muscle cells (VSMCs). Ca2+ channel blockers, such as amlodipine, have been suggested to retard or even prevent the progression of atherosclero...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Stepien O,Gogusev J,Zhu DL,Iouzalen L,Herembert T,Drueke TB,Marche P

    更新日期:1998-05-01 00:00:00

  • Pharmacological doses of atrial natriuretic factor do not inhibit canine hypoxic pulmonary vasoconstriction.

    abstract::It has been recently suggested that atrial natriuretic factor (ANF) might be involved in the physiological regulation of pulmonary circulation. Therefore, we investigated the pulmonary hemodynamic response to 20-min infusions of 0.05, 0.1, and 0.2 micrograms kg-1 min-1 of alpha human ANF in five dogs alternatively ven...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Vachiery JL,Lejeune P,Brimioulle S,Debiève MF,Abramow M,Naeije R

    更新日期:1989-12-01 00:00:00

  • Bisoprolol improves survival in rats with heart failure.

    abstract::The cardioprotective effects of bisoprolol were studied in a rat model of severe heart failure induced by autoimmune myocarditis. Twenty-eight days after immunization, Lewis rats were divided into four groups: 0.1 mg/kg/day bisoprolol (Group 0.1), 1.0 mg/kg/day bisoprolol (Group 1) and 10 mg/kg/day bisoprolol (Group 1...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Watanabe K,Ohta Y,Inoue M,Ma M,Wahed MI,Nakazawa M,Hasegawa G,Naito M,Fuse K,Ito M,Kato K,Hanawa H,Kodama M,Aizawa Y

    更新日期:2001-10-01 00:00:00

  • Cardiovascular and renal effects of the beta-blocker SE2395 in conscious normotensive dogs.

    abstract::The cardiac and renal hemodynamic effects of SE2395, a beta-blocking agent, were examined after intravenous administration (50 micrograms/kg) in normotensive conscious dogs. Beta-blocking action of SE2395 was evidenced by a reduction in heart rate and cardiac output without change in the mean arterial pressure. An inc...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Walker BR,Erickson AL,Prost JF,Rochat C,Burke TJ

    更新日期:1985-11-01 00:00:00

  • Selection of initial and maintenance dosages for lacidipine, a new once-daily calcium antagonist for the treatment of hypertension.

    abstract::Selection of the appropriate dose of a new drug for initiation of treatment and then for maintenance is a complicated task. It requires the careful assessment and weighing of benefit vs. risk. A series of studies was carried out with lacidipine to determine the optimal initial dose in a general hypertensive population...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验,评审


    authors: Perelman M

    更新日期:1991-01-01 00:00:00

  • Diminished responses to nifedipine imply severe end-organ damage in spontaneously hypertensive rats.

    abstract::This study was designed to investigate the effect of end-organ damage (EOD), the initial blood pressure levels, and baroreflex sensitivity (BRS) on the blood pressure-lowering effect of nifedipine in spontaneously hypertensive rats (SHRs). Nifedipine was intravenously administered at a dose of 1 mg/kg. BP was continuo...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Lu LH,Xie HH,Cai GJ,Shen FM,Su DF

    更新日期:2005-12-01 00:00:00

  • Effect of mast cell stabilizers in hyperhomocysteinemia-induced cardiac hypertrophy in rats.

    abstract:BACKGROUND:The present study has been designed to investigate the effect of sodium cromoglycate and ketotifen, mast cell stabilizers in hyperhomocysteinemia-induced cardiac hypertrophy in rats. METHODS:Rats were administered L-methionine (1.7 g/kg/day PO) for 8 weeks to produce hyperhomocysteinemia. Sodium cromoglycat...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Singh AP,Singh M,Balakumar P

    更新日期:2008-06-01 00:00:00

  • Thromboxane A2 does not contribute to arrhythmogenesis during evolving canine myocardial infarction.

    abstract::During the healing phase of evolving myocardial infarction, inflammatory cells invade the affected region and produce metabolites that may influence electrophysiological parameters and the genesis of malignant arrhythmias. We have recently shown an increased synthetic capacity within an evolving infarct for thromboxan...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Kramer JB,Davis AG,Dean R Jr,McCluskey ER,Needleman P,Corr PB

    更新日期:1985-11-01 00:00:00

  • Secretion of endothelin-1 and adrenomedullin by SW-13 human adrenocortical carcinoma cells.

    abstract::The adrenal medulla and pheochromocytomas are known to secrete various neuropeptides and vasoactive peptides. On the other hand, the production and secretion of peptides by adrenocortical tumors have not been studied in detail. The study reported here therefore set out to examine these two functions for two vasoactive...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Takahashi K,Yoshinoya A,Murakami O,Totsune K,Shibahara S

    更新日期:2000-11-01 00:00:00

  • Clobutinol delays ventricular repolarization in the guinea pig heart: comparison with cardiac effects of HERG K+ channel inhibitor E-4031.

    abstract::Clobutinol has been clinically reported to induce long QT syndrome. To clarify its cardiac electrophysiological properties, we compared effects of clobutinol on the isolated myocardium and anesthetized guinea pig heart with those of a hERG K channel blocker, E-4031. In isolated guinea pig ventricular tissues, clobutin...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Takahara A,Sasaki R,Nakamura M,Sendo A,Sakurai Y,Namekata I,Tanaka H

    更新日期:2009-12-01 00:00:00

  • Antihypertensive effects and pharmacokinetics of single and consecutive administration of doxazosin in patients with mild to moderate essential hypertension.

    abstract::A single dose of doxazosin, a long-acting postsynaptic alpha 1-adrenoceptor antagonist, was administered to seven patients with essential hypertension. Following administration of a single dose, all the patients except one who was forced to be discharged from the hospital for work, continuously received doxazosin once...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Shionoiri H,Yasuda G,Yoshimura H,Umemura S,Miyajima E,Miyakawa T,Takagi N,Kaneko Y

    更新日期:1987-07-01 00:00:00

  • Angiotensin converting enzyme inhibition does not prevent the natriuretic effect of felodipine.

    abstract::The mechanism of natriuresis with calcium entry blockers such as felodipine is largely unexplained. As these drugs prevent sodium retention following exogenous angiotensin II, the natriuretic effect of felodipine might be due to a similar interaction with endogenous angiotensin II. In such a case, angiotensin converti...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: van Hamersvelt HW,Wetzels JF,Kloke HJ,Koene RA,Huysmans FT

    更新日期:1993-03-01 00:00:00

  • ITF 296, a new endothelium-independent vasodilator: comparison with nitroglycerin and isosorbide dinitrate.

    abstract::The effects of a new nitrate ester derivative, ITF 296, on large conductance and small resistance coronary arteries were investigated and compared with those of nitroglycerin and isosorbide dinitrate in chronically instrumented conscious dogs with an intact or with a deendothelialized large coronary artery. In a wide ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Ghaleh B,Dubois-Randé JL,Hittinger L,Berdeaux A,Giudicelli JF

    更新日期:1995-01-01 00:00:00

  • Effect of endothelin-1 on arterioles and venules in vivo.

    abstract::The vasoconstrictor effects of endothelin-1 (ET-1) and norepinephrine (NE) were compared in the exteriorized rat mesentery in situ. ET-1 was 1,000 times more potent than NE in constricting both arterioles and venules. Vasoconstrictions induced by ET-1 lasted much longer than those caused by the catecholamine. At nonre...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Fortes ZB,de Nucci G,Garcia-Leme J

    更新日期:1989-01-01 00:00:00

  • Osmoregulation and baroregulation of plasma vasopressin in essential hypertension.

    abstract::Vasopressin secretion is stimulated by hyperosmolality, hypovolemia, or hypotension and is inhibited by hypoosmolality, hypervolemia, or hypertension. These osmotic and hemodynamic influences are mediated by neuronal afferents that originate in separate osmoreceptors or baroreceptors but ultimately converge to act on ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Robertson GL,Ganguly A

    更新日期:1986-01-01 00:00:00

  • Endothelin-1-induced contraction of rat thoracic aorta depends on calcium entry through three types of calcium channel.

    abstract::We have recently shown that endothelin-1 (ET-1) activates two types of Ca2+-permeable nonselective cation channels (designated NSCC-1 and NSCC-2) and store-operated Ca2+ channel (SOCC). These channels can be pharmacologically discriminated using 1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1-H-imidazoe l h...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Zhang XF,Iwamuro Y,Okamoto Y,Kawanabe Y,Masaki T,Miwa S

    更新日期:2000-11-01 00:00:00

  • Effects of adenosine and verapamil on anatomic no-reflow in a rabbit model of coronary artery occlusion and reperfusion.

    abstract::Adenosine and verapamil have successfully been used in the treatment of clinical no-reflow after direct angioplasty for acute myocardial infarction. However, their effects on anatomic perfusion defects in experimental myocardial ischemia/reperfusion are unknown. Thus the area of no-reflow (ANR), visualized after in-vi...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Reffelmann T,Kloner RA

    更新日期:2004-04-01 00:00:00

  • Impaired L-arginine uptake but not arginase contributes to endothelial dysfunction in rats with chronic kidney disease.

    abstract::Reduced nitric oxide bioavailability contributes to increased cardiovascular disease risk in patients with chronic kidney disease (CKD). Arginase has been implicated as a potential therapeutic target to treat vascular dysfunction by improving substrate availability for endothelial nitric oxide synthase. The purpose of...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Martens CR,Kuczmarski JM,Lennon-Edwards S,Edwards DG

    更新日期:2014-01-01 00:00:00

  • Prazosin first-pass metabolism and hepatic extraction in the dog.

    abstract::The short half-life, low plasma concentrations, and extensive biotransformation of prazosin suggest that it might be subject to extensive first-pass metabolism. Bioavailability, disposition, and hepatic extraction were studied in the dog. In conscious dogs whole blood prazosin concentrations were measured after oral a...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Rubin P,Yee YG,Anderson M,Blaschke T

    更新日期:1979-11-01 00:00:00

  • The utility of hERG and repolarization assays in evaluating delayed cardiac repolarization: influence of multi-channel block.

    abstract::Drug-induced delayed cardiac repolarization is a recognized risk factor for proarrhythmia and is associated with block of IKr (the potassium current encoded by the human ether-a- go-go-related gene [hERG]). To evaluate the utility of 2 in vitro assays widely used to assess delayed repolarization, we compared the effec...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Martin RL,McDermott JS,Salmen HJ,Palmatier J,Cox BF,Gintant GA

    更新日期:2004-03-01 00:00:00

  • Heterogeneity of postjunctional alpha-adrenoceptors in isolated mesenteric resistance arteries from rats, rabbits, pigs, and humans.

    abstract::Mesenteric resistance arteries (internal diameter 174-337 microns) from rats, rabbits, pigs, and humans were isolated and mounted in a myograph. In all preparations, phenylephrine (alpha 1-adrenoceptor agonist) evoked concentration-dependent contractions that were antagonized by prazosin (alpha 1-adrenoceptor antagoni...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章


    authors: Nielsen H,Pilegaard HK,Hasenkam JM,Mortensen FV,Mulvany MJ

    更新日期:1991-07-01 00:00:00