We tried to determine alpha 1-adrenoceptor subtypes involved in noradrenaline-induced contractions of rat thoracic aorta and dog carotid artery. Prazosin competitively antagonized the contractions induced by noradrenaline in both the arteries with a high pKB value (approximately 9.7). WB4101, benoxathian, phentolamine, HV723 and 5-methylurapidil also competitively antagonized the responses to n...

The action of beta- and alpha-adrenoceptor agonists (isoprenaline, orciprenaline, noradrenaline, phenylephrine and ephedrine) and antagonists (propranolol, metipranolol, exaprolol, BL 445 and phentolamine) on the resting tension and cAMP level of the guinea pig and the mechanical and electrical activities of the dog trachea were studied. By activating beta 2-adrenoceptors, isoprenaline and orci...

MIcHIo MOTOHASHI AND MASAO NISHIKAWA. Conformational Analysis of Beta2-Adrenoceptor-Stimulating Agents 22 THOMAS N. LAVIN, BRIAN B. HOFFMAN, AND ROBERT J. LEFKOWITZ. Determination of Subtype Selectivity of Alpha-Adrenergic Antagonists: Comparison of Selective and Nonselective Radioligands 28 w. POWELL-JONES, S. RAEFORD, AND G. W. LUCIER. Binding Properties of Zearalenone Mycotoxins to Hepatic E...

1. The whole-cell patch-clamp was used for studying the effects of various beta1- and beta2-adrenoceptor agonists and antagonists on the L-type Ca current (Ica) in frog ventricular myocytes. 2. Dose-response curves for the effects of isoprenaline (non selective beta-agonist), salbutamol (beta2-agonist), dobutamine (beta1-agonist) on ICa were obtained in the absence and presence of various conce...

Recent evidence from our laboratory has demonstrated that a1-adrenoceptor antagonists doxazosin and terazosin induced apoptosis in prostate epithelial and smooth muscle cells in patients with benign prostatic hypertrophy (BPH; J. Urol., 159: 1810–1815, 1998; J. Urol., 161: 2002– 2007, 1999). In this study, we investigated the biological action of three a1-adrenoceptor antagonists, doxazosin, te...

Recent evidence from our laboratory has demonstrated that alpha1-adrenoceptor antagonists doxazosin and terazosin induced apoptosis in prostate epithelial and smooth muscle cells in patients with benign prostatic hypertrophy (BPH; J. Urol., 159: 1810-1815, 1998; J. Urol., 161: 2002-2007, 1999). In this study, we investigated the biological action of three alpha1-adrenoceptor antagonists, doxazo...

Rhinovirus (RV) infections account for approximately two thirds of all virus-induced asthma exacerbations and often result in an impaired response to β2 agonist therapy. Using an in vitro model of RV infection, we investigated the mechanisms underlying RV-induced β2 adrenoceptor desensitization in primary human airway smooth muscle cells (ASMC). RV infection of primary human bronchial epithelia...

Many G-protein-coupled receptors, including the alpha(1b)-adrenoceptor, form homo-dimers or oligomers. Mutation of hydrophobic residues in transmembrane domains I and IV alters the organization of the alpha(1b)-adrenoceptor oligomer, with transmembrane domain IV playing a critical role. These mutations also result in endoplasmic reticulum trapping of the receptor. Following stable expression of...

EMETIC AND ANTIEMETIC DRUGS 4.1. Neuroleptics 4.1.1. Phenothiazines 4.1.2. Butyrophenones and Related Compounds 4.1.3. Substituted Benzamides; Metoclopramide. Sulpiride and Others 4.2. Antihistamines 4.3. Miscellaneous Antiemetic Drugs 4.3.1. 4.3.2. 4.3.3. 4.3.4. 4.3.5. 4.3.6. 4.3.7. 4.3.8. 4.3.9. 4.3.10. Cannabinoids Steroids Domperidone Anxiolytics and Sedatives Analgesics Tricyclic Antidepre...

Noradrenergic inputs modulate hippocampal function via distinct receptors. In hippocampal neuronal cultures, mRNA expression of adrenoceptor subtypes is maintained from 1 day in vitro (DIV) to 22 DIV. Noradrenaline dose-dependently stimulates phosphoinositide (PI) breakdown in both immature and mature cultures through the activation of alpha1 receptors. At 22 DIV, basal PI breakdown depends on ...