- Abstract: 1. The homogeneity of beta-adrenoceptors in femoral, superior mesenteric and renal vascular beds was investigated by the use of the regional perfusion technique in dogs. 2. Isoprenaline and salbutamol produced dose-related increases in femoral and superior mesenteric blood flow. The dose-response curves for the two agonists were parallel, but salbutamol was approximately 1/15 as potent as isoprenaline on a weight basis. 3. Isoprenaline and salbutamol increased renal blood flow in a... Show More
- Abstract: The bronchodilator and cardiovascular actions of 5-(1-hydroxy 2-isopropylaminobutyl)-8-hydroxycarbostyril hydrochloride hemihydrate (OPC-2009) were investigated in anesthetized dogs and compared with those of isoproterenol, salbutamol or trimetoquinol. Bronchodilator and cardiovascular effects of OPC-2009 were attributable to its beta adrenoceptor stimulant action because they were antagonized by propranolol or pindolol. OPC-2009 was almost equiactive to isoproterenol and trimetoquinol but... Show More
- Abstract: 1. The antiarrhythmic properties of 5-(3-tert-butylamino-2-hydroxy)propoxy-3,4-dihydrocarbostyril hydrochloride (opc-1085) were compared with those of propranolol and pindolol using various kinds of preparations for experimental arrhythmia in dogs. 2. Although OPC-1085 was the most potent drug to antagonize adrenaline-induced arrhythmia in animals anaesthetized with either pentobarbitone sodium or halothane, it was scarcely effective on ouabain-induced arrhythmia in pentobarbitone sodium... Show More
- Abstract: Effects of procaterol (PRO) on the CNS were investigated in comparison with those of salbutamol (SAL) and isoproterenol (ISO). PRO, 15 to 50 mg/kg given subcutaneously suppressed spontaneous movement in mice, rats and rabbits and with a large dose, 1000 mg/kg, the animals became quiet and immobile. In dogs, PRO produced similar symptoms and in addition, there was nausea and vomiting. The animals recovered within 3--8 hours. ID50's in depressing spontaneous movement were 20.2 and 245 mg/kg... Show More
- Abstract: Pharmacological properties of procaterol (PRO) in the peripheral organs were examined in comparison with those of sulbutamol (SAL) and isoproterenol (ISO). PRO slightly enhanced twitch tension of the tibialis anterior muscle but affected little the mono- and poly-synaptic spinal reflexes and ganglionic transmission. PRO depressed spontaneous contractions of the isolated ileum, non-pregnant and pregnant uterus and also the gastrointestinal and uterine movements in vivo. PRO prolonged the time... Show More
- Abstract: 1. The antiarrhythmic properties of 5–(3-tert-butylarnino-2-hydroxy)propoxy-3,4-dihydrocarbostyril hydrochloride (OPC-1085) were compared with those of propranolol and pindolol using various kinds of preparations for experimental arrhythmia in dogs. 2. Although OPC-1085 was the most potent drug to antagonize adrenaline-induced arrhythmia in animals anaesthetized with either pentobarbitone sodium or halothane, it was scarcely effective on ouabain-induced arrhythmia in pentobarbitone sodium... Show More
Publications citing this author (92)
[Show abstract] [Hide abstract] ABSTRACT: beta-Adrenergic receptors (beta-AR) are essential regulators of cardiovascular homeostasis. In addition to their prominent function in the heart, beta-AR are located on vascular smooth muscle cells, where they mediate vasodilating effects of endogenous catecholamines. In this study, we have investigated in an isometric myograph different types of blood vessels from mice lacking beta(1)- and/or beta(2)-adrenergic receptor subtypes (beta(1)-KO, beta(2)-KO, beta(1)beta(2)-KO). In wild-type mice, isoproterenol induced relaxation of segments from thoracic aorta, carotid, femoral and pulmonary arteries, and portal vein. The relaxant effect of beta-receptor stimulation was absent in femoral and pulmonary arteries from beta(1)-KO mice. In aortic and carotid arteries and in portal veins, the vasodilating effect of isoproterenol was reduced in mice lacking beta(1)- or beta(2)-receptors. However, in these vessels the vasodilating effect was only abolished in double KO mice lacking both beta(1)- and beta(2)-receptors. Vessel relaxation induced by forskolin did not differ between wild-type and KO mice. Similar contributions of beta(1)- and beta(2)-receptors to isoproterenol-induced vasorelaxation were found when vessels from KO mice were compared with wild-type arteries in the presence of subtype-selective beta-receptor antagonists. These studies demonstrate that beta(1)-adrenergic receptors play a dominant role in the murine vascular system to mediate vasodilation. Surprisingly, beta(2)-receptors contribute to adrenergic vasodilation only in a few major blood vessels, suggesting that differential distribution of beta-adrenergic receptor subtypes may play an important role in redirection of tissue perfusion.
- These experiments demonstrate that norepinephrine's vasodilatory action, which is mediated by the ␤ 1 -AR, is usually masked by the strong activation of constricting ␣-AR. ␤ 1 -AR contribute significantly to vasodilation in bovine, canine, and rat coronary arteries (Vatner et al., 1984, 1986; Nakane et al., 1988; Abdelrahman et al., 1990; Young et al., 1990), rat superior mesenteric and renal arteries (Taira et al., 1977; Zwaveling et al., 1996), and rat mesenteric and portal veins (Kaumann and Groszmann, 1989). Similar data exist for ␤-adrenergic vasodilation in human blood vessels.
[Show abstract] [Hide abstract] ABSTRACT: The potent, subtype-selective radioligand (+/-)-erythro-5-(1-hydroxy-2-[11C]isopropyl-aminobutyl)-8-hydroxy-car bostyril ([11C]procaterol) was synthesized and evaluated for visualization of pulmonary beta2-adrenoceptors with positron emission tomography (PET). Procaterol was labelled by reductive alkylation of the desisopropyl precursor with [11C]acetone under the influence of NaCNBH3 and acetic acid. Synthesis and HPLC purification were performed in 34 min. Specific activities ranged from 26.5-39.3 TBq (about 700-1000 Ci)/mmol and the radiochemical yield was 2.4-8.6% (corrected for decay). Biodistribution studies were performed in male Wistar rats which were either untreated or predosed with (D,L)-propranolol hydrochloride (beta-adrenoceptor antagonist, 2.5 mg/kg), ICI 118551 (beta2-adrenoceptor antagonist, 0.15 mg/kg), CGP 20712A (beta1-adrenoceptor antagonist, 0.15 mg/kg) or isoprenaline (beta1-adrenoceptor agonist, 15 mg/kg). Specific binding was observed in lungs, spleen and red blood cells, tissues known to contain beta2-adrenoceptors. Pulmonary binding was blocked by propranolol, ICI 118551 and isoprenaline, but not by CGP 20712A. This binding pattern is consistent with the beta2 selectivity of the radioligand. The clearance of [11C]procaterol was biphasic, with a rapid distribution phase (t1/2 0.17 min) representing 90% of the injected dose followed by an elimination phase (t1/2 18.1 min). About 45% of the plasma radioactivity was unmetabolized procaterol at 15 min postinjection. In a dynamic PET-study, the lungs of untreated control rats could barely be detected and total/non-specific binding ratios rose to only 1.2 at 20 min postinjection. Although labelling and administration of (-) erythroprocaterol, the most active of 4 stereoisomers, may produce better results, [11C]procaterol seems unsuitable for beta-adrenoceptor imaging.
- Many bblockers have been labeled via this route in the past, such as propranolol (Berger et al., 1980Berger et al., , 1982 ), practolol (Berger et al., 1983), pindolol (Prenant et al., 1987) and carazolol (Berridge et al., 1992 ). Moreover, procaterol is known to be relatively slowly metabolized (Yabuuchi et al., 1977; Yamashita et al., 1978). Because of its rapid and facile synthesis, [ 11 C]procaterol could be more suitable for human studies than [ 11 C]formoterol.