Abstract:
:1. alpha 1-Adrenoceptor subtypes in rabbit thoracic aorta have been examined in binding and functional experiments. 2. [3H]-prazosin bound to two distinct populations of alpha 1-adrenoceptors (pKD,high = 9.94, Rhigh = 79.2 fmol mg-1 protein; pKD,low = 8.59, Rlow = 215 fmol mg-1 protein). Pretreatment with chloroethylclonidine (CEC, 10 microM) almost inactivated the prazosin-high affinity sites and reduced the number of the low affinity sites without changing the pKD value. 3. In the displacement experiments with CEC-untreated membranes, unlabelled prazosin, WB4101 and HV723 displaced the binding of 200 pM [3H]-prazosin monophasically; the affinities for WB4101 (pK1 = 8.88) and HV723 (8.49) were about 10 times lower than that for prazosin (9.99). In the CEC-pretreated membranes also, the antagonists inhibited the binding of 1000 pM [3H]-prazosin monophasically; the pK1 values for prazosin, WB4101 and HV723 were 9.09, 8.97 and 8.17, respectively. These results suggest that the prazosin-high and low affinity sites can be independently appraised in the former and latter experimental conditions. Noradrenaline, but not methoxamine, showed slightly higher affinity for the prazosin-high affinity site than for the low affinity site. 4. In the functional experiments, noradrenaline (0.001-100 microM) and methoxamine (0.1-100 microM) produced concentration-dependent contractions. Pretreatment with CEC inhibited the contractions induced by low concentrations of noradrenaline but without effect on the responses to methoxamine. Prazosin inhibited the concentration-response curves for noradrenaline in the CEC-untreated aorta in a manner which was not consistent with competitive antagonism at a single site, and two distinct affinity constants(pKB = 9.71 and 8.74) were obtained. However, after CEC-pretreatment, Schild plots for prazosin were not significantly different from unity (pKB = 8.50). WB4101 and HV723 competitively inhibited the noradrenaline-induced contraction with low pKB values (approximately 8.30), irrespective of CEC pretreatment.Methoxamine-induced contractions were competitively inhibited by prazosin, WB4101 and HV723 with low pKB values similar to those obtained when noradrenaline was used as the agonist.These were not affected by CEC-pretreatment.5. The affinity constant for noradrenaline (pKA = 6.40) in CEC-untreated aorta was slightly greater than that obtained in CEC-pretreated aorta (5.78). On the other hand, methoxamine showed a similar affinity in CEC-untreated and pretreated aortae (pKA = approximately 4.5).6. Nifedipine (1 microM) slightly attenuated the contractile responses to noradrenaline and methoxamine in CEC-untreated and pretreated aortae, suggesting that nifedipine cannot discriminate between alpha 1-adrenoceptors involved in CEC-sensitive and -resistant contractions.7. From these results it is suggested that in the rabbit thoracic aorta there are two distinct alpha 1-adrenoceptor subtypes (presumably alpha 1B and alpha 1L subtypes according to recently proposed subclassification),both of which are involved in noradrenaline-induced contraction. The alpha 1L subtype predominantly mediates the contraction induced by methoxamine.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Oshita M,Kigoshi S,Muramatsu Idoi
10.1111/j.1476-5381.1993.tb13507.xsubject
Has Abstractpub_date
1993-04-01 00:00:00pages
1071-6issue
4eissn
0007-1188issn
1476-5381journal_volume
108pub_type
杂志文章abstract::(1) We determined the effects of long-term treatment with aminoguanidine (AG), an inhibitor of advanced glycation end products, on the mechanical properties of the arterial system in aged Fisher 344 rats, using the aortic impedance analysis. (2) Normotensive rats were treated from 18 to 24 months with AG (1 g/l-1 in d...
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abstract::The cardiovascular effects of doxazosin, a quinazoline derivative related to prasozin were investigated and compared to prazosin in the rabbit. Radioligand binding studies using rabbit cerebral membranes showed that both doxazosin and prazosin were roughly equipotent at displacing [3H]-prazosin from specific binding s...
journal_title:British journal of pharmacology
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abstract::1 The effects of prostaglandin (PGE(1)), following local administration during different phases of developing sponge-induced granulomata, were studied in normal and essential fatty acid deficient (EFAD) rats.2 In normal rats, a single dose of 1 mug PGE(1) on implantation (day 1) increased exudate production without al...
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abstract::1. The aim of the present experiments was to investigate the pharmacological action of a toxin from the spider Phoneutria nigriventer, Tx3-3, on the function of calcium channels that control exocytosis of synaptic vesicles. 2. Tx3-3, in confirmation of previous work, diminished the intracellular calcium increase induc...
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更新日期:1997-10-01 00:00:00
abstract::1. The dihydropyridine calcium channel activator, Bay K 8644, is believed to increase mean arterial blood pressure in several animal models, as a result of direct activation of vascular smooth muscle cells by increasing calcium influx through the voltage-dependent calcium channels. The purpose of the current study was...
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abstract::1. Steady state fever has been produced in rabbits with a priming injection followed by a sustaining infusion of homologous plasma containing endogenous pyrogen (EP). This fever appears to last as long as the infusion continues.2. Intravenous salicylate given 1 h after the start of the EP infusion produced only a smal...
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abstract::1. We have investigated the effects of RP 73401, a novel, potent and highly selective cyclic nucleotide phosphodiesterase (PDE) type IV inhibitor, in guinea-pig and rat models of bronchoconstriction and allergic inflammation. In some models, the effects of RP 73401 have been compared with those of the standard PDE typ...
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更新日期:1994-12-01 00:00:00
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更新日期:1990-08-01 00:00:00
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pub_type: 杂志文章,随机对照试验
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更新日期:2014-04-01 00:00:00
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更新日期:2000-09-01 00:00:00
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更新日期:2000-05-01 00:00:00
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