Abstract:
:The effect of the imidazolidine Sgd 101/75 (2-[2-methylindazol-4-imino]-imidazolidine HCl) on blood pressure, as well as its alpha-adrenoceptor agonist activity and affinity for these receptors, were examined in various animal preparations. After both intravenous administration to conscious spontaneously hypertensive rats and intravenous injection or infusion via the vertebral artery in chloralose-anaesthetized cats, Sgd 101/75 (1-10 mg kg-1) elicited pressor responses. Intracisternal application of Sgd 101/75 (1 mg kg-1) to chloralose-anaesthetized cats did not affect blood pressure. In the pithed rat and pithed cat the vasopressor responses to i.v. Sgd 101/75 were effectively antagonized by prazosin (0.1-1.0 mg kg-1, i.v.) but much less by yohimbine (1 mg kg-1, i.v.). Sgd 101/75 proved a less potent and less selective displacing agent of [3H]-clonidine- and [3H]-prazosin-binding in rat brain membranes than clonidine. The results suggest that Sgd 101/75 is a selective alpha 1-adrenoceptor agonist, devoid of any centrally or peripherally mediated hypotensive activity; this is probably caused by the low capacity of Sgd 101/75 for stimulating alpha 2-adrenoceptors.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Mathy MJ,Thoolen MJ,Timmermans PB,van Zwieten PAdoi
10.1111/j.1476-5381.1984.tb10072.xsubject
Has Abstractpub_date
1984-02-01 00:00:00pages
255-62issue
2eissn
0007-1188issn
1476-5381journal_volume
81pub_type
杂志文章abstract::1. Simultaneous computer modelling of control and guanfacine-masked [3H]-MK 912 saturation curves as well as guanfacine competition curves revealed that the drugs bound to two alpha 2-adrenoceptor subtypes in the rat cerebral cortex with very different selectivities. These alpha 2-adrenoceptor subtypes were designated...
journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1992.tb14446.x
更新日期:1992-08-01 00:00:00
abstract:BACKGROUND AND PURPOSE:Excessive production of nitric oxide (NO) by inducible NO synthase (iNOS) is thought to underlie the vascular dysfunction, systemic hypotension and organ failure that characterize endotoxic shock. Plasma levels of atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP) and C-type natriu...
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1985.tb08888.x
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1985.tb08856.x
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abstract::1. Using a guinea-pig model of allergic asthma, in which the animals display early (0-5 h) and late phase (8-23 h after antigen challenge) bronchoconstrictor reactions, the function of prejunctional inhibitory M2 and postjunctional M3 receptors in isolated tracheal preparations have been investigated. In addition, car...
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abstract:BACKGROUND AND PURPOSE:Voltage-gated sodium channels (VGSCs) are assembled from two classes of subunits, a pore-bearing α-subunit (NaV 1) and one or two accessory β-subunits (NaV βs). Neurons in mammals can express one or more of seven isoforms of NaV 1 and one or more of four isoforms of NaV β. The peptide μ-conotoxin...
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doi:10.1111/j.1476-5381.1976.tb07477.x
更新日期:1976-06-01 00:00:00
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1985.tb08825.x
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abstract::Resting blood flow, arterio-venous glucose and oxygen (A-V)O2 differences, glucose uptake and oxygen consumption by a segment of the upper jejunum were measured in anaesthetized dogs. Systemic arterial pressure was also measured. The effect of nicotine infusion (25 micrograms kg-1 i.v., over 10 min) on these measureme...
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更新日期:1985-08-01 00:00:00
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doi:10.1038/sj.bjp.0705289
更新日期:2003-06-01 00:00:00
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doi:10.1111/j.1476-5381.1994.tb13050.x
更新日期:1994-05-01 00:00:00
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更新日期:2001-09-01 00:00:00
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doi:10.1111/j.1476-5381.1993.tb12845.x
更新日期:1993-03-01 00:00:00
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更新日期:2011-05-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2005-12-01 00:00:00
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更新日期:1996-09-01 00:00:00
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更新日期:1993-08-01 00:00:00
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更新日期:2000-03-01 00:00:00
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journal_title:British journal of pharmacology
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更新日期:1971-09-01 00:00:00
abstract::1. The present study has compared the relative anti-aggregatory effect of various compounds which interfere with thromboxane (Tx) A2-dependent aggregation of human platelets in whole blood in vitro. These included the cyclo-oxygenase inhibitor aspirin, the TxA2 synthase inhibitor dazoxiben, the TxA2 (TP-) receptor blo...
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pub_type: 杂志文章
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更新日期:1991-02-01 00:00:00
abstract::1. We have studied the effect of cannabinoid agonists (CP 55,940 and cannabinol) on intestinal motility in a model of intestinal inflammation (induced by oral croton oil in mice) and measured cannabinoid receptor expression, endocannabinoids (anandamide and 2-arachidonylglycerol) and anandamide amidohydrolase activity...
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pub_type: 杂志文章
doi:10.1038/sj.bjp.0704293
更新日期:2001-10-01 00:00:00