Abstract:
:1. Muscularis mucosae of the distal oesophagus of the opossum contracts in response to substance P and to a variety of tachykinins. To delineate the nature of the receptors present in this tissue, we evaluated contractile responses to substance P, neurokinin A, neurokinin B, eledoisin and analogues believed to be highly selective for NK-1, NK-2 and NK-3 receptors. In addition, the effects of prolonged exposure to each of these agents (10(-6) M or 10(-5) M) on contractile responses to substance P and to itself were evaluated. Similarly effects of prolonged exposure to the various tachykinins and their analogues on the field-stimulated responses of this muscle were studied. 2. All naturally occurring tachykinins were full agonists and differed in potency (comparing ED50 values) by less than ten fold. In nearly all cases there was cross tachyphylaxis between substance P and the other tachykinins and each reduced tonic responses to field stimulation, a response previously shown to be mediated by a substance P like agent. Eledoisin failed to cause tachyphylaxis under the conditions of these experiments. 3. When highly selective tachykinin analogues were used, only that believed to activate NK-1 receptors was a full agonist. [beta-Ala4,Sar9,MetO2(11)]SP(4-11) was also only slightly less potent than substance P. In contrast, an agonist selective for NK-2 (NK-A) receptors, [Nle10]NKA(4-10), and one selective for NK-3 (NK-B) receptors, [beta-Asp4, MePhe7]NKB(4-10) were unable to produce a response equal to 50% of the maximum even at 10(-5) M. However, all three selective tachykinin analogues reduced responses to substance P but not to carbachol. They usually reduced both phasic and tonic responses to field stimulation. 4. We conclude, based on this and earlier study, that the tachykinin receptors of opossum oesophagus muscularis mucosae recognize all naturally occurring tachykinins but may represent only NK-1 receptors. The ability of analogues selective for other types of tachykinin receptors to reduce responses to substance P raises the possibility that their selectivity depends in part on diminished efficacy rather than totally on diminished affinity at some classes of receptor.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Daniel EE,Cipris S,Manaka Y,Bowker P,Regoli Ddoi
10.1111/j.1476-5381.1989.tb12556.xsubject
Has Abstractpub_date
1989-08-01 00:00:00pages
1013-8issue
4eissn
0007-1188issn
1476-5381journal_volume
97pub_type
杂志文章abstract::1 Peptide 401, a potent mast cell degranulating factor from bee venom, substantially inhibited the oedema provoked by subplantar injection of carrageenin or intra-articular injection of turpentine in the rat. The ED(50) of 401 was c. 0.1 mg/kg. The anti-inflammatory effect was assessed by measurement of the increased ...
journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1974.tb09613.x
更新日期:1974-03-01 00:00:00
abstract:BACKGROUND AND PURPOSE:Bleomycin (BLM), one of the most common sclerosants, is often used to treat venous malformations (VMs). The present study was designed to investigate whether endothelial mesenchymal transition (EndoMT) contributes to the therapeutic effects of BLM. EXPERIMENTAL APPROACH:Endothelial and mesenchym...
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journal_title:British journal of pharmacology
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更新日期:1982-02-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1982.tb09348.x
更新日期:1982-12-01 00:00:00
abstract::1 Anthopleurin-B (AP-B, greater than 3 x 10(-9) M), a newly isolated polypeptide from sea anemone (Anthopleura xanthogrammica), caused powerful rhythmic contractions in the guinea-pig isolated vas deferens. The other polypeptides anthopleurin-A from A. xanthogrammica and anthopleurin-C from A. elegantissima, elicited ...
journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1981.tb09951.x
更新日期:1981-09-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
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更新日期:1990-10-01 00:00:00
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pub_type: 杂志文章
doi:10.1038/sj.bjp.0704127
更新日期:2001-07-01 00:00:00
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pub_type: 杂志文章
doi:10.1111/j.1476-5381.1988.tb11699.x
更新日期:1988-11-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
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更新日期:1984-01-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1038/sj.bjp.0701168
更新日期:1997-06-01 00:00:00
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pub_type: 杂志文章
doi:10.1038/sj.bjp.0706232
更新日期:2005-07-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1979.tb07867.x
更新日期:1979-04-01 00:00:00
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pub_type: 杂志文章
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更新日期:1993-07-01 00:00:00
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pub_type: 杂志文章
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更新日期:1993-04-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 评论,杂志文章
doi:10.1038/sj.bjp.0706941
更新日期:2007-01-01 00:00:00
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pub_type: 杂志文章
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更新日期:2008-06-01 00:00:00
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journal_title:British journal of pharmacology
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更新日期:2000-09-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1993.tb13577.x
更新日期:1993-06-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1992.tb14308.x
更新日期:1992-05-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章,评审
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更新日期:2019-02-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
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更新日期:1995-12-01 00:00:00
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journal_title:British journal of pharmacology
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更新日期:1977-09-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
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更新日期:1982-04-01 00:00:00
abstract::1. Effects of an orally active non-peptide (BK) B2 receptor antagonist, FR173657 ((E)-3-(6-acetamido-3-pyridyl)-N-[N-[2,4-dichloro-3-[(2-methyl-8-quinoli nyl) oxymethyl]phenyl]-N-methylaminocarbonylmethyl] acrylamide) on the plasma exudation in rat carrageenin-induced pleurisy were investigated. 2. Plasma exudation in...
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更新日期:1997-06-01 00:00:00
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pub_type: 杂志文章
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更新日期:1998-09-01 00:00:00
abstract::The presence of functional cannabinoid CB2 receptors in the CNS has provoked considerable controversy over the past few years. Formerly considered as an exclusively peripheral receptor, it is now accepted that it is also present in limited amounts and distinct locations in the brain of several animal species, includin...
journal_title:British journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1038/sj.bjp.0707505
更新日期:2008-01-01 00:00:00