Abstract：
:1. The effects of methylflavonolamine hydrochloride (4'-methyl-7-(2-hydroxy-3-isopropylamino-propoxy)-flavone hydrochloride, MFA) were investigated and compared with verapamil and papaverine on rabbit isolated aortic strips, which were contracted by noradrenaline, calcium and potassium. 2. Pre-incubation for 25 min with either MFA (0.03 to 0.2 mM) or papaverine (0.03 to 0.2 mM) induced non-parallel and concentration-dependent rightward displacements of the curves to noradrenaline (0.00001 to 0.1 mM) with the maximal response depressed. The calculated pD2' values (mean +/- s.d.) were 3.89 +/- 0.15 for MFA and 3.93 +/- 0.05 for papaverine, respectively. Verapamil (0.03 to 0.2 mM) inhibited the contraction induced by noradrenaline in a competitive manner with a pA2 value of 5.91 +/- 0.83. 3. In depolarized aortic strips of the rabbit, prior exposure to MFA (0.03 to 0.3 mM) and papaverine (0.03 to 0.2 mM) shifted the cumulative curves to Ca2+ (0.003 to 100 mM) parallel to the right with the maximal responses depressed, pD'2 values being 3.88 +/- 0.05 and 3.89 +/- 0.13, respectively. Verapamil produced comparable inhibition of the contraction at much lower concentrations (30 to 300 nM). 4. MFA (0.03 and 0.1 mM) inhibited the contraction elicited by graded depolarization at a constant Ca2+ concentration with a pD'2 value of 4.09 +/- 0.07. 5. The present results show that MFA has some actions consistent with a calcium antagonist. It resembles papaverine more closely than verapamil.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Zhang MS,Zhou EFdoi
10.1111/j.1476-5381.1988.tb11637.xsubject
Has Abstractpub_date
1988-08-01 00:00:00pages
1184-8issue
4eissn
0007-1188issn
1476-5381journal_volume
94pub_type
杂志文章abstract：:1. Several cations (Ba2+, Cd2+, Co2+, Cu2+, Mn2+, Ni2+, Zn2+ and La3+, all as chloride salts, 1-1000 microM) were tested in the guinea-pig urinary bladder for their ability to: (i) modify contractile responses to electrical field stimulation (EFS), ATP, alpha,beta-methylene ATP (alpha,beta-meATP), carbachol (CCh), and...
journal_title：British journal of pharmacology
pub_type： 杂志文章
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更新日期：1995-02-01 00:00:00
abstract：:1 alpha-Monofluoromethyldopa (MFMD, RMI 71963), a potent and selective enzyme-activated irreversible inhibitor of aromatic L-amino acid decarboxylase produces a substantial and long-lasting decrease in the catecholamine content of mouse brain, heart and kidney. 2 Single doses of MFMD reduce the 5-hydroxytryptamine con...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1980.tb09776.x
更新日期：1980-12-01 00:00:00
abstract：:(1) Rapid desensitization of ligand-gated ion channel receptors can alter the apparent activity of receptor modulators, as well as make detection of fast-channel activation difficult. Investigation of the antagonist pharmacology of ATP-sensitive homomeric P2X3 receptors is limited by agonist-evoked fast-desensitizatio...
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doi：10.1038/sj.bjp.0705411
更新日期：2003-09-01 00:00:00
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journal_title：British journal of pharmacology
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abstract：:1. Heterologous desensitization or intermolecular cross-talk plays a critical role in regulating intracellular signalling by diverse members of the G-protein-coupled receptor superfamily. We have previously established that the alpha and beta isoforms of the human thromboxane A(2) receptor (TP) undergo differential de...
journal_title：British journal of pharmacology
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doi：10.1038/sj.bjp.0705695
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abstract：:1 The beta-adrenoceptor agonist isoprenaline normally causes only a small and inconsistent increase in the membrane potential of cells in guinea-pig liver slices, in contrast to the large hyperpolarizations seen with alpha-agonists. However, after a selective alpha-adrenoceptor agonist has been applied, the response t...
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1977.tb06991.x
更新日期：1977-01-01 00:00:00
abstract：:1. Isolated tissues of the guinea-pig were bathed with Krebs solution at 37 degrees C and subjected to 100 ms pulses of electrical stimulation for 30 min at a frequency of 0.1 or 1.0 Hz. The tissues were then dried, ashed, and the ash analysed for calcium, sodium, potassium and magnesium.2. Gastric smooth muscle, card...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1972.tb08124.x
更新日期：1972-08-01 00:00:00
abstract：:1. To examine further the potentiation by endothelin-1 on the vascular response to sympathetic stimulation, we studied the isometric response of isolated segments, 2 mm long, from the rabbit central ear artery to electrical field stimulation (1-8 Hz), under different conditions, at 37 degrees C and during cooling (30 ...
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abstract：BACKGROUND AND PURPOSE:Catechol-O-methyltransferase (COMT) inhibitors are used in Parkinson's disease in which pain is an important symptom. COMT polymorphisms modulate pain and opioid analgesia in humans. In rats, COMT inhibitors have been shown to be pro-nociceptive in acute pain models, but also to attenuate allodyn...
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0704485
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pub_type： 历史文章,杂志文章,评审
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更新日期：2006-01-01 00:00:00
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更新日期：1999-05-01 00:00:00
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doi：10.1111/j.1476-5381.1971.tb09936.x
更新日期：1971-01-01 00:00:00
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doi：10.1111/j.1476-5381.2011.01486.x
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1987.tb11195.x
更新日期：1987-03-01 00:00:00
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更新日期：2000-12-01 00:00:00
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pub_type： 传,社论,历史文章
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更新日期：2009-10-01 00:00:00
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pub_type： 杂志文章
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更新日期：1985-08-01 00:00:00
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pub_type： 杂志文章
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更新日期：1988-02-01 00:00:00
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更新日期：1992-06-01 00:00:00
abstract：:British Journal of Pharmacology (BJP) is pleased to publish a new set of guidelines for reporting research involving animals, simultaneously with several other journals; the 'ARRIVE' guidelines (Animals in Research: Reporting In Vivo Experiments). This editorial summarizes the background to the guidelines, gives our v...
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pub_type： 社论
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pub_type： 杂志文章
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更新日期：2004-08-01 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2009-04-01 00:00:00
abstract：BACKGROUND AND PURPOSE:11β-hydroxysteroid dehydrogenase type I (11β-HSD1), a target for Type 2 diabetes mellitus, converts inactive glucocorticoids into bioactive forms, increasing tissue concentrations. We have compared the pharmacokinetic-pharmacodynamic (PK/PD) relationship of target inhibition after acute and repea...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/bph.13251
更新日期：2015-10-01 00:00:00
abstract：:1. The fall in arterial blood pressure with bradycardia that occurs on injection of clonidine into the cerebral ventricles and into the cisterna magna is attributed to an action on ;chemosensitive zones' situated at the ventral surface of the brain stem. This conclusion is based on the following results obtained in ca...
journal_title：British journal of pharmacology
pub_type： 杂志文章
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