The CGP7930 analogue 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP) potentiates baclofen action at GABA(B) autoreceptors.


:The pharmacological actions of 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP), a putative presynaptic GABA(B) receptor modulator, were examined in electrically stimulated rat neocortical brain slices preloaded with [3H]-GABA or [3H]-glutamic acid. At 10 mmol/L, BSPP inhibited the release of [3H]-GABA in the presence of baclofen, but not that of [3H]-glutamic acid. This effect was sensitive to the GABA(B) receptor antagonist (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch 50911). Alone, BSPP had no effect on the release of [3H]-GABA or [3H]-glutamic acid. It is concluded that BSPP selectively potentiates the action of baclofen at GABA(B) autoreceptors, but not heteroreceptors and may be a useful ligand to discriminate between presynaptic GABA(B) receptor subtypes.


Parker DA,Marino V,Ong J,Puspawati NM,Prager RH




Has Abstract


2008-09-01 00:00:00














  • Cyp2c19 genotype and omeprazole hydroxylation phenotype in Chinese Li population.

    abstract::1. CYP2C19 is a polymorphism of cytochrome P450, which is responsible for the metabolism of many drugs. The genetic polymorphism shows interethnic variation and it has been demonstrated that the frequency of poor metabolizers (PM) and the distribution of alleles of CYP2C19 vary among Chinese ethnic nationalities. The ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Wang JH,Li PQ,Fu QY,Li QX,Cai WW

    更新日期:2007-05-01 00:00:00

  • Effect of furazolidone and nitrofurazone on brain gamma-amino butyric acid and glutamate concentrations in chickens.

    abstract::1. The concentrations of gamma-amino butyric acid (GABA) and glutamate were measured in the brains of chickens which were treated with furazolidone (FZ) or nitrofurazone (NF) at oral doses of 12.5, 25 or 50 mg/kg for 5 days. 2. At the end of the treatment, birds on the small dose of FZ or NF lost about 9% of their bod...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Ali BH

    更新日期:1988-12-01 00:00:00

  • Microcomputer statistics packages for biomedical scientists.

    abstract::1. There are hundreds of commercially available microcomputer statistics packages, ranging from the very cheap and elementary to the very expensive and complex, and from the very general to the very specialized. This review covers only those that appear to be popular with biomedical investigators who deal with fairly ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Ludbrook J

    更新日期:1995-12-01 00:00:00

  • L-arginine and aminoguanidine reduce colonic damage of acetic acid-induced colitis in rats: potential modulation of nuclear factor-κB/p65.

    abstract::The transcription factor, nuclear factor-κB (NF-κB) is a key inducer of inducible nitric oxide synthase (iNOS) gene expression. The aim of the present study was to investigate the potential protective effect of l-arginine (Arg; nitric oxide precursor) and aminoguanidine (inducible nitric oxide synthase inhibitor) agai...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Farghaly HS,Thabit RH

    更新日期:2014-10-01 00:00:00

  • Hantavirus diseases pathophysiology, their diagnostic strategies and therapeutic approaches: A review.

    abstract::Hantaviruses are enveloped negative (-) single-stranded RNA viruses belongs to Hantaviridae family, hosted by small rodents and entering into the human body through inhalation, causing haemorrhagic fever with renal syndrome (HFRS) and hantavirus pulmonary syndrome (HPS) also known as hantavirus cardiopulmonary syndrom...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Munir N,Jahangeer M,Hussain S,Mahmood Z,Ashiq M,Ehsan F,Akram M,Ali Shah SM,Riaz M,Sana A

    更新日期:2020-09-07 00:00:00

  • Deleterious effects of salt intake other than effects on blood pressure.

    abstract::1. Salt intake is not only known to play an important role in determining blood pressure (BP) but has been shown to have other deleterious effects independent of BP. 2. Epidemiological and animal studies have provided evidence that salt intake may have an adverse effect on stroke mortality independent of BP. 3. Signif...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Antonios TF,MacGregor GA

    更新日期:1995-03-01 00:00:00

  • Structure of human renin and expression of the renin gene.

    abstract::The amino acid sequence of human renin was identified for the first time. This was determined from the nucleotide sequence of exons in the human renin gene identified in a genomic library by recombinant DNA techniques. Examination of amino acid residues involved in the enzymatic hydrolysis by human renin of the unique...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Morris BJ,Catanzaro DF,Hardman J,Mesterovic N,Tellam J,Hort Y,Bennetts BH,Shine J

    更新日期:1984-07-01 00:00:00

  • Carotid body potentiation induced by intermittent hypoxia: implications for cardiorespiratory changes induced by sleep apnoea.

    abstract::1. The most usual form of chronic hypoxia in humans is the intermittent hypoxia resulting from obstructive sleep apnoea (OSA). The OSA syndrome is a highly prevalent sleep breathing disorder that is considered an independent risk factor for hypertension and cardiovascular diseases. Endothelial dysfunction, oxidative s...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Iturriaga R,Moya EA,Del Rio R

    更新日期:2009-12-01 00:00:00

  • Role of nitric oxide in the control of glomerular microcirculation.

    abstract::1. Nitric oxide (NO) plays an important role in the control of glomerular haemodynamics and is synthesized from the amino acid L-arginine by a family of enzymes, NO synthase (NOS). 2. Nitric oxide synthase is present in the endothelium and also in the macula densa, a plaque of specialized tubular epithelial cells. End...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Ito S,Carretero OA,Abe K

    更新日期:1997-08-01 00:00:00

  • Controlled study of the effects of dietary protein on blood pressure in normotensive humans.

    abstract::1. The object of this study was to determine whether meat protein per se is responsible for the higher blood pressures (BP) in omnivores compared with vegetarians. 2. Assessments were made by a double blind randomized control trial in 64 normotensive volunteers recruited from Royal Perth Hospital staff. 3. All volunte...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Prescott SL,Jenner DA,Beilin LJ,Margetts BM,Vandongen R

    更新日期:1987-03-01 00:00:00

  • Reperfusion injury in the human forearm is mild and not attenuated by short-term ischaemic preconditioning.

    abstract::1. Ischaemia-reperfusion (IR) injury is an important contributor to tissue damage and has been shown to be attenuated by preconditioning (PC) in some animal models. A recent report has suggested that the forearm can be used for the study of this phenomenon in humans. We aimed to reproduce and further characterize this...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 临床试验,杂志文章


    authors: Kilian JG,Nakhla S,Griffith K,Harmer J,Skilton M,Celermajer DS

    更新日期:2005-01-01 00:00:00

  • Serum dopamine beta-hydroxylase (D beta H) levels during tilting in patients with spinal cord injuries.

    abstract::The activity of dopamine-beta-hydroxylase (D beta H) in the serum was measured in patients with quadriplegia and in healthy subjects. We assume that the plasma D beta H levels reflect sympathetic tone. Quadriplegics had significantly lower D beta H levels at rest. After head-up tilting a significant decrease in D beta...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Ohry A,Rabinowitz R,Korczyn AD

    更新日期:1980-07-01 00:00:00

  • Sample size requirements for clinical trials of isolated systolic hypertension.

    abstract::1. This study investigated components of blood pressure variability in elderly subjects with isolated systolic hypertension (ISH) using both ambulatory blood pressure monitoring (ABPM) and casual clinic blood pressure measurement. These were then used to determine sample size requirements for clinical trials of differ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Silagy CA,McNeil JJ,McGrath BP

    更新日期:1992-05-01 00:00:00

  • Physiological role of large, Ca2+-activated K+ channels in human glomerular mesangial cells.

    abstract::1. Contraction assays and patch clamp methods were used to determine the role of K+ channels in the regulation of contractile tone of human mesangial cells (MC) in culture. 2. MC contraction was induced by vasoconstrictor agents, such as angiotensin II (AngII; 100 nmol/L) and glybenclamide (Glyb), but not by iberiotox...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Sansom SC,Stockand JD

    更新日期:1996-01-01 00:00:00

  • Characterization of lymphocyte beta 2-adrenoceptor signalling in patients with left ventricular volume overload disease.

    abstract::1. Studies using animal experimental models have suggested that the beta2-adrenoceptor is uncoupled in association with alterations in the expression of G-protein-coupled receptor kinases (GRK) 2/3 in heart failure. However, the functional expression of the components of this pathway in human disease has not been full...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Dzimiri N,Basco C,Moorji A,Afrane B,Al-Halees Z

    更新日期:2002-03-01 00:00:00

  • Tetanic fade during partial transmission failure produced by non-depolarizing neuromuscular blocking drugs in the cat.

    abstract::1. A comparison has been made of the effects of three acetylcholine antagonists--hexamethonium, tubocurarine and pancuronium--on maximal tetani of limb muscles of cats under chloralose anaesthesia. In most experiments, the indirectly stimulated soleus muscle was studied, but observations were also made on the tibialis...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Bowman WC,Webb SN

    更新日期:1976-11-01 00:00:00

  • Cardiac arrest temperature: the effect of ethyl alcohol and carbon dioxide on rats, guinea-pigs and isolated rat hearts.

    abstract::1. Previous clinical and experimental reports have suggested that the systemic administration of ethyl alcohol permits lower body temperatures before the onset of hypothermic cardiac arrest. 2. In the investigations described here, the effect of ethyl alcohol on the temperature at which cardiac arrest occurred in rats...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Duthie AM,White JF

    更新日期:1977-07-01 00:00:00

  • Effect of exercise on plasma adrenomedullin and natriuretic peptide levels in myocardial infarction.

    abstract::1. We investigated the effect of exercise on plasma adrenomedullin, atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP) concentrations and studied the relationship between these peptides and haemodynamic parameters in nine patients with old myocardial infarction (MI) and in eight normal subjects. 2. T...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Morimoto A,Nishikimi T,Takaki H,Okano Y,Matsuoka H,Takishita S,Kitamura K,Miyata A,Kangawa K,Matsuo H

    更新日期:1997-05-01 00:00:00

  • Agonist function of the recombinant alpha 4 beta 3 delta GABAA receptor is dependent on the human and rat variants of the alpha 4-subunit.

    abstract::1. It is known that the alpha(4)-subunit is likely to occur in the brain predominantly in alpha(4)beta(3)delta receptors at extrasynaptic sites. Recent studies have revealed that the alpha(1)-, alpha(4)-, gamma(2)- and delta-subunits may colocalize extrasynaptically in dentate granule cells of the hippocampus. In the ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Wang MD,Rahman M,Johansson IM,Bäckström T

    更新日期:2010-07-01 00:00:00

  • β-lactam pharmacokinetics and pharmacodynamics in critically ill patients and strategies for dose optimization: a structured review.

    abstract::1. Infections and related sepsis are two of the most prevalent issues in the care of critically ill patients, with mortality as high as 70%. Appropriate antibiotic selection, as well as adequate dosing, is important to improve the clinical outcome for these patients. 2. β-Lactams are the most common antibiotic class u...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Sinnollareddy MG,Roberts MS,Lipman J,Roberts JA

    更新日期:2012-06-01 00:00:00

  • Sympathetic rhythms and nervous integration.

    abstract::1. The present review focuses on some of the processes producing rhythms in sympathetic nerves influencing cardiovascular functions and considers their potential relevance to nervous integration. 2. Two mechanisms are considered that may account for rhythmic sympathetic discharges. First, neuronal elements of peripher...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Gilbey MP

    更新日期:2007-04-01 00:00:00

  • Effects of atropine on the time and frequency domain estimates of blood pressure and heart rate variability in mice.

    abstract::1. Indices quantifying blood pressure (BP) and heart rate (HR) variability have been recently developed and may be used to assess the contribution of the autonomic nervous system to cardiovascular fluctuations. 2. Cardiovascular variables were measured in eight conscious mice equipped with a BP telemetric device. Each...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Laude D,Baudrie V,Elghozi JL

    更新日期:2008-04-01 00:00:00

  • Activation of imidazoline-I3 receptors ameliorates pancreatic damage.

    abstract::Agmatine, an endogenous ligand of imidazoline receptors, is reported to exhibit anti-hyperglycaemic and many other effects. It has been established that the imidazoline I3 receptor is involved in insulin secretion. The current study characterizes the role of the imidazoline I3 receptor in the protection of pancreatic ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Li Y,Cheng KC,Asakawa A,Amitani H,Takimoto Y,Runtuwene J,Inui A

    更新日期:2015-09-01 00:00:00

  • Effect of plasma cholesterol on red blood cell oxygen transport.

    abstract::1. Oxygen (O2) transfer from the blood to tissues is a function of the red blood cell (RBC) O2 saturation (SO2), the plasma O2 content being negligible. Under conditions of increased tissue O2 demand, the SO2 of arterial blood does not change appreciably (97%); however, the SO2 of mixed venous blood, equal to that of ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Buchwald H,O'Dea TJ,Menchaca HJ,Michalek VN,Rohde TD

    更新日期:2000-12-01 00:00:00

  • Antisense oligonucleotides: from design to therapeutic application.

    abstract::1. An antisense oligonucleotide (ASO) is a short strand of deoxyribonucleotide analogue that hybridizes with the complementary mRNA in a sequence-specific manner via Watson-Crick base pairing. Formation of the ASO-mRNA heteroduplex either triggers RNase H activity, leading to mRNA degradation, induces translational ar...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Chan JH,Lim S,Wong WS

    更新日期:2006-05-01 00:00:00

  • Dissociation of blood pressure and sympathetic activation of renin release in sinoaortic-denervated rats.

    abstract::1. Blood pressure (BP) and heart rate (HR) increase 6 and 24 h after sinoaortic baroreceptor denervation (SAD), whereas plasma renin activity (PRA) and renal renin mRNA levels remain unchanged. We postulated that a simultaneous rise in BP could offset the expected activation of renin associated with an increased renal...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Krieger MH,Moreira ED,Oliveira EM,Oliveira VL,Krieger EM,Krieger JE

    更新日期:2006-05-01 00:00:00

  • Opioid receptors mediate inotropic and depressor effects of apelin in rats with 2K1C-induced chronic renovascular hypertension.

    abstract::Apelin receptors (APJ) cross-talk with other G-protein-coupled receptors. However, the role of APJ interaction with opioid receptors (OPR) on the cardiovascular effects of apelin in hypertension is not clear. Renovascular hypertension was induced by placing a Plexiglas clip on the left kidney of rats. After 16 weeks, ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Rostamzadeh F,Najafipour H,Yeganeh-Hajahmadi M,Joukar S

    更新日期:2018-02-01 00:00:00

  • Effects of brain lesions on the antinociceptive properties of morphine in rats.

    abstract::1. Electrolytic lesions were made in various brain regions of the rat, and the effects of these lesions on nociceptive threshold and the antinociceptive actions of morphine were tested using a shock titration technique. 2. Lesions in the medial thalamus, the periaqueductal grey area, or the caudate nucleus, had no eff...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Yeung JC,Yaksh TL,Rudy TA

    更新日期:1975-05-01 00:00:00

  • Effects of glutamate transport substrates and glutamate receptor ligands on the activity of Na-/K(+)-ATPase in brain tissue in vitro.

    abstract::1. It has been suggested that Na+/K(+)-ATPase and Na(+)-dependent glutamate transport (GluT) are tightly linked in brain tissue. In the present study, we have investigated Na+/K(+)-ATPase activity using Rb+ uptake by 'minislices' (prisms) of the cerebral cortex. This preparation preserves the morphology of neurons, sy...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Nanitsos EK,Acosta GB,Saihara Y,Stanton D,Liao LP,Shin JW,Rae C,Balcar VJ

    更新日期:2004-11-01 00:00:00

  • Comparison of digoxin versus low-dose amiodarone for ventricular rate control in patients with chronic atrial fibrillation.

    abstract::1. Rapid ventricular rate (VR) and rhythm irregularity during atrial fibrillation (AF) impair cardiac performance. Although digoxin has been widely used in patients with AF, its efficacy for the control of VR and rhythm irregularity is unsatisfactory. Whether low-dose amiodarone is more effective remains unclear. 2. W...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Tse HF,Lam YM,Lau CP,Cheung BM,Kumana CR

    更新日期:2001-05-01 00:00:00