The actions of some cholinomimetic drugs on the isolated taenia of the guinea-pig caecum.

Abstract:

:1. The actions on the taenia of 4-(m-chlorophenylcarbamoyloxy)-2-butynyl-trimethylammonium chloride (McN-A-343), N-benzyl-3-pyrrolidyl acetate methobromide (AHR-602), tetramethylammonium (TMA) and choline phenyl ether have been examined and compared with the actions of acetylcholine, nicotine and 1,1-dimethyl-4-phenylpiperazinium (DMPP).2. Responses of the taenia to these agonists are quantitatively and often qualitatively dependent on the tone of the preparation. A method is described which makes allowance for the effect of tone on heights of contractions.3. Acetylcholine, McN-A-343 and AHR-602 produced only contractions; TMA produced contractions or biphasic responses; and choline phenyl ether, nicotine and DMPP produced contractions, relaxations or biphasic responses.4. The mode of action of these compounds has been analysed by means of hyoscine, ganglion-blocking drugs, tetrodotoxin and local anaesthetics.5. It is concluded that acetylcholine, McN-A-343, AHR-602, TMA and choline phenyl ether act on muscarinic receptors in the smooth muscle. Choline phenyl ether has an additional action on nicotinic receptors of cholinergic neurones. Nicotine and DMPP act on nicotinic receptors of cholinergic neurones and of inhibitory neurones. An action on the latter is sometimes also seen with TMA and choline phenyl ether.6. With nicotine or DMPP, and TMA or choline phenyl ether in the presence of hyoscine, part of the contraction phase of biphasic responses (in which a contraction follows relaxation) is best explained as being triggered by the initial relaxation-that is, as a "rebound contraction".7. None of the compounds tested appeared to exert an atropine-sensitive action on neurones.8. In the presence of hyoscine high concentrations of agonists can act on sites not involved with lower concentrations.

journal_name

Br J Pharmacol

authors

Hobbiger F,Mitchelson F,Rand MJ

doi

10.1111/j.1476-5381.1969.tb08303.x

subject

Has Abstract

pub_date

1969-05-01 00:00:00

pages

53-69

issue

1

eissn

0007-1188

issn

1476-5381

journal_volume

36

pub_type

杂志文章
  • Endocannabinoid modulation by FAAH and monoacylglycerol lipase within the analgesic circuitry of the periaqueductal grey.

    abstract:BACKGROUND AND PURPOSE:Endogenous cannabinoids (endocannabinoids) in the periaqueductal grey (PAG) play a vital role in mediating stress-induced analgesia. This analgesic effect of endocannabinoids is enhanced by pharmacological inhibition of their degradative enzymes. However, the specific effects of endocannabinoids ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12839

    authors: Lau BK,Drew GM,Mitchell VA,Vaughan CW

    更新日期:2014-12-01 00:00:00

  • Developmental responses to opioids reveals a lack of effect on stress-induced corticosterone levels in neonatal rats.

    abstract::The neonate has an unusual capacity for survival and the possibility exists that mechanisms for controlling stress responses may differ in the developing animal. In adults both endogenous and exogenous opioids can modulate the corticosterone responses to stress. We have studied this effect in neonatal rats and found t...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1987.tb08990.x

    authors: Bailey CC,Kitchen I

    更新日期:1987-05-01 00:00:00

  • Effect of pertussis toxin on A1-receptor-mediated inhibition of insulin secretion.

    abstract::Previous studies have provided evidence for the presence on B cell membrane of adenosine receptors (P1-purinoceptors) of the A1-subtype which inhibit insulin secretion. In this work we have investigated the implication of a guanosine triphosphate (GTP) binding protein (G protein) in the A1 purinoceptor-induced inhibit...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1989.tb11775.x

    authors: Hillaire-Buys D,Gross R,Loubatières-Mariani MM,Ribes G

    更新日期:1989-01-01 00:00:00

  • Prostaglandin endoperoxide-dependent vasospasm in bovine coronary arteries after nitration of prostacyclin synthase.

    abstract::In the present study we used a bioassay to study the effects of peroxynitrite (ONOO-) on angiotensin II (A-II)-triggered tension in isolated bovine coronary arteries in order to show the consequences of the previously reported PGI2-synthase inhibition by ONOO- in this model. The following results were obtained: 1. 1 m...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702434

    authors: Zou M,Jendral M,Ullrich V

    更新日期:1999-03-01 00:00:00

  • The role of nitric oxide in the regional vasodilator effects of endothelin-1 in the rat.

    abstract::1. The role of nitic oxide (NO) derived from L-arginine in the regional vasodilator effects of endothelin-1 has been investigated in anaesthetized, spontaneously hypertensive (SH) rats in which autonomic reflexes were abolished by ganglion blockade. The experimental design incorporated animals infused with phenylephri...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1992.tb09049.x

    authors: Fozard JR,Part ML

    更新日期:1992-03-01 00:00:00

  • Electrophysiological effects of diprafenone, a dimethyl congener of propafenone on guinea-pig ventricular cells.

    abstract::1. The effects of diprafenone and propafenone on transmembrane action potential were examined and compared in papillary muscles and single ventricular myocytes isolated from guinea-pig hearts. 2. In papillary muscles, both diprafenone and propafenone > or = 10(-6) M caused a significant and dose-dependent decrease in ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1992.tb14529.x

    authors: Kodama I,Suzuki R,Honjo H,Toyama J

    更新日期:1992-11-01 00:00:00

  • Adrenal origin of plasma catecholamines after decapitation: a study in normal and diabetic rats.

    abstract::The concentrations of catecholamines and the activities of dopamine-beta-hydroxylase were measured in blood obtained from decapitated diabetic and aged-matched control rats. The activity of dopamine-beta-hydroxylase in blood from diabetic rats was much greater (5 fold) than that seen for control rats. For both diabeti...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1978.tb08632.x

    authors: Berkowitz BA,Head RJ

    更新日期:1978-09-01 00:00:00

  • Effects of GABA and various allosteric ligands on TBPS binding to cloned rat GABA(A) receptor subtypes.

    abstract::1. [35S]t-butylbicyclophosphorothionate (TBPS) is a high affinity ligand for the picrotoxin site of GABA(A) receptors. Here we examined TBPS binding to the cloned receptors made of alpha 1, alpha 3 or alpha 6 in combination with beta 2 or beta 2 and gamma 2 subunits, in the presence of GABA and several allosteric liga...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb13185.x

    authors: Im WB,Pregenzer JF,Thomsen DR

    更新日期:1994-08-01 00:00:00

  • Mechanism of neuromuscular blockade induced by phenthonium, a quaternary derivative of (-)-hyoscyamine, in skeletal muscles.

    abstract::1. The mechanisms underlying the postjunctional blockade induced by phenthonium [N-(4-phenyl) phenacyl 1-hyoscyamine] were investigated in mammalian and amphibian muscles. This muscarinic antagonist was previously shown to enhance specifically the spontaneous acetylcholine (ACh) release at concentrations that blocked ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701932

    authors: Souccar C,Lima-Landman MT,Ballejo G,Lapa AJ

    更新日期:1998-07-01 00:00:00

  • Inhibitory effect of sodium cromoglycate on pulmonary responses to histamine administered after indomethacin in anaesthetized guinea-pigs.

    abstract::1. Histamine (2-4 micrograms kg-1 i.v.) increased airways resistance (Raw) and decreased dynamic lung compliance (Cdyn) in urethane-anaesthetized guinea-pigs. The effects on Raw were almost abolished by atropine (0.1 mg kg-1 i.v.) and reduced by vagal cooling (11-16 degrees C). 2. Histamine-induced changes in Raw and ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1988.tb11555.x

    authors: Mitchell HW

    更新日期:1988-06-01 00:00:00

  • Effect of L-arginine/nitric oxide pathway on MPP(+)-induced cell injury in the striatum of rats.

    abstract::1. Protection against 1-methyl-4-phenylpyridinium ion (MPP+) neurotoxicity by two nitric oxide-related compounds, N omega-nitro-L-arginine (L-NOARG) and L-arginine, was studied in the corpus striatum by means of two MPP+ perfusions separated by 24 h. Dopamine extracellular output after the second MPP+ (1, 5 and 10 mM)...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb14814.x

    authors: Santiago M,Machado A,Cano J

    更新日期:1994-03-01 00:00:00

  • Anti-inflammatory, membrane-stabilizing interactions of salmeterol with human neutrophils in vitro.

    abstract::1. We have investigated the effects of salmeterol (0.3-50 microM) on several pro-inflammatory activities of human neutrophils in vitro. 2. Oxidant production by FMLP- and calcium ionophore (A23187)-activated neutrophils was particularly sensitive to inhibition by low concentrations (0.3-3 microM) of salmeterol, while ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15297.x

    authors: Anderson R,Feldman C,Theron AJ,Ramafi G,Cole PJ,Wilson R

    更新日期:1996-04-01 00:00:00

  • A comparison of the inhibitory effects of sodium nitroprusside, pinacidil and nifedipine on pressor response to NG-nitro-L-arginine.

    abstract::1. The inhibitory effects of sodium nitroprusside (SNP), a nitric oxide (NO) donor, on mean arterial pressure (MAP) responses to NG-nitro-L-arginine (L-NNA) (NO synthase inhibitor), angiotensin II (AII) and noradrenaline (NA) were compared with those of pinacidil (KATP channel opener) and nifedipine (L-type calcium an...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb12816.x

    authors: Wang YX,Zhou T,Pang CC

    更新日期:1993-02-01 00:00:00

  • A comparison of the anti-anaphylactic activities of salbutamol and disodium cromoglycate in the rat, the rat mast cell and in human lung tissue.

    abstract::1 Salbutamol and disodium cromoglycate were compared for anti-anaphylactic activity against passive anaphylaxis in rat skin and peritoneum in vivo and in rat mast cells and human lung fragments in vitro.2 Salbutamol administered intravenously to rats inhibited cutaneous anaphylaxis, but also inhibited cutaneous respon...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:

    authors: Butchers PR,Fullarton JR,Skidmore IF,Thompson LE,Vardey CJ,Wheeldon A

    更新日期:1979-09-01 00:00:00

  • Altered pharmacology of native rodent spinal cord TRPV1 after phosphorylation.

    abstract:BACKGROUND AND PURPOSE:Evidence suggests that phosphorylation of TRPV1 is an important component underlying its aberrant activation in pathological pain states. To date, the detailed pharmacology of diverse TRPV1 receptor agonists and antagonists has yet to be reported for native TRPV1 under phosphorylating conditions....

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12005

    authors: Mogg AJ,Mill CE,Folly EA,Beattie RE,Blanco MJ,Beck JP,Broad LM

    更新日期:2013-02-01 00:00:00

  • G protein-coupled receptor kinase 6 (GRK6) selectively regulates endogenous secretin receptor responsiveness in NG108-15 cells.

    abstract::1. To determine the role of G protein-coupled receptor kinases (GRKs) in the regulation of endogenous secretin receptor responsiveness, we have transiently overexpressed both wild-type (WT) and dominant negative mutant (DNM) GRKs in NG108-15 mouse neuroblastoma x rat glioma hybrid cells and investigated the effects of...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705101

    authors: Ghadessy RS,Willets JM,Kelly E

    更新日期:2003-02-01 00:00:00

  • Characterization of the binding of DL-[3H]-2-amino-4-phosphonobutyrate to L-glutamate-sensitive sites on rat brain synaptic membranes.

    abstract::The binding of DL-[3,4-3H] 2-amino-4-phosphonobutyric acid DL[3H]-APB to rat whole brain synaptic membranes was investigated. Binding was linear with membrane protein concentration, and optimal at physiological pH and temperature. The association rate was rapid, achieving equilibrium within 10 min. Prolonged incubatio...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1983.tb10041.x

    authors: Butcher SP,Collins JF,Roberts PJ

    更新日期:1983-10-01 00:00:00

  • Modulation of the isoprenaline-induced membrane hyperpolarization of mouse skeletal muscle cells.

    abstract::1. The hyperpolarization of the resting membrane potential, Vm, induced by isoprenaline in the lumbrical muscle fibres of the mouse, was investigated by use of intracellular microelectrodes. 2. In normal Krebs-Henseleit solution (potassium concentration: K+o = 5.7 mM, 'control'), Vm was -7.40 +/- 0.2 mV; lowering K+o ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb15940.x

    authors: van Mil HG,Kerkhof CJ,Siegenbeek van Heukelom J

    更新日期:1995-12-01 00:00:00

  • Human podocytes express functional thermosensitive TRPV channels.

    abstract:BACKGROUND AND PURPOSE:Heat-sensitive transient receptor potential vanilloid (TRPV) channels are expressed in various epithelial tissues regulating, among else, barrier functions. Their expression is well established in the distal nephron; however, we have no data about their presence in podocytes. As podocytes are ind...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14052

    authors: Ambrus L,Kelemen B,Szabó T,Bíró T,Tóth BI

    更新日期:2017-12-01 00:00:00

  • Comparative effects of continuous infusion of mCPP, Ro 60-0175 and d-fenfluramine on food intake, water intake, body weight and locomotor activity in rats.

    abstract::1. The aim of the study was to compare the effects of 14 day subcutaneous infusion of the 5-HT(2C) receptor agonists, m-chlorophenylpiperazine (mCPP, 12 mg kg(-1) day(-1)) and Ro 60-0175 (36 mg kg(-1) day(-1)) and the 5-HT releasing agent and re-uptake inhibitor, d-fenfluramine (6 mg kg(-1) day(-1)), on food and water...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703443

    authors: Vickers SP,Benwell KR,Porter RH,Bickerdike MJ,Kennett GA,Dourish CT

    更新日期:2000-07-01 00:00:00

  • The effects of formoterol on plasma exudation produced by a localized acute inflammatory response to bradykinin in the tracheal mucosa of rats in vivo.

    abstract::1. The effects of formoterol, a beta 2-adrenoceptor agonist, on plasma protein exudation and microvascular permeability induced by topical, i.e. applied onto the tracheal mucosal surface, bradykinin (10 nmol; 20 microM, 5 min, 0.1 ml min-1) were studied in a perfused segment of trachea prepared in situ in anaesthetize...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb16374.x

    authors: O'Donnell SR,Anderson GP

    更新日期:1995-09-01 00:00:00

  • A facilitatory effect of bicuculline on the enteric neurones in the guinea-pig isolated colon.

    abstract::Changes in the efficiency of the peristaltic reflex, acetylcholine (ACh) output and motor responses to transmural and periarterial nerve stimulation produced by bicuculline and gamma-aminobutyric acid (GABA) receptor desensitization were investigated in the guinea-pig isolated colon. Bicuculline, at concentrations una...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1987.tb16822.x

    authors: Frigo GM,Galli A,Lecchini S,Marcoli M

    更新日期:1987-01-01 00:00:00

  • Antithrombotic activity of a monoclonal antibody inducing the substrate form of plasminogen activator inhibitor type 1 in rat models of venous and arterial thrombosis.

    abstract::1. Elevated plasminogen activator inhibitor 1 (PAI-1) is a risk factor for thrombosis, and inhibitors of the interaction between PAI-1 and tissue plasminogen activator (t-PA) have antithrombotic and prothrombolytic activity in animals. We describe the antithrombotic effects in the rat of a monoclonal antibody (MA33H1)...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702030

    authors: Berry CN,Lunven C,Lechaire I,Girardot C,O'Connor SE

    更新日期:1998-09-01 00:00:00

  • Excessive stimulation of poly(ADP-ribosyl)ation contributes to endothelial dysfunction in pre-eclampsia.

    abstract::1. Pre-eclampsia is a serious pregnancy disorder associated with widespread activation of the maternal vascular endothelium. Recent evidence implicates a role for oxidative stress in the aetiology of this condition. 2. Reactive oxygen species, particularly superoxide anions, invokes endothelial cell activation through...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0706055

    authors: Crocker IP,Kenny LC,Thornton WA,Szabo C,Baker PN

    更新日期:2005-03-01 00:00:00

  • Heparin-insensitive calcium release from intracellular stores triggered by the recombinant human parathyroid hormone receptor.

    abstract::1. In the present study we have characterized the parathyroid hormone (PTH)-induced calcium signalling in 293 cells stably transfected with the human PTH receptor cDNA. In these cells, human PTH-1(1-38) strongly stimulates adenosine 3':5'-cyclic monophosphate (cyclic AMP) formation (EC50 = 0.39 nM) but fails to activa...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb14947.x

    authors: Seuwen K,Boddeke HG

    更新日期:1995-04-01 00:00:00

  • Effects of anticonvulsants in vivo on high affinity choline uptake in vitro in mouse hippocampal synaptosomes.

    abstract::The effects of several anticonvulsant drugs on sodium-dependent high affinity choline uptake (HACU) in mouse hippocampal synaptosomes was investigated. HACU was measured in vitro after in vivo administration of the drug to mice. HACU was inhibited by drugs which have in common the ability to facilitate gamma-aminobuty...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:

    authors: Miller JA,Richter JA

    更新日期:1985-01-01 00:00:00

  • Glucocorticoids potently block tumour necrosis factor-alpha- and lipopolysaccharide-induced apoptotic cell death in bovine glomerular endothelial cells upstream of caspase 3 activation.

    abstract::1. Endothelial cell damage in glomeruli and kidney arterioles appears to play a pivotal role in glomerular inflammatory diseases. Glomerular endothelial cells, a specialized microvascular cell type involved in the regulation of glomerular ultrafiltration, die by apoptosis in response to tumour necrosis factor-alpha (T...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702726

    authors: Messmer UK,Winkel G,Briner VA,Pfeilschifter J

    更新日期:1999-08-01 00:00:00

  • Cardiac NO signalling in the metabolic syndrome.

    abstract::It is well documented that metabolic syndrome (i.e. a group of risk factors, such as abdominal obesity, elevated blood pressure, elevated fasting plasma glucose, high serum triglycerides and low cholesterol level in high-density lipoprotein), which raises the risk for heart disease and diabetes, is associated with inc...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.12960

    authors: Pechánová O,Varga ZV,Cebová M,Giricz Z,Pacher P,Ferdinandy P

    更新日期:2015-03-01 00:00:00

  • The partial purification and bioassay of a toxin present in extracts of the sea anemone, Tealia felina (L.).

    abstract::1. Column chromatography with Agarose A50m followed by Sephadex G100 was used to separate a fraction (extract II) in the molecular weight range 12,000 to 14,000 daltons from saline extracts of the sea anemone, Tealia felina. 2. Extract II inhibited histamine-induced contractions of the guinea-pig ileum and produced ha...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1981.tb09115.x

    authors: Aldeen SI,Elliott RC,Sheardown M

    更新日期:1981-02-01 00:00:00

  • Stimulating action of atropine on the release of acetylcholine by rat cerebral cortex in vitro.

    abstract::1. In cortical slices from rat brain incubated in a medium containing the irreversible cholinesterase inhibitor, soman (0.005 mM) and a high concentration of KCl (25 mM), atropine exerts a stimulating action on the release of acetylcholine (ACh).2. Two possible explanations for this action were examined. Atropine migh...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1971.tb07068.x

    authors: Polak RL

    更新日期:1971-04-01 00:00:00