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A STUDY OF STIMULATION‐EVOKED ACTIVATION OF α2‐ADRENOCEPTORS IN THE RAT ISOLATED VAS DEFERENS |
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Clinical and Experimental Pharmacology and Physiology,
Volume 10,
Issue 4,
1983,
Page 381-393
Jocelyn N. Pennefather,
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摘要:
SUMMARY1. Experiments were performed with prostatic and epididymal segments of rat vas deferens to determine whether α2‐adrenoceptors in this organ were activated during field stimulation of sympathetic terminals with short trains of pulses applied at low frequencies.2. In prostatic segments the magnitude of twitches evoked by trains of ten field pulses at 1 or 2 Hz declined after 2–3 s of stimulation. In contrast, facilitation of twitches and fusion of contractions occurred when similar stimulation was applied to epididymal segments.3. In prostatic segments from rats treated with reserpine (2.5 mg/kg i.p.) 24 h previously, there was no decline in the magnitude of twitches produced by successive impulses in a train of stimulating pulses. In epididymal segments from reserpine‐treated rats facilitation of twitches in response to successive impulses in each train still occurred.4. In prostatic segments cocaine (5 and 10 μmol/1) enhanced twitch fade with stimulation at 1 and 2 Hz without altering the time for onset of this effect. In epididymal segments cocaine led to enhancement and prolongation of contractile responses.5. In prostatic segments yohimbine (0.01–0.06 μmol/l) reduced or reversed the effect of cocaine in enhancing twitch fade. In preparations where the reversal of the effect of cocaine by yohimbine was incomplete, subsequent addition of phentolamine (1 μmol/l) produced complete reversal.6. In epididymal segments yohimbine (0.01 μmol/l) produced a further enhancement in the twitch responses to stimulation at 1 and 2 Hz. Subsequent addition of phentolamine (1 μmol/l) reversed the facilitatory effects of cocaine and yohimbine.7. Propranolol (10 μmol/l) was without effect upon responses to stimulation in either segment of rat vasa deferentia.8. These experiments indicate that noradrenaline, released by short trains of impulses applied at low frequency to hypogastric nerve terminals activates prejuctional α2‐adrenoceptors in the prostatic segment of the vas deferens. In the epididymal portion the effects arising from activation of prejunctional α2‐adrenoceptors are outweighed by the consequences of activation of extrajunctional α1‐adrenoceptors located on longitu
ISSN:0305-1870
DOI:10.1111/j.1440-1681.1983.tb00843.x
出版商:Blackwell Publishing Ltd
年代:1983
数据来源: WILEY
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QUANTITATIVE STRUCTURE‐ACTIVITY RELATIONSHIPS OF IMIDAZOLIDINE DERIVATIVES RELATED TO CLONIDINE AT PERIPHERAL α‐ADRENOCEPTORS |
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Clinical and Experimental Pharmacology and Physiology,
Volume 10,
Issue 4,
1983,
Page 395-410
I. C. Medgett,
M. W. McCulloch,
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摘要:
SUMMARY1. The effects of clonidine, oxymetazoline and thirteen substituted phenyl‐iminoimidazolidine analogues of clonidine were studied and compared on postjunctional α‐adrenoceptors in guinea‐pig and rabbit aorta and on prejunctional α‐adrenoceptors in guinea‐pig atria.2. In the aorta all compounds were partial agonists at postjunctional α‐adrenoceptors. Correlation of agonist potency with various combinations of their physicochemical parameters showed that, with the present series of compounds, physicochemical parameters alone determined 92% of the variance in the data with potency being primarily and highly correlated with pKa.3. Similarly in atria, all compounds, with the possible exceptions of St 95 and St 1943, appeared to be partial agonists at prejunctional α‐adrenoceptors; transmitter noradrenaline release could either be inhibited (field stimulation at 1 Hz for 5 s) or enhanced (5 Hz for 30 s).4. The results indicate that 2,6‐substitution in the phenyl ring appears to be a specific non‐physicochemical activity‐enhancing factor at prejunctional but not postjunctional α‐adrenoceptors.5. A comparison with data in the literature giving the acute hypotensive potencies of the compounds suggests that central α‐adrenoceptors may more closely resemble atrial prejunctional α‐adrenoceptors than aortic postjunctional α‐adrenoceptors.6. Quantitative correlations between centrally‐mediated hypotensive and peripheral vasoconstrictor effects of clonidine‐like imidazolidines do not provide a sufficiently sensitive method of disting
ISSN:0305-1870
DOI:10.1111/j.1440-1681.1983.tb00844.x
出版商:Blackwell Publishing Ltd
年代:1983
数据来源: WILEY
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PHARMACOKINETICS OF AN OSMOTICALLY CONTROLLED DELIVERY INDOMETHACIN PREPARATION IN NORMAL VOLUNTEERS |
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Clinical and Experimental Pharmacology and Physiology,
Volume 10,
Issue 4,
1983,
Page 411-414
J. V. Bertouch,
S. Maycock,
B. Harrington,
P. M. Brooks,
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摘要:
SUMMARYIndomethacin is still used commonly for the treatment of rheumatic diseases but is associated with side effects, particularly headache, in a number of patients. A controlled or sustained release formulation of indomethacin might provide lower peak plasma levels and thus reduce side effects while still maintaining adequate plasma levels to control pain and inflammation.In this single dose crossover study, normal volunteers received the new formulation of indomethacin (Indocid GITS 6/85) fasting or with a standard meal, indomethacin 75 mg with a standard meal or indomethacin 25 mg three times daily with a standard meal.Plasma concentration data showed that peak plasma levels were reduced but the area under the plasma concentration curve was not significantly different between the four treatments.
ISSN:0305-1870
DOI:10.1111/j.1440-1681.1983.tb00845.x
出版商:Blackwell Publishing Ltd
年代:1983
数据来源: WILEY
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4. |
INFLUENCE OF SEASON AND ANAESTHETIC ON CUTANEOUS VASCULAR PERMEABILITY RESPONSES TO HISTAMINE, SEROTONIN AND MAST CELL‐RELEASING AGENTS IN RATS |
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Clinical and Experimental Pharmacology and Physiology,
Volume 10,
Issue 4,
1983,
Page 415-420
Loris A. Chahl,
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摘要:
SUMMARYThe influences of season and anaesthetic on the cutaneous vascular permeability responses to histamine (2.5 × 10−8mol), serotonin (5HT, 2.5 × 10−10mol), and to the mast cell‐releasing agents adenosine 51‐triphosphate (2.5 × 10−7mol), dextran (5 × 10−5g) and compound 48/80 (1 × 10−7g) were examined using an Evans blue dye leakage technique.In rats anaesthetized with urethane (1 g/kg i.p.), responses to irritants were significantly less than in rats given ether for the period of administration of irritants and allowed to recover consciousness. The response to histamine was mediated by Hi‐receptors since it was abolished by mepyramine but not by metiamide.The only seasonal variation observed was in responses to 5HT in urethane‐anaesthetized rats, which were significantly less in winter than in summer. It was concluded that dye leakage responses to irritants are affected more by anaesthetic than
ISSN:0305-1870
DOI:10.1111/j.1440-1681.1983.tb00846.x
出版商:Blackwell Publishing Ltd
年代:1983
数据来源: WILEY
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LEAKAGE OF CATECHOLAMINES FROM RABBIT CEREBROSPINAL FLUID FOLLOWING INTRACEREBROVENTRICULAR INJECTION |
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Clinical and Experimental Pharmacology and Physiology,
Volume 10,
Issue 4,
1983,
Page 421-425
C. Maccarrone,
E. Malta,
C. Raper,
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摘要:
SUMMARY1. The intracerebroventricular (i.c.v.) injection of (‐)‐isoprenaline and the selective β1‐adrenoceptor agonist, RO363, elicited reproducible dose‐related increases in heart rate in unanaesthetized and anaesthetized rabbits. (‐)‐Isoprenaline produced vasodepressor effects in unanaesthetized animals, whereas both catecholamines decreased blood pressure in anaesthetized rabbits.2. Pretreatment with guanethidine sulphate (5 mg/kg i.v.) reduced but did not abolish the tachycardia elicited by i.c.v. RO363, whereas heart rate responses to i.c.v. (‐)‐isoprenaline were unaffected.3. Pretreatment of anaesthetized rabbits with hexamethonium bromide (10 mg/kg i.v.) did not markedly affect the tachycardia elicited by i.c.v. RO363 and reduced the response to i.c.v. (‐)‐isoprenaline in only one out of five experiments.4. The results suggest that there is a marked leakage of centrally administered catecholamines into the peripheral circulation and that the rabbit may be unsuited for examining centrally mediated cardiovascular effec
ISSN:0305-1870
DOI:10.1111/j.1440-1681.1983.tb00847.x
出版商:Blackwell Publishing Ltd
年代:1983
数据来源: WILEY
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6. |
PROCEEDINGS OF THE AUSTRALIAN SOCIETY FOR MEDICAL RESEARCH |
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Clinical and Experimental Pharmacology and Physiology,
Volume 10,
Issue 4,
1983,
Page 427-496
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摘要:
1.The adult sleep apnoea syndromes.C. E. Sullivan2.The influence of prenatal factors on brainstem maturation and apnoea in infants.D. J. Henderson‐Smart, A. G. Pettigrew, D. J. Campbell and D. A. Edwards3.The ventilatory response to hypoxia: implications for mountaineers and patients with chronic lung disease.M. C. F. Pain4.Macrophage differentiation.William F. Doe5.The role of protein phosphorylation in the control of cell growth and differentiation.S. A. Livesey, K. W. Ng, N. C. Partridge and T. J. Martin6.Polyamines may maintain the structural integrity of chromosomes during cell division. A. W.Braithwaite7.Identification of antigens of parasites with immunodiagnostic or vaccination potential in malaria and schistosomiasis.G. F. Mitchell8.Necrotizing enteritis in Papua New Guinea and the isolation ofClostridium welchiitype C.G. Lawrence9.Cholera: remaining problems and prospects for their solution.D. Rowley10.Intratesticular regulatory mechanisms.D. M. De Kretser11.T Cell‐derived lymphokines in the regulation of lymphoid and haemopoietic cells.J. W. Schrader, I. Clark‐Lewis and G. H. W. Wong12.Acetylcholine hydrolyses certain neuropeptides.I. W. Chubb, E. Ranieri and A. J. Hodgson13.Mechanisms of heparin induced thrombocytopenia and thrombosis.B. H. Chong and P. A. Castaldi14.Effects of nifedipine, verapamil and diltiazem on calmodulin mediated, calcium stimulation of phosphodiesterase activity.M. J. Daly, S. E. Perry and W. G. Nayler15.Lymphocyte cytogenetics in breast cancer patients receiving adjuvant chemotherapy.E. J. Stephan, M. H. N. Tattersall, R. S. U. Baker and C. B. Gillies16.Persistence of alkylation induced alkali‐labile sites in DNA from human peripheral lymphocytes.V. C. Griffith and D. R. Turner17.Cytosine arabinoside transport and cytosine arabinoside triphosphate formation in acute leukaemia.J. M. Taupin, J. S. Wiley and W. H. Sawyer18.Angiotensin converting enzyme (ACE) induction in the rat by enalapril (MK 421). B.Jackson, R. Cubela and C. I. Johnston19.Effect of the histamine H2 receptor antagonist, cimetidine, on human T lymphocyte suppressor cell function.L. A. Butterworth, W. G. E. Cooksley, J. W. Halliday, W. J. Halliday, J. F. Kerr and L. W. Powell20.Deoxycoformycin induced metabolic changes in T cell chronic lymphocytic leukaemia. L.Hallam, M. B. Van der Weyden, A. S. Bagnara, S. Ackland and M. G. Whiteside21. In vitrouptake of57Co‐cyanocobalamin.E. Bowman, L. Butterworth, W. G. E. Cooksley and J. S. D. Scott22.Isolation and characterization of an hepatic ferritin receptor.U. Mack, L. W. Powell and J. W. Halliday23.Down‐regulation by growth hormone of specific growth hormone receptors on mouse fibroblasts.L. J. Murphy, E. Vrhovsek and L. Lazarus24.Effects of 1,25‐dihydroxyvitamin D3 on cultured human cancer cells.R. J. Frampton, S. Omond and J. A. Eisman25.Oestrogen and androgen receptors in guinea‐pig prostrate epithelium and stroma.W. D. Tilley, D. J. Horsfall and V. R. Marshall26.Some properties of a high affinity, microsomal binding site for tamoxifen and other structurally related nonsteroidal compounds.C. K. W. Watts, L. C. Murphy and R. L. Sutherland27.Antitumor activity of nonsteroidal antioestrogensin vitro:relationship to affinity for oestrogen receptor (ER) and another high affinity ‘antioestrogen binding site’ (AEBS).L. C. Murphy and R. L. Sutherland28.Regulation of transferrin receptor expression in human tumour cells.D. Hedley, E. Musgrove, C. Rugg and I. Taylor29.Differences in calcium handling between matrix vesicle enriched microsomes and more purified vesicles.R. Shankar and J. D. Sallis30.A calmodulin‐stimulated (Ca2+‐Mg2+)‐ATPase in cultured B but not T lymphoblasts.L. C. Wright and R. M. Fox31.Suppression of autoantibody production lost by exposing suppressor cells to the foreign antigens inducing the autoimmunity.K. O. Cox and Anne Howies32.Cytotoxic and cell cycle effects of adenosine analogues on dividing and nondividing human lymphoid cells.R. F. Kefford and R. M. Fox33.The intracellular factor XIII activity of platelets during platelet activation.G. W. Lynch and S. L. Pfueller34.Kupffer cell synthesis of chemotactic factors and cirrhosis of the liver.C. Mclvor, G. Cooksley, G. Grotendorst, G. Martin, J. Hoofnagle and E. A. Jones35.Detection of mutant human lymphocytes.A. Morley, K. Trainor, J. Dempsey, R. Seshadri and R. G. Ryall36.Granulocyte‐monocyte interactions in man.M. A. Vadas and L. Callegaro37.Studies on phosphoglycerate kinase deficiency.L. G. Svirklys and W. J. O'Sullivan42.Hereditary spherocytosis of man: functional identification of an abnormal cytoskeletal protein.J. S. Hill, W. H. Sawyer, G. J. Howlett and J. S. Wiley.43. In vitroprostaglandin production by isolated ovine endometrial cells.W. S. O, J. K. Findlay, N. Colvin, J. Swaney and B. Doughton44.Influence of dietary polyunsaturated fatty acids on renal and aortic prostaglandin synthesis in 1‐kidney 1‐clip Goldblatt hypertensive rats.D. Mahoney, K. Croft and L. J. Beilin45.Decreased aortic prostacyclin production in rats fed a diet supplemented with fish oil.S. P. Rogers, W. E. Connor, S. Wong, and R. G. Larkins46.Effect of prostaglandin E2 on DNA synthesis in osteoblastic cells.N. C. Partridge, A. L. Opie, S. A. Livesey, K. W. Ng and T. J. Martin47.Regulation of prostaglandin production and ectoenzyme activities in cultured pig aortic endothelial cells.C. N. Chesterman, Ann Ager and J. L. Gordon48.Arachidonic acid metabolism, cAMP‐dependent protein kinase and macrophage functions.N. H. Hunt, L. K. Lim, R. D. Eichner and M. J. Weidemann49.Ultrastructural and biochemical studies on the immunohistochemistry of Toxoplasma gondii antigens using monoclonal antibodies.A. M. Johnson, W. D. Haynes, P. J. Leppard, P. J. McDonald and S. H. Neoh50.Effects of ultraviolet (UV) light exposure in solariums on the immune system.P. Hersey, G. Haran, M. Bradley, E. Hasic, E. Murray and E. Edwards51.Inflammatory process in viral meningoencephalitis.P. C. Doherty.52.A possible role for reactive oxygen species in parasite death and pathological changes during malarial infection.I. A. Clark and N. H. Hunt53.Interleukin‐2 and immune response of bone marrow transplant patients.H. S. Warren, K. Atkinson, R. G. Pembrey and J. Biggs54.Host defences in the upper genital tract of the female: studies in a murine system.T. C. Sorrell, P. A. Baker and A. W. Chow55.Cortisol infusion mimics ACTH‐induced hypertension in man.J. A. Whitworth, D. Saines and B. A. Scoggins56.The perception of breathlessness in asthma.J. G. W. Burdon, E. F. Juniper, K. J. Killian, F. E. Hargreave and E. J. M. Campbell57.Biliary transport of apolipoprotein components of high density lipoproteins in the isolated perfused rat liver.R. B. Sewell, T. Kawamoto, L. J. Kost, S. J. T. Mao and N. F. La Russo58.Plasma vasopressin and noradrenaline after lesions of the ventrolateral medulla.J. M. Elliott, R. Woods, M. J. West, C. l. Johnston and J. P. Chalmers59.Depletion of substance P in primary afferents does not affect baroreceptor reflexes.J. M. Elliott, J. B. Furness, R. Murphy, M. Costa and J. P. Chalmers60.Induction of puberty in male primates by administration of pulsatile gonadotropin releasing hormone.C. J. Carati, J. Bertolini and E. J. Keogh61.Activation of inhibitory nerves in the enteric nervous system by cholecystokinin octapeptide.M. C. Ngu.62.Confirmation of the functional heterogeneity of the liver.G. P. Timms, L. Bass, J. W. Halli‐day, W. G. E. Cooksley, R. A. Ferris and L. W. Powell69.Calcium regulatory hormones in immobilization hypercalcaemia associated with renal failure.R. L. Prince, J. A. Eisman and R. W. Simpson70.Somatic cell genetic analysis of deoxyadenosine toxicity in human lymphocytes.R. M. Fox, E. H. Tripp and M. S. Hershfield71.Cloning of lymphocytes at limiting dilution.K. Trainor, A. Morley and R. Seshadri.72.The effect of succinylcholine on malignanthyperpyrexia‐susceptible muscle. G. J. Galloway and M. A. Denborough.73.Effect of hypoxia on the growth of human melanomas in culture.P. C. Vincent and R. M. Joyce74.Preparation and characterization of platelet‐derived growth factor.T. Walker, C. N. Ches6‐thioguanine‐resistant variant of the 13762 cell line which is no longer tumorigenic or metastatic.I. A. Ramshaw.76.Human CTP synthetase: a biochemical marker of aggressive lymphoid malignancy. P. H.Ellnis and G. Medley77.A novel method for identifying the progeny of a multipotent stem cell.A. J. Hapel.78.Investigation of the biochemical mechanisms of cyclophosphamide resistance in human melanoma cells.M. H. Boon and P. G. Parsons79.Incorporation of 2‐deoxyadenosine into poly(A)RNA of human T lymphoblasts.R. F. Kefford, R. M. Fox, E. McCairns, D. Fahey, G. E. O. Muscat and P. B. Rowe80.Application of NMR spectroscopy to lymphocytes and tumours.C. Mount ford, G. Grossman, G. Reid and R. M. Fox81.The distribution of methylcytosine at a specific site in human highly repeated DNA.P. C. Vincent, J. Prosser and M. Frommer82.Purine levelsin vivo. M. H. N. Tattersall, P. Slowiaczek and A. De Fazio83.Affinity purification and characterization of human x‐casein, a potential cancer marker.A. R. Nash, A. G. Mackinlay, G. A. Sarfaty and P. Castillo84.The dopaminergic enhancement of the renal response to aldosterone is intrarenal, ex‐traneuronal and probably receptor‐mediated.B. A. Adams, R. M. Wellard and W. R. Adam85.Platelets deficient in glycoprotein I have normal Fc receptor expression.S. L. Pfueller, N. Kerlero de Rosbo and R. Bilston86.Characterization and reconstitution of the binding activity of receptor purified radio‐iodinated thyrotropins.P. G. Stanton, A. R. Roberts and M. T. W. Hearn87.Evidence for adenylate cyclase coupled adenosine receptors in guinea‐pig ventricles.E. Leung and E. A. Woodcock88.The use of a monoclonal antibody in the investigation of platelet glycoprotein Hb‐HIa function.B. Barlow, J. Connellan, P. Thurlow and I. L. Smith89.Kidney β‐adrenergic receptors are modulated by baroreflex activity.M. J. Morris, E. A. Woodcock and C. I. Johnston117.Whole ceU NMR: its application to virology and immunology.C. Mountford, K. T. Holmes, G. Grossman, A. W. Hampson and R. Raison118.The first International Workshop on human leucocyte differentiation antigens: analysis of 200 monoclonal antiodies by immunoperoxidase on tissue sections.J. Quirk and D. G. Jose119.Immunoregulation in glomerulonephritis (GN).K. M. Bannister, P. A. Drew, A. R. Clarkson and A. J. Woodroffe120.Allograft responsiveness in rats treated with cyclosporin A to prolong heart allograft survival.M. E. Jelbart, B. M. Hall and S. E. Dorsch121.Synergistic interaction between cytomegalovirus infection and graft vs host reaction in the development of interstitial pneumonia in mice.Jane E. Grundy (Chalmer), J. D. Shanley and G. M. Shearer122.Heterogeneity of ovine squamous cell carcinoma determined by flow cytometric DNA analysis.G. J. S. Harker, R. A. Zbroja, J. Wass, J. Grace, P. C. Vince
ISSN:0305-1870
DOI:10.1111/j.1440-1681.1983.tb00848.x
出版商:Blackwell Publishing Ltd
年代:1983
数据来源: WILEY
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