Library

feed icon rss

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
  • 1
    ISSN: 1474-8673
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Chemistry and Pharmacology , Medicine
    Notes: 1 The present study compared the effect of the administration of tachykinin NK1- and NK2-receptor antagonists alone and in combination on exogenous and endogenous tachykinin-induced contractions using three different guinea-pig airway preparations: isolated bronchus, isolated perfused lung and in vivo. 2 In the isolated bronchi, the tachykinin NK1-receptor antagonist CP 99994 (0.01–1 μm)produced concentration-dependent inhibition of contractions induced the tachykinin NK1-receptor agonists substance P (SP) and [Met-OMe11] SP ([Met-OMe11]SP), whereas the tachykinin NK2-receptor antagonist SR 48968 (0.1 μm) had no effect. SR 48968 (0.001–0.01 μm)concentration-dependently inhibited contractions induced by the tachykinin NK2-receptor agonists neurokinin A (NKA) and [β-Ala8]-neurokinin A (4–10) ([βAla8]-NKA) whereas CP 99994 (0.1 μm) did not inhibit the contractions. The contractile activity of capsaicin, an agent that releases endogenous tachykinins from sensory C-fibres, was inhibited in a concentration dependent manner by SR 48968 (0.001–0.03 μm) but not by CP 99994 (0.1 μm). Combination of CP 99994 and SR 48968 caused increased inhibitory effects on the concentration–response curves to SP, [Met-OMe11]SP, NKA, [β-Ala8]-NKA and capsaicin. 3 In isolated perfused lungs, SR 48968 concentration (0.01–10 μm) dependently inhibited NKA-, [β-Ala8]-NKA- and capsaicin-induced bronchoconstriction whereas CP 99994 (30 μm) had no effect on SP-, NKA-, [β-Ala8]-NKA- and capsaicin-induced bronchoconstriction. Combination of inactive concentrations of CP 99994 and SR 48968 produced an increased inhibitory effect on all previous stimuli-induced bronchoconstriction. 4 In in vivo guinea-pig studies, intravenous and oral pretreatment with SR 48968 (0.01–1 mg kg−1 i.v. and 0.1–3 mg kg−1 p.o., respectively), but not with CP 99994 (1 mg kg−1 i.v. and 0.3–30 mg kg−1 p.o., respectively), produced a dose-dependent inhibition of the bronchoconstrictor responses induced by NKA, [β-Ala8]-NKA and capsaicin. CP 99994 intravenously (0.3 mg kg−1) and orally (3–10 mg kg−1) inhibited SP-induced bronchoconstriction only. Intravenous and oral low dose combinations of CP 99994 and SR 48968 produced an increased inhibition of SP-, NKA-, [β-Ala8]-NKA- and capsaicin-induced bronchoconstriction, respectively. 5 The present data indicate that combined tachykinin NK1- and NK2-receptor antagonist treatment compared with single antagonist treatment, using CP 99994 and SR 48968, produced an augmented blockade of tachykinin NK1-, NK2- and capsaicin-mediated contractions in guinea pig airways. These findings support the hypothesis that a dual NK1- and NK2-receptor antagonist may provide an advantage over single activity tachykinin NK1- or NK2-receptor antagonists in pulmonary obstructive diseases.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    ISSN: 1474-8673
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Chemistry and Pharmacology , Medicine
    Notes: 1 Pig nasal mucosal strips were incubated with α-adrenoceptor antagonists followed by α2-adrenoceptor agonist concentration–response curves. 2 Contractions elicited by the α2-adrenoceptor agonists BHT-920 (pD2 = 6.16 ± 0.07), UK 14,304 (pD2 = 6.89 ± 0.13) and PGE-6201204 (pD2 = 7.12 ± 0.21) were blocked by the α2-adrenoceptor antagonist yohimbine (0.1 μm). In contrast, the α1-adrenoceptor antagonist prazosin (0.03 μm) had no effect on the BHT-920-, UK 14,304- and PGE-6201204-induced contractions, but blocked the contractile response to the α1-adrenoceptor agonist phenylephrine (pD2 = 5.38 ± 0.04) and the mixed α1- and α2-adrenoceptor agonist oxymetazoline (pD2 = 6.30 ± 0.22). 3 The α2-adrenoceptor antagonist yohimbine (0.01–0.1 μm, pA2 = 8.04), α2B/C-adrenoceptor antagonist ARC 239 (10 μm, pKb = 6.33 ± 0.21), α2A/C-adrenoceptor antagonist WB 4101 (0.3 μm, pKb = 8.01 ± 0.24), α2A-adrenoceptor antagonists BRL44408 (0.1 μm, pKb = 6.82 ± 0.34) and RX 821002 (0.1 μm, pKb = 8.31 ± 0.35), α2C-adrenoceptor antagonists spiroxatrine (1 μm, pKb = 7.32 ± 0.32), rauwolscine (0.1 μm, pKb = 8.16 ± 0.14) and HV 723 (0.3 μm, pKb = 7.68 ± 0.14) inhibited BHT-920-induced contractions in pig nasal mucosa. 4 The present antagonist potencies showed correlations with binding affinity estimates (pKi) obtained for these antagonists at the human recombinant α2A- and α2C-adrenoceptors (r = 0.78 and 0.83, respectively) and with binding affinity estimates (pKd) obtained in pig native α2A- and α2C-monoreceptor assays (r = 0.85 and 0.78, respectively). No correlation was observed for the α2B-subtype. 5 In conclusion, contractile responses to phenylephrine, BHT-920, UK 14,304, PGE-6201204 and oxymetazoline indicate that α1- and α2-adrenoceptors are present and mediate vasoconstriction in pig nasal mucosa. Furthermore, correlation analysis comparing antagonist potency in pig nasal mucosa with affinities for human recombinant α2-adrenoceptors and native pig α2-adrenoceptors suggest that α2A- and α2C-adrenoceptor subtypes constrict pig nasal mucosa vasculature.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Plant and soil 173 (1995), S. 239-250 
    ISSN: 1573-5036
    Keywords: fertility ; Oryza sativa ; pollen viability ; rice ; salinity ; seed set ; stigma ; stigmatic receptivity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition
    Notes: Abstract The effect of salinity on the reproductive physiology of five rice genotypes (IR54, IR26, IR2153-26-3-5-2, IR15324-117-3-2-2 and BR6), was investigated by treatment from panicle initiation with sodium concentrations of 20, 35 or 50 mol m-3 in an ‘artificial seawater’. In an experiment conducted in a glasshouse, plant height and dry weight were little affected by the treatments. There was, however, genotypic variation in the extent of the sodium accumulation, with IR15324-117-3-2-2 containing the highest and IR2153-26-3-5-2 the lowest concentrations: sodium concentrations were higher in older than younger leaves. Salinity delayed flowering, reduced the number of productive tillers, the number of fertile florest per panicle, the weight per grain and the grain yield: effects on grain yield were very much more severe than on vegetative growth. Panicle length was also reduced as was the number of primary branches in a panicle: again there was genotypic variation in the response of these characters to salinity, with the number of branches in IR2153-26-3-5-2 being particularly sensitive. The concentration of sodium increased in the pollen, stigmas, lemmas and paleas with each increment of external salinity. The highest concentrations of sodium in pollen and stigmas was recorded in IR54 and IR15324-117-3-2-2. Pollen viability, whether tested with the tetrazolium salt thiazolyl blue (3-{4,5-dimethylthiazolyl-2}-2,5-diphenyl monotetrazolium bromide or MTT), germination on stigmas, growth through the stylar tissue or F1 seed set, was reduced particularly in those genotypes accumulating most sodium. At all three salt levels, a genotype which accumulated more Na in its pollen produced less-viable pollen than those with less Na in their pollen. Since the amount of Na in the pollen was highly correlated with the Na in the flag leaf, assessment of flag leaf Na should prove a useful indicator of the likely pollen viability. Stigmatic receptivity was also reduced, when estimated either from germination of viable pollen on stigmas of salt-grown plants, its growth through the stylar tissue or F1 seed set. The reduction of seed set in crosses suggested that the overall consequences of salinity are dominated by effects on panicle development, stigmas and grain filling rather than on pollen. Analysis of the data suggests that genotypic variation exists in the extent to which salinity affects aspects of the plants reproductive physiology and development: this variation might be used in attempts to enhance the resistance of rice to salinity.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...