摘要:

Azelastine hydrochloride, chemically known as l(2H)‐phthalazinone, 4‐[(4‐chlorophenyl)methyl] ‐2‐(hexahydro‐l‐methyl‐lH‐azepine‐4‐yl)‐, monohydrochloride, is a novel, orally effective, long‐acting, antiallergic/antiasthmatic agent. The ability of azelastine and selected antiallergic drugs to inhibit SRS‐A (leukotriene)‐mediated acute lung anaphylaxis in guinea pigs (Konzett‐Rossler method) was investigated. Azelastine and ketotifen were administered p.o. 2 and 24 h before antigen challenge; disodium cromoglycate (DSCG) was administered i.v. immediately before antigen challenge. The oral dose of azelastine required to inhibit leukotriene‐mediated allergic bronchospasm by 50% (ID50: mg/kg) was 0.063 at 2 h and 0.120 at 24 h. Ketotifen at a dose of 0.05 to 10 mg/kg at 2 and 24 h, p.o., as well as DSCG at a dosage of 0.3 to 10 mg/kg at 0 min, i.v., produced weak, inconsistent and nondose‐related antianaphylactic effects. Azelastine is an orally effective and long‐acting inhibitor ofin vivosyn

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00331.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

The microtiter plate ELISA using monoclonal antibody is a specific, sensitive and quantitative technique for measuring CR1 on human erythrocytes. The present investigations established that receptor occupancy by immune complexes did not affect the measurements. The monoclonal anti‐CR1 antibody To5 bound unimpeded to receptors that had reacted with an excess of complement‐opsonized tetanus toxoid anti‐tetanus toxoid complexes prepared at antigen: antibody ratios between 32:1 and 1:8. The CR1 levels on erythrocytes from 11 patients with systemic lupus erythematosus (SLE) were not increased (P>0.30) after release of CR1‐bound immune complexes by incubation with factor I. Neither did the serum from these patients contain blocking anti‐CR1 activity (P>0.10). Additionally, the number of antigenic CR1 sites in 10 normals and in the 11 patients with SLE was well correlated with the number of functional receptor sites as assessed by binding of soluble complexes (P<0.001). These data establish that the true CR1 levels are determined using the microtiter plate ELISA for quantitation of CR1 in patients with diseases involving immune complexes and/or autoa

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00332.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

An experimental model was established in order to study the release of immune complexes (IC) bound by complement C3b receptors (CR1) on human erythrocytes (RBC). Soluble tetanus toxoid anti‐tetanus toxoid complexes were incubated with RBC in the presence of autologous serum at optimal conditions for binding. The RBC carrying complement‐opsonized complexes were incubated with appropriate serum reagents, and ii was shown that factor I was required for release of the complexes, which occurred without loss of CR1. Suramin was, irrespective of factor I, found to induce release of CR1‐bound IC in the absence of EDTA, whereas factor I‐mediated release was inhibited by soramin in the presence of EDTA. EDTA probably interfered through a charge‐dependent interaction. These observations are decisive for the interpretation of in vitro experiments involving these reagents. The combination of EDTA and suramin was found inappropriate for use in quantitative determination ofin vivoCR1

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00333.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

AA‐861, a selective inhibitor of 5‐lipoxygenase of arachidonic acid, was tested for ability to inhibit leukotriene C4and leukotriene B4synthesis in human polymorphonuclear leukocytes after calcium ionophore stimulation. AA‐861 dose‐dependently inhibited leukotriene B4and leukotriene C4generation in human polymorphonuclear leukocytes; the concentration required to inhibit generation by 50 % (IC50) was 3 × 10−7M for leukotriene B4and 1 × 10−8M for leukotriene C4. BW‐755C inhibited the generation of leukotriene C4with an IC50of about 10−5M, indicating that AA‐861 is about 1000 times more potent than BW‐755C. AA‐861 did not affect the activity‐ of either cyclooxygenase or 12‐lipoxygenase at a concentration up to 10−5M in human platelets. AA‐861 did not inhibit histamine release from human basophils. These results indicate that AA‐861 selectively inhibits 5‐lipoxygenase but not cyclooxygenase or

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00334.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

Statidardized exercise challenge tests, symptom scores and whole‐blood eosinophil and basophil counts were made before and during the pollen season in 32 children suffering from hay fever (n= 16) or hay fever and asthma (n= 16). All participants developed rhinitis symptoms during the season. The hay fever group showed in addition a significant seasonal increase in cough score (but in no other asthma symptom) and in circulating eosinophils (P<0.01); mean exercise‐induced bronchoconstriction (EIB) did not change despite a slight increase in a few subjects. The asthma group showed seasonal increases in EIB (P<0.001), asthma symptom score (P<0.002), and total eosinophil count (P<0.001) The increase in the latter was significantly higher (P<0.05) than that in the hay fever group. The relative basophil count remained unchanged in both groups. In conclusion, the hay fever group and the asthma group could be clearly distinguished with respect to EIB during natural pollen exposure. The significantly higher increases in EIB and circulating eosinophils observed in the asthma group might possibly be due to greater pollen antigen sensitivity in the asthmat

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00335.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

A placebo‐controlled, double‐blind study of immunotherapy with the mould speciesCladosporiumwas performed in 22 adult asthmatics. The diagnosis ofCladosporiumallergy was based on a combination of bronchial provocation test and daily symptom score in theCladosporiumseason. An aqueous preparation of a potent, biologically standardized and purified extract was used in a clustered dose‐increase regimen. The clinical efficacy was evaluated by a combination of symptoms (asthma score + peak flow) and consumption of antiasthmatic medication. The mean changes in symptoms and medication consumption over a 10–week registration period (peakCladosporiumseason) in 1982 after 5–7 months of immunotherapy were compared with the corresponding 1981 pretreatment 10‐week period A significant (P= 0.03) difference in terms of “improved”, “unchanged” and “deteriorated” patients in favour ofCladosporiumtreatment was found. Approximately 80% in theCladosporiumgroup showed improved/unchanged symptoms contrary to 30% of the placebo treated. Side effects were observed frequently but only in theCladosporium‐treated. About 70% experienced a large local reaction and 100% had episodes of asthma during dose‐increase phase. Only a few severe systemic reactions occurred. Based on the clinical efficacy of the treatment we consider immunotherapy withCladosporiumfeasible for

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00336.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

“The sick‐building syndrome” (WHO) is reported with increasing intensity in non‐industrial places of work, such as schools, kindergartens, and offices, all of which have a heavy load of traffic (people). The construction of these buildings (e.g. flat roofs) often leads to water damage with subsequent microbial growth. Further, reduced cleaning budgets in connection with the wide use of needle‐felt carpets, as well as ventilation systems not regularly maintained, will lead to pollution by dust and microorganisms. A systematic registration of dust and microbial parameters has been carried out since 1980 in buildings with indoor climate complaints, m order to elucidate the possible influence of thes

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00337.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

Allergen‐mediated histamine release from human leukocytes represents an important model forin vitrostudies of allergic reactions. The purpose of this study was to determine whether the measurement of histamine released in allergic patients by radioenzymatic assay following mixing of their blood with common allergens represents a reliable index for diagnosis of atopic allergy. Three categories of allergens were used: 1) house dust and mite; 2) cat and dog dander; 3) trees, gasses and ragweed mixture. The presence of allergy was established by clinical history and intradermal skin testing in the study group of 150 patients. A significant allergen‐mediated histamine release ranging from 4 to 65% of the total blood histamine content was observed in 96 % of the patients with skin test sensitivity of ≥ 3+. There was a significant correlation between skin testing and histamine release in terms of the allergens causing the response. Thus, the measurement of histamine by radioenzymatic technique following its release in blood in response to allergen challenge represents a clinically usefulin vitrotest for the diagnosis of atopic di

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00338.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

Thein vivoandin vitroeffects of indomethacin on the natural killer (NK) cell activity against K 562 target cells were studiedIn vivoadministration of indomethacin, 3 × 50 mg for 7 days to normal donors did not influence baseline NK cell activity, which means that treatment with prostaglandin (PG) inhibitors can be allowed in studies on NK cell activity of persons with normal PG production. The NK cell activity of fresh mono‐nuclear cells was boosted with pharmacological concentrations of indomethacinin vitro, while frozen cells were not. Our results indicate that indomethacin enhances the NK cell activityin vitroby blocking the prostaglandin production of monocytes, since monocyte depleted effector cells were not boosted by indomethac

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00339.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY

摘要:

Natural killer (NK) cell activity against K 562 target cells was inhibited by pharmacological concentrations of chloroquine, mefloquine and quinine. The most potent were mefloquine and quinine. The drug‐induced inhibition of the NK cell activity was abolished by addition of α interferon (IF) or interleukin 2 (II‐2); preincubation of mononuclear cells with IF or II‐2 followed by addition of anti‐malarial drugs decreased the inhibitory effects of the drugs. The drug‐induced inhibition of the NK cell activity was not dependent on the presence of monocytes. Using monocyte depleted Percoll fractionated NK cell enriched populations in a single cell agarose assay, it was shown that the inhibitory effects of mefloquine, but not of chloroquine and quinine were due to an inhibition of the formation of effector/target cell

ISSN:0105-4538    

DOI:10.1111/j.1398-9995.1986.tb00340.x

出版商:Blackwell Publishing Ltd    

年代:1986

数据来源: WILEY