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  • 1
    Electronic Resource
    Electronic Resource
    AHR-10037, a non-steroidal anti-inflammatory compound of low gastric toxicity (1990)
    Springer
    Inflammation research 31 (1990), S. 117-126 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract AHR-10037 is an anti-inflammatory compound possessing analgesic and antipyretic properties and a high therapeutic index. AHR-10037 was comparable to indomethacin in suppressing acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation. There was a delayed onset of antipyresis (yeast-induced hyperthermia in rats), analgesia (acetylcholine-induced abdominal constriction in mice) and inhibition of caster oil-induced diarrhea in rats. Antipyresis occurred 3 hours after administration of AHR-10037, 4 mg/kg, PO, vs 1 hour after administration of acetylsalicylic acid, 100 mg/kg, PO; maximum analgesic activity (ED50-4.1 mg/kg) occurred at 4 hours. AHR-10037 was inferior to indomethacin in suppressing castor oil-induced diarrhea in rats. The therapeutic index of AHR-10037 (relating acute anti-inflammatory potency to gastric toxicity potency relative to indomethacin) ranged from 56–91. The pharmacological profile suggests that AHR-10037 is a prodrug convertedin vivo to a cyclooxygenase inhibitor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02003231
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  • 2
    Electronic Resource
    Electronic Resource
    Thein vivo andin vitro activity of AHR-13268D, a new antiallergic/antihistaminic agent (1990)
    Springer
    Inflammation research 31 (1990), S. 210-218 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract AHR-13268D (4-[3-[4-[Bis(4-flurophenyl)hydroxymethyl]-1-piperidinyl]propoxy]benzoic acid, sodium salt) is a potent, long-acting water soluble, antiallergic and antihistaminic agent. AHR-13268D protects sensitive guinea pigs from collapse induced by aerosolized antigen; 1, 5, and 24 h ED50s in the test were 0.27, 0.25, 0.93 mg/kg, PO, respectively. AHR-13268D was also active when given as an aerosol, the 1 h ED50=0.29%. In the rat passivefoot anaphylaxis test, AHR-13268D was slightly more active (1.55 times) than AHR-5333B when given orally 1 h prior to challenge and equipotent to cromolyn when given intravenously immediately prior to challenge. AHR-13268D displayed potent, long-acting antihistaminic activity in naive guinea pigs; the 1, 5, and 24 h oral ED50s being in the range of 0.3 mg/kg. AHR-13268D (10 to 20 mg/kg, PO) attenuated the skin responses to ascaris antigen in sensitive dogs and did not alter the EEG pattern or sleep/wake patterns of cats at doses in vast excess of its antihistaminic activity.In vitro, AHR-13268D was a potent inhibitor of histamine release from rat peritoneal mast cells (IC50=0.51 nM) and was as potent as the reference 5-LO inhibitor phenidone in inhibiting antigen-induced contractions of guinea pig ileum in the presence of pyrilamine, atropine, and imidazole (IC50∼300 μM). AHR-13268B was bioavailable (∼88%) from capsules or from oral solutions.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01997610
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  • 3
    Electronic Resource
    Electronic Resource
    Rocastine (AHR-11325), a rapid acting, nonsedating antihistamine (1989)
    Springer
    Inflammation research 28 (1989), S. 53-61 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Rocastine [AHR-11325, 2-[2-(dimethylamino)ethyl]-2,3-dihydro-4-methylpyrido-[3,2-f]-1,4-oxazepine-5(4H)-thione (E)-2-butenedioate)] is a rapid-acting, potent, nonsedating antihistamine. In guinea pigs challenged with a lethal dose of histamine, rocastine is as effective [based on 1 hr. oral, protective dose (PD50s)] as brompheniramine, chlorpheniramine, pyrilamine, and promethazine and superior to astemizole, diphenhydramine, terfenadine, and oxaomide. Rocastine has a faster onset of action than does terfenadine; rocastine being as effective with a 15 min pretreatment time (PD50=0.13 mg/kg) as it is with a 1 hr pretreatment time (PD50=0.12 mg/kg), while the 15 min PD50 of terfenadine (PD50=44.0 mg/kg) is 22 times greater than the 1 hr PD50 (PD50=1.93 mg/kg). Against aerosolized histamine, rocastine was 7.12×, 2.63×, and equipotent to pyrilamine in preventing histamine-induced prostration at pretreatment times of 1, 3, and 6 hr, respectively. Rocastine protected guinea pigs from collapse induced by aerosolized antigen; rocastine was ∼36 × more potent (based on 1 hr PD50) than diphenhydramine and as potent as oxatomide and terfenadine. Rocastine did not alter the EEG of cats at doses in vast excess (150×) of its antihistaminic dose nor did it potentiate yohimbine toxicity in mice. Further, rocastine possesses no anticholinergic, antiadrenergic, or antiserotonergic propertiesin vitro. Rocastine is a selective, nonsedating, H1-antagonist with a rapid onset of action.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02022980
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  • 4
    Electronic Resource
    Electronic Resource
    Studies on the effects of cyclo-oxygenase and lipoxygenase inhibitors on the macrophage stimulated synthesis of collagenase by rabbit chondrocytes (1985)
    Springer
    Inflammation research 17 (1985), S. 73-76 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Recent work from this laboratory has shown that macrophages in culture synthesize and secrete a soluble factor(s) that induces the synthesis of collagenase in primary cultures of rabbit chondrocytes (Arth. Rheum. 23, 448, 1980). The current studies were undertaken to determine the role of arachidonate metabolism in this process. Incubation of chondrocytes with MCM (Macrophage Conditioned Medium) and low doses of indomethacin (1–10 μM) had no effect on collagenase synthesis. The lipoxygenase inhibitor NDGA, indomethacin at high doses (50 μM), diethyl-carbamazine and the phospholipase inhibitor dibromoaceto-phenone, inhibited the MCM dependent synthesis of collagenase in chondrocytes. These inhibitors did not affect collagenase activity nor did they interfere with the activation of latent collagenase. Our data indicate that although cyclo-oxygenase plays no role in the MCM dependent induction of collagenase in chondrocytes, lipoxygenase activity may be essential.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01966685
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  • 5
    Electronic Resource
    Electronic Resource
    The effect of calcium channel blockers and calmodulin inhibitors on the macrophage factor-stimulated synthesis of collagenase by rabbit chondrocytes (1988)
    Springer
    Inflammation research 25 (1988), S. 71-76 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Macrophages and monocytes secrete a factor(s) which can stimulate the synthesis of collagenase in synovial cells and in chondrocytes. Incubation of rabbit chondrocytes with macrophage conditioned medium (MCM) and with the calcium channel blockers, nifedipine, verapamil or diltiazem (up to 200 μM) had no effect on collagenase synthesis. However, TMB-8 (8-[N, N-diethylamino]-octyl 3,4,5,-trimethoxybenzoate hydrochloride), an inhibitor of internal calcium movement, did inhibit the process with an IC50 of approximately 130 μM. The calmodulin antagonists, trifluoperazine, chlorpromazine and calmidazolium (R-24571) were effective inhibitors of the process with IC50's of 40 μM, 18 μM and 3.5μM, respectively. Collagenase activity itself was not affected by these agents. The data suggests that calmodulin and/or internal calcium movement may play a role in the macrophage factor-stimulated synthesis of collagenase in rabbit chondrocytes.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01969097
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  • 6
    Electronic Resource
    Electronic Resource
    The topical anti-inflammatory and analgesic properties of bromfenac in rodents (1988)
    Springer
    Inflammation research 25 (1988), S. 77-85 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Bromfenac [2-amino-3-(4-bromobenzoyl) benzeneacetic acid sodium slat sesquihydrate] is an anti-inflammatory/analgesic agent that possesses potent topical activity in rats, guinea pigs, and mice. In rat models of acute (carrageenan paw edema) and chronic (adjuvant arthritis) inflammation, preparations of bromfenac at concentrations as low as 0.01–0.32% (0.01–0.32 mg bromfenac) produced significant anti-inflammatory activity when applied to the injected paw or to the backs of rats. In the acute paw edema test, topical bromfenac was more potent than indomethacin or hydrocortisone and about as active as triamcinolone acetonide. Bromfenac, at concentrations of 0.1–0.32%, showed topical analgesic more potent than indomethacin (24.9×), more potent than ketoprofen (⊂14.9×), and superior to piroxicam. In the guinea pig UV-erythema test, bromfenac was active (26.1×indomethacin) when applied to the UV-exposed site, but not when applied away from the site. The results suggest that bromfenac has activity topically because of a local and a systemic effect. Test results obtained with a long (4–7 hr) pretreatment time (paw edema, adjuvant arthritis, abdominal constriction) are due in great part to a systemic effect of topically applied bromfenac, while the UV-erythema test (1-hr treatment time) clearly indicates a local effect.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01969098
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