Document Detail

The pharmacology of the lipoxygenase inhibitors oxphaman (1-(2,5-dihydroxybenzylidene)aminoadamantane) and oxphalin (1-(3,4-dihydroxybenzylidene)-2,4,6-trimethylaniline
MedLine Citation:
PMID:  2512586     Owner:  NLM     Status:  MEDLINE    
Oxphaman and particularly oxphalin, among other phenolic azomethines, have been proven as strong inhibitors of lipoxygenases (LOX) from reticulocytes, soybean, thrombocytes as well as of quasi-LOX (hemoglobin) with IC50 values which correspond with those of known LOX inhibitors. The 5-LOX is likewise strongly, the cyclooxygenase of sheep seminal vesicles only weakly inhibited. Nevertheless, antiinflammatory effectivity was found in some carrageenin-induced inflammatory models of the rat as well as in the arachidonic acid- and croton oil-induced ear oedema of the mouse. Adjuvant arthritis, experimental pain, skin permeability and allergy models (anaphylactic paw oedema, cutaneous anaphylaxis, asthma, picryl chloride ear oedema) were not, only weakly or irregularly influenced. In the guinea pig ileum a certain antihistaminic, anticholinergic and leukotriene antagonistic activity was found. An inflammation-induced vasodepression (anaphylactic shock, dextran paw oedema. UV irradiation) was dose-dependently prevented or even reversed, obviously on the basis of oxygen radical scavenging.
H Bekemeier; R Hirschelmann; A Langner; A J Giessler; E Krause; T Funke; F Hänsel; K Schmidt; S Zarnack; H H Schumann
Publication Detail:
Type:  English Abstract; In Vitro; Journal Article    
Journal Detail:
Title:  Die Pharmazie     Volume:  44     ISSN:  0031-7144     ISO Abbreviation:  Pharmazie     Publication Date:  1989 Aug 
Date Detail:
Created Date:  1990-01-23     Completed Date:  1990-01-23     Revised Date:  2007-01-29    
Medline Journal Info:
Nlm Unique ID:  9800766     Medline TA:  Pharmazie     Country:  GERMANY, EAST    
Other Details:
Languages:  ger     Pagination:  550-5     Citation Subset:  IM    
Martin Luther-Universität Halle-Wittenberg, Sektion Pharmazie, Wissenschaftsbereich Pharmakologie.
Vernacular Title:
Zur Pharmakologie der Lipoxygenasehemmer Oxphaman, 1-(2,5-Dihydroxybenzyliden)aminoadamanten, und Oxphalin, 1-(3,4-Dihydroxybenzyliden)-2,4,6-trimethylanilin.
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MeSH Terms
Adamantane / analogs & derivatives*,  pharmacology
Aniline Compounds / pharmacology*
Anti-Inflammatory Agents, Non-Steroidal*
Arthritis, Experimental / drug therapy,  physiopathology
Asthma / drug therapy
Benzyl Compounds / pharmacology*
Edema / drug therapy
Free Radicals
Guinea Pigs
Histamine Antagonists
Lipoxygenase Inhibitors*
Reticulocytes / enzymology
Skin Absorption / drug effects
Soybeans / enzymology
Reg. No./Substance:
0/Aniline Compounds; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Benzyl Compounds; 0/Free Radicals; 0/Histamine Antagonists; 0/Lipoxygenase Inhibitors; 112851-89-5/oxphaman; 120370-70-9/oxphalin; 281-23-2/Adamantane

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