Document Detail

Yangambin: a new naturally-occurring platelet-activating factor receptor antagonist: in vivo pharmacological studies.
MedLine Citation:
PMID:  7753914     Owner:  NLM     Status:  MEDLINE    
The pharmacological profile of a novel specific platelet-activating factor (PAF) receptor antagonist-yangambin-isolated from the Brazilian plant Ocotea duckei Vattimo (Lauraceae), was investigated in the pentobarbitone-anaesthetized rabbit. The i.v. administration of PAF (0.03-3.0 microgram kg-1) induced marked but reversible hypotensive effects and mild reductions in the heart rate. Both effects are independent of the respiratory conditions imposed on the animals. Moreover, PAF (3.0 microgram kg-1, i.v.) induced a reversible decrease of the circulating levels of platelets and of polymorphonuclear leukocytes. Pretreatment with yangambin (10 and 20 mg kg-1, i.v.) dose-dependently attenuated PAF-induced cardiovascular changes and thrombocytopaenia. Nevertheless, the neutropenic leukopaenia elicited by PAF (3.0 microgram kg-1, i.v.) was not prevented by yangambin whereas the reference PAF antagonists WEB 2086 (2 mg kg-1, i.v.) and SR 27417 (1 mg kg-1, i.v.) significantly inhibited the phenomenon. The hypotensive effects of acetylcholine, histamine, and 5-hydroxytryptamine were not affected by prior administration of yangambin. It is concluded that yangambin is a selective antagonist of the cardiovascular effects of PAF which could be useful in pathological states characterized by abnormal PAF release, such as anaphylactic and septic shocks. Furthermore, yangambin might discriminate a PAF receptor subtype present in the cardiovascular system and platelets from the one existing in polymorphonuclear leukocytes in the rabbit.
H C Castro-Faria-Neto; C V Araújo; S Moreira; P T Bozza; G Thomas; J M Barbosa-Filho; R S Cordeiro; E V Tibiriçá
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Planta medica     Volume:  61     ISSN:  0032-0943     ISO Abbreviation:  Planta Med.     Publication Date:  1995 Apr 
Date Detail:
Created Date:  1995-06-21     Completed Date:  1995-06-21     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0066751     Medline TA:  Planta Med     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  106-12     Citation Subset:  IM    
Departamento de Fisiologia e Farmacodinâmica, Instituto Oswaldo Cruz, FIOCRUZ, Rio de Janeiro, Brazil.
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MeSH Terms
Antihypertensive Agents / pharmacology*
Azepines / pharmacology
Blood Platelets / drug effects
Furans / pharmacology*
Heart Rate / drug effects
Leukocytes / drug effects
Lignans / pharmacology*
Plants / chemistry*
Platelet Membrane Glycoproteins / antagonists & inhibitors*
Receptors, Cell Surface*
Receptors, G-Protein-Coupled*
Thiazoles / pharmacology
Triazoles / pharmacology
Reg. No./Substance:
0/Antihypertensive Agents; 0/Azepines; 0/Furans; 0/Lignans; 0/Platelet Membrane Glycoproteins; 0/Receptors, Cell Surface; 0/Receptors, G-Protein-Coupled; 0/Thiazoles; 0/Triazoles; 0/platelet activating factor receptor; 105219-56-5/WEB 2086; 136468-36-5/SR 27417; 24192-64-1/epiyangambin

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