PAF receptor. 2. Quantitative hydrophobic contribution of the agonist's etheroxid chain.
In order to undertake a quantitative assessment of the contribution of the hydrophobic effect of the etheroxid chain to agonistic activity, it was necessary to include in the calculated data a highly lipophilic platelet-activating factor (PAF) analogue. The synthesis of such a compound--racemic 1-O-docosyl-2-O-acetylglycero-3-phosphocholine (C22 PAF)--is described. The regression analysis performed with data of 14 etheroxid analogues (reviewed by Godfroid et al., 1987), combined with data obtained with C22 PAF, is significant with respect to a parabolic evolution between lipophilicity of the chain and the logarithm of relative platelet stimulation. This result is characteristic of a hydrophobic interaction between the agonist and the PAF receptor.
Heymans
F
F
Laboratoire de Pharmacochimie Moléculaire, Université Paris, France.
Steiner
E
E
Jouquey
S
S
Godfroid
J J
JJ
D000818:Animals; D001980:Bronchi / Q000187:drug effects; D006168:Guinea Pigs; D007022:Hypotension / Q000139:chemically induced; D066298:In Vitro Techniques; D008297:Male; D010972:Platelet Activating Factor / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D010980:Platelet Membrane Glycoproteins; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000187:drug effects*; D043562:Receptors, G-Protein-Coupled; D013329:Structure-Activity Relationship
D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; C072667:1-O-docosyl-2-O-acetylglycero-3-phosphocholine