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Effects of PAF-acether and structural analogues on platelet activation and bronchoconstriction in guinea-pigs.
The results indicate that PAF-acether and the analogues studied trigger platelet activation and the consequent bronchoconstriction through mechanisms which share sensitivity to same antagonists. Expand
Structure-activity relationship in PAF-acether. 3. Hydrophobic contribution to agonistic activity.
It is concluded that the ether oxide function is absolutely essential at the glycerol 1-position for potent agonist activity and that potency correlates well with hydrophobicity parameters. Expand
Decreased Thermogenic Response to an Oral Glucose Load in Older Subjects
It is suggested that the thermogenic response to an oral glucose load is blunted in older people, and this may represent an additional factor that contributes to the decreased energy requirement with age and therefore to the increased propensity to obesity if energy intake is not adjusted. Expand
Structure-activity relationship in PAF-acether. 2. rac-1-O-Octadecyl-2-O-acetyl-3-O-[gamma-(dimethylamino)propyl]glycerol .
Two products without phosphoryl groups were synthesized from 1-O-octadecyl-2- O-acetyl-3-O-[gamma-(dimethylamino)propyl]glycerol and its quaternary salt, which lost aggregating and bronchoconstrictive activities and did not show any antagonistic effects. Expand
Structure-activity relationship in PAF-acether. 4. Synthesis and biological activities of carboxylate isosteres.
The synthesis and biological characterization of some 3-carboxylate isosteres of PAF-acether structurally modified in positions 1 (ether, carbamate), 2 (acetoyl, ethoxy), and 3 (chain length andExpand
Cytotoxic activity of synthetic aza alkyl lysophospholipids against drug sensitive and drug resistant human tumor cell lines.
It is demonstrated that aza alkyl lysophospholipids are cytotoxic to a variety of human tumor cell lines and do not appear to discriminate between drug/cytokine sensitive or resistant cells. Expand
Membrane cholesterol content and sensitivity of human carcinoma-cells to antineoplastic ether phospholipids.
The lipid membrane composition of three human carcinoma cell lines that have been found to possess different sensitivity to the tumoricidal activity of four antitumor ether phospholipids are measured and a statistically significant difference has been found in the membrane cholesterol content of the three cell lines. Expand
Structure-activity relationships in platelet-activating factor (PAF). 5. Synthesis and in vitro antagonistic activities of ketophosphonates.
These ketophosphonates differing in chain length in position 3 exhibit potent agonistic activities on rabbit platelets which increase with the number of methylene groups between the phosphonate and the ammonium moieties. Expand
Synthesis and characterization of a radioiodinated, photoreactive and physiologically active analogue of platelet activating factor.
The multistep synthesis of a photoreactive, radioactive and aggregating analogue of platelet-activating factor (PAF)-acether is described, and the covalent binding of the analogue to protein (BSA) after 10-min irradiation times at 300 nm was proved. Expand