[Pharmacokinetics of S 3341. Analysis by inhibition of the specific binding of 3H-clonidine].
1. The radioreceptor assay for S 3341, an alpha 2-adrenergic agonist, is based on the ability of the S 3341 to compete with the specific binding of [3H] clonidine to alpha-receptors of rat cerebral cortex membranes. The technique described was used for S 3341 plasma determination. 2. S 3341 levels in plasma and blood pressure were measured in hypertensive subjects 1, 3, 5, 8, 12, 24 and 48 hours after ingestion of the drug. 3. The s 3341 plasma level rose to a maximum between the first and the third hours after ingestion and then declined, with a mean half-life of 14 hours. There were substantial inter-individual variations, ranging from 3 to 24 hours. 4. The fall in blood pressure mirrored the increase in the s 3341 plasma level during the three hours following the ingestion of the drug.
D000316:Adrenergic alpha-Agonists / Q000378:metabolism*; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D003000:Clonidine; D006801:Humans; D006973:Hypertension / Q000097:blood; D007700:Kinetics; D008297:Male; D008566:Membranes / Q000378:metabolism; D010080:Oxazoles / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D000077769:Rilmenidine; D013997:Time Factors
D000316:Adrenergic alpha-Agonists; D010080:Oxazoles; D003000:Clonidine; D000077769:Rilmenidine
Pharmacocinétique du S 3341. Dosage par inhibition de la liaison spécifique de la clonidine [3H].