Increased methylation of chloroform extractable products in brain membrane preparations after propranolol injection to the rat.
1. One and four hours after acute or chronic (8 days) intraperitoneal injection of propranolol to rat at doses up to 25 mg/kg, a beta-adrenergic receptor blockage occurred in brain homogenates, as monitored by [3H]dihydroalprenolol binding. 2. A dose-dependent increased methylation of chloroform extractable products was observed (acute treatment: 18% increase, chronic treatment: 136% increase for the dose of 25 mg/kg). 3. The implication of beta-adrenergic receptors in this effect was studied and this revealed that: (a) acute intraperitoneal injection of the less active propranolol stereoisomer (+) did not produce any effect; (b) the chronic intraperitoneal injection of salbutamol, a beta-adrenergic receptor agonist, induced a decreased methylation of chloroform extractable products (62% decrease for the dose of 2.5 mg/kg). 4. It is concluded that injection of beta-adrenergic antagonist to the rat increases basal methyltransferase activity in the brain. This induces a decreased sensitivity of the enzyme activity to noradrenaline.
Benistant
C
C
Unité INSERM 205, Institut National des Sciences Appliquées, Villeurbanne, France.
Rey
C
C
Fonlupt
P
P
D000420:Albuterol / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002725:Chloroform; D004082:Dihydroalprenolol; D066298:In Vitro Techniques; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D008745:Methylation; D009638:Norepinephrine / Q000494:pharmacology; D011433:Propranolol / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011943:Receptors, Adrenergic, beta / Q000187:drug effects; D013237:Stereoisomerism; D014020:Tissue Extracts / Q000378:metabolism*
D011943:Receptors, Adrenergic, beta; D014020:Tissue Extracts; D004082:Dihydroalprenolol; D002725:Chloroform; D011433:Propranolol; D000420:Albuterol; D009638:Norepinephrine