Reduction of gastric acid secretion and ulcer formation by 3,3-dimethyl-1-(3-methylaminopropyl)-1-phenylphthalan (Lu 3–010); an inhibitor of noradrenaline uptake
- 1 August 1970
- journal article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 22 (8), 568-573
- https://doi.org/10.1111/j.2042-7158.1970.tb10572.x
Abstract
Lu 3–010 [3,3-dimethyl-1-(3-methylaminopropyl)-1-phenylphthalan], administered intraperitoneally, blocks the uptake of [3H]noradrenaline into the mouse and rat heart and has an activity 5 times greater than imipramine and comparable to that of desipramine. Lu 3–010 inhibits basal gastric acid secretion in the rat and is 4 and 2 times more potent than imipramine and desipramine, respectively. The drug is about 9 times more potent than desipramine in preventing the pentagastrin-induced stimulation of gastric acid secretion in the rat. Lu 3–010 reduces the incidence of stress-induced gastric lesions in the rat, exhibiting an ED50 ± s.e. of 6.3 ± 1.4 mg/kg, and at 10 mg/kg, ulcer development in the 17-hour Shay test is reduced by 50%.Keywords
This publication has 12 references indexed in Scilit:
- Inhibition of gastric acid secretion by a potent synthetic prostaglandinJournal of Pharmacy and Pharmacology, 1970
- Blockade of norepinephrine uptake and other activities of 5-(3′-dimethylaminopropyl)-dibenzo[a,d] [1,4]cycloheptadiene hydrochloride (AY-8794) and structurally related compoundsBiochemical Pharmacology, 1969
- Antigastric secretory activity of 4-chloro-α,α-dimethylphenethylaminopropan-2-one and related compoundsCellular and Molecular Life Sciences, 1968
- Inhibition of amine uptake in the mouse heart by some new “thymoleptic” drugsJournal of Pharmacy and Pharmacology, 1968
- Synergism Between Gold and Restraint for Rapid Production of Stress Ulcers in Rats.Experimental Biology and Medicine, 1967
- Pharmacological Studies of a New Series of Bicyclic ThymolepticsActa Pharmacologica et Toxicologica, 1966
- The Chemorelease of Norepinephrine from Mouse Hearts. Structure-Activity Relationships. I. Sympathomimetic and Related AminesJournal of Medicinal Chemistry, 1966
- Thyroid Function and the Cardiac Disposition of CatecholaminesEndocrinology, 1963
- Uptake and Metabolism of Tritiated Norepinephrine in the Isolated Canine HeartCirculation Research, 1963
- Effect of Drugs on the Uptake and Release of 3H-Norepinephrine in the Rat HeartNature, 1962