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Effect of acetyl derivatives of some sympathomimetic amines on the blood pressure of the rat

Effect of acetyl derivatives of some sympathomimetic amines on the blood pressure of the rat. Fristrom, Sinikka; Marvola, Martti; Klinge, Erik; Halmekoski, Jaakko (Sch. Pharm., Univ. Helsinki, Helsinki, Finland). Acta Pharmacol. Toxicol., 40(2), 247-58 (English) 1977. CODEN: APTOA6. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) The effect of 5 sympathomimetic amines and some of their acetyl derivs. on the blood pressure of the rat was detd. on the left carotid artery. After pretreatment with chlorisoandamine (1 mg/kg subcutaneously), the blood pressure rise by sympathomimetic amines and their acetyl derivs. was compared with that of adrenaline. If the potency of adrenaline was specified as 100, the potencies of the other drugs were phenylephrine-HCl [61-76-7] 37, tyramine-HCl [60-19-5] 1.1, O-acetyltyramine-HCl [14383-55-2] 0.52, amphetamine sulfate [60-13-9] 0.50, O3,O-diacetyl-phenylephrine-HCl [58952-79-7] 0.25, l-ephedrine-HCl [50-98-6] 0.23, O-acetylephedrine-HCl [14383-62-1] 0.02, N-acetylphenylephrine [58952-80-0] 0.01. The effects of N-acetyltyramine [1202-66-0], N-acetylephedrine [2272-83-5] and N-acetylamphetamine [14383-60-9] were even weaker. Reserpine 5.0 or 0.05 mg/kg intraperitoneally 24 hs before the expt. increased the blood pressure rise by the directly acting sympathomimetic amines and their acetyl derivs., but decreased the effects of the indirectly acting drugs. After treatment with phenoxybenzamine (2 mg/kg intraperitoneally), adrenaline exhibited the greatest blood pressure decrease and the effects of the other drugs in descending order: orciprenaline, O-acetyltyramine, phenylephrine, ephedrine, amphetamine, O-diacetylphenylephrine and O-acetylephedrine. Tyramine did not show any blood pressure decrease. The blood pressure decrease by sympathomimetic amines and by their acetyl derivs. was probably due to .beta.-receptor stimulation because it was prevented by propranolol.In this experiment, several chemicals are used like 60-19-5 and 14383-62-1 The N-acetyl derivs. resembled their parent drugs with regard to the immediate onset and short duration of their effects. The O-acetyl derivs. exhibited slower onset and longer duration of effect than their parent drugs. Physostigmine-pretreatment diminished the rise in blood pressure by O-acetyltyramine, but the effect of tyramine remained unchanged. .

The metabolism of tyrosine, tyramine and L-3,4-dihydroxyphenylalanine by cerebral and thoracic ganglia of the locust, Schistocerca gregaria

The metabolism of tyrosine, tyramine and L-3,4-dihydroxyphenylalanine by cerebral and thoracic ganglia of the locust, Schistocerca gregaria. Vaughan, Peter F. T. 59-92-7 and 1202-66-0 are also occured in this study.; Neuhoff, Volker (Dep. Biochem., Glasgow Univ., Glasgow, Scot.). Brain Res., 117(1), 175-80 (English) 1976. CODEN: BRREAP. DOCUMENT TYPE: Journal CA Section: 12 (Nonmammalian Biochemistry) Tyrosine was converted to dopa and p-hydroxyphenylpyruvic acid by hemolymph of S. gregaria but was converted to tyramine, N-acetyltyramine, and N-acetyldopamine by cerebral and thoracic ganglia without formation of dopa. This suggests that the 1st step in catecholamine formation by the ganglia is decarboxylation to tyramine rather than hydroxylation to dopa. The ganglia converted dopa to dopamine and N-acetyldopamine, and converted tyramine to N-acetyltyramine, N-acetyldopamine, and smaller amts. of unidentified metabolites. .