Uptake kinetics and metabolism of 7-3H-dopamine in the isolated perfused rat heart. 1971

G Hellmann, and G Hertting, and B Peskar

1. The isolated, perfused rat heart accumulates dopamine by two distinct uptake mechanisms characterized by different kinetic constrants and different patterns of metabolite production (Uptake 1: Km 0.69 x 10(-6)M and Vmax (1.45 x 10(-9) mol/g)/min; Uptake 2: Km 5.9 x 10(-4)M and Vmax (0.14 x 10(-6) mol/g)/min).2. The metabolic fate of dopamine taken up by the isolated, perfused rat heart depends on the concentration of dopamine in the perfusion medium. At a very low perfusion concentration (0.047 x 10(-10) mol/ml) most of the radioactivity is stored as unchanged dopamine and the main metabolite is noradrenaline. With increasing perfusion concentrations deamination becomes the main metabolic pathway, deaminated metabolites accounting for more than 50% of the total radioactivity after perfusion with 2,614.4 x 10(-10) mol/ml for 16 minutes. The O-methylated, and the O-methylated deaminated metabolites are of minor importance at all perfusion concentrations.3. The resistance to wash out of the dopamine taken up by the isolated, perfused rat heart is dependent on the perfusion concentration used. At a concentration of 66.9 x 10(-10) mol/ml, 50% of the total activity is washed out during an 8 min wash period. Within the same time interval there is no wash out when a perfusion concentration of 0.042 x 10(-10) mol/ml is used.4. It is concluded that the metabolic fate of dopamine taken up at various perfusion concentrations reflects the distribution of dopamine within intra- and extraneuronal compartments in the hearts.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D009206 Myocardium The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow. Muscle, Cardiac,Muscle, Heart,Cardiac Muscle,Myocardia,Cardiac Muscles,Heart Muscle,Heart Muscles,Muscles, Cardiac,Muscles, Heart
D009638 Norepinephrine Precursor of epinephrine that is secreted by the ADRENAL MEDULLA and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers, and of the diffuse projection system in the brain that arises from the LOCUS CERULEUS. It is also found in plants and is used pharmacologically as a sympathomimetic. Levarterenol,Levonorepinephrine,Noradrenaline,Arterenol,Levonor,Levophed,Levophed Bitartrate,Noradrenaline Bitartrate,Noradrénaline tartrate renaudin,Norepinephrin d-Tartrate (1:1),Norepinephrine Bitartrate,Norepinephrine Hydrochloride,Norepinephrine Hydrochloride, (+)-Isomer,Norepinephrine Hydrochloride, (+,-)-Isomer,Norepinephrine d-Tartrate (1:1),Norepinephrine l-Tartrate (1:1),Norepinephrine l-Tartrate (1:1), (+,-)-Isomer,Norepinephrine l-Tartrate (1:1), Monohydrate,Norepinephrine l-Tartrate (1:1), Monohydrate, (+)-Isomer,Norepinephrine l-Tartrate (1:2),Norepinephrine l-Tartrate, (+)-Isomer,Norepinephrine, (+)-Isomer,Norepinephrine, (+,-)-Isomer
D010477 Perfusion Treatment process involving the injection of fluid into an organ or tissue. Perfusions
D004298 Dopamine One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action. Hydroxytyramine,3,4-Dihydroxyphenethylamine,4-(2-Aminoethyl)-1,2-benzenediol,Dopamine Hydrochloride,Intropin,3,4 Dihydroxyphenethylamine,Hydrochloride, Dopamine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001711 Biotransformation The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
D014316 Tritium The radioactive isotope of hydrogen also known as hydrogen-3. It contains two NEUTRONS and one PROTON in its nucleus and decays to produce low energy BETA PARTICLES. Hydrogen-3,Hydrogen 3
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

Related Publications

G Hellmann, and G Hertting, and B Peskar
April 1988, Naunyn-Schmiedeberg's archives of pharmacology,
G Hellmann, and G Hertting, and B Peskar
August 1990, Lipids,
G Hellmann, and G Hertting, and B Peskar
May 1978, Naunyn-Schmiedeberg's archives of pharmacology,
G Hellmann, and G Hertting, and B Peskar
January 1985, Advances in myocardiology,
G Hellmann, and G Hertting, and B Peskar
May 1978, Naunyn-Schmiedeberg's archives of pharmacology,
G Hellmann, and G Hertting, and B Peskar
March 1991, Toxicology and applied pharmacology,
G Hellmann, and G Hertting, and B Peskar
November 1980, Bollettino della Societa italiana di biologia sperimentale,
G Hellmann, and G Hertting, and B Peskar
September 1983, Biochemical pharmacology,
G Hellmann, and G Hertting, and B Peskar
January 1990, Experimental lung research,
G Hellmann, and G Hertting, and B Peskar
January 1978, Biochemical pharmacology,
Copied contents to your clipboard!