Pharmacological profile of the abeorphine 201-678, a potent orally active and long lasting dopamine agonist

Journal Article · Mon Jan 13 04:00:00 EST 1986 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(86)90007-X· OSTI ID:6381429

Jaton, A L; Giger, R K.A.; Vigouret, J M; Enz, A; Frick, W; Closse, A; Markstein, R

The central dopaminergic effects of an abeorphine derivative 201-678 were compared to those of apomorphine and bromocriptine in different model systems. After oral administration, this compound induced contralateral turning in rats with 6-hydroxydopamine induced nigral lesions and exhibited strong anti-akinetic properties in rats with 6-hydroxydopamine induced hypothalamic lesions. It decreased dopamine metabolism in striatum and cortex, but did not modify noradrenaline and serotonin metabolism in the rat brain. 201-678 counteracted the in vivo increase of tyrosine hydroxylase activity induced by ..gamma..-butyrolactone. In vitro it stimulated DA-sensitive adenylate cyclase and inhibited acetylcholine release from rat striatal slices. This compound had high affinity for /sup 3/H-dopamine and /sup 3/H-clonidine binding sites. These results indicate that 201-678 is a potent, orally active dopamine agonist with a long duration of action. Furthermore it appears more selective than other dopaminergic drugs. 29 references, 5 figures, 3 tables.

• Research Organization: Sandoz Ltd., Basel, Switzerland
• OSTI ID: 6381429
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 38:2; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ACETYLCHOLINE
ADRENAL HORMONES
AFFINITY
ALKALOIDS
AMINES
AMINO ACIDS
AMMONIUM COMPOUNDS
ANALGESICS
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZOLES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CARBOXYLIC ACIDS
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM DEPRESSANTS
COMPARATIVE EVALUATIONS
CYCLASES
DATA
DOPAMINE
DRUGS
ENZYME ACTIVITY
ENZYMES
ESTERS
EXPERIMENTAL DATA
HETEROCYCLIC COMPOUNDS
HORMONES
HYDROXY ACIDS
HYDROXY COMPOUNDS
HYDROXYLASES
INDOLES
INFORMATION
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LYASES
MAMMALS
METABOLISM
MORPHINE
NARCOTICS
NERVOUS SYSTEM
NEUROREGULATORS
NORADRENALINE
NUMERICAL DATA
OPIUM
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
OXIDOREDUCTASES
PARASYMPATHOMIMETICS
PHENOLS
POLYPHENOLS
PYRROLES
QUATERNARY COMPOUNDS
RADIOPROTECTIVE SUBSTANCES
RATS
REACTION KINETICS
RECEPTORS
RODENTS
SEROTONIN
STEROID HORMONES
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
TRYPTAMINES
TYROSINE
VERTEBRATES