Details

Autor(en) / Beteiligte

• Kyncl, John J
• Buckner, Steven A
• Brondyk, Harold
• Kerkman, Daniel J
• DeBernardis, John F
• Bush, Eugene N
• Kuchel, Otto

Titel

Adrenergic and Dopaminergic Properties of Dopamine Sulfoconjugates

Ist Teil von

• Journal of cardiovascular pharmacology, 1985-11, Vol.7 (6), p.1198-1204

Ort / Verlag

Philadelphia, PA: Lippincott-Raven Publishers

Erscheinungsjahr

1985

Quelle

MEDLINE

Beschreibungen/Notizen

• The 3- and 4-sulfate esters of dopamine (DA-3-SO4 and DA-4-SO4, respectively), the two main metabolites of DA, were evaluated for potential intrinsic or indirect catecholaminergic activities. Both compounds lacked any appreciable affinities for α1, α2, β1, β2 and DA-2 receptors. In the superfused [H]norepinephrine-preloaded dog saphenous vein, both dopamine sulfates were devoid of any intrinsic inhibitory activity such as observed with dopamine pre- and postsynaptically. In addition, they did not displace the labeled vesicular neurotransmitter as did dopamine. In anesthetized dogs the two compounds failed to stimulate either the dopaminergic receptors (DA-1) of mesenteric vascular beds or the adrenergic receptors mediating the vasodilatory and pressor responses to dopamine. ConclusionIn our experimental conditions DA-3-SO4 and DA-4-SO4, the products of dopamine sulfoconjugation, lacked any demonstrable intrinsic affinity and/or efficacy on the dopaminergic and adrenergic receptors directly or indirectly (a) through their metabolic transformation or (b) through displacement of endogenous neurotransmitter.