Synthesis and pharmacological evaluation of N,N-di-n-propyldopamine congeners containing phenolic bioisosteres
| Autor: | Toni A. Petty, Joan M. Caroon, Mcclelland Deborah L, A. D. Michel, Robin D. Clark, Rosenkranz Roberto P, L. David Waterbury, Nancy E. Isaac |
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| Rok vydání: | 1987 |
| Předmět: |
Agonist
Male Chemical Phenomena Stereochemistry medicine.drug_class Dopamine Rat model Pharmaceutical Science Receptors Dopamine Renal Circulation chemistry.chemical_compound Stereospecificity Phenols In vivo Dopamine receptor D2 medicine Animals Sulfonamides Formamides Receptors Dopamine D2 Receptors Dopamine D1 Hemodynamics Rats Inbred Strains Rats Chemistry chemistry Selectivity Derivative (chemistry) |
| Zdroj: | Journal of pharmaceutical sciences. 76(5) |
| ISSN: | 0022-3549 |
| Popis: | A series of analogues of N,N-di-n-propyldopamine (DPDA) in which the 3-hydroxyl group was replaced by bioisosteric groups was prepared and evaluated for D1- and D2-receptor affinity. The 3-methane-sulfonamide analogue (18) had a higher affinity for the D2 receptor than DPDA and was more selective for the D2 receptor. The 3-formamide derivative (15) also retained significant D2 affinity. Both of these compounds demonstrated in vivo cardiovascular and renal profiles in an anesthetized rat model that were consistent with selective D2-receptor agonism. |
| Databáze: | OpenAIRE |
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