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Hydrazides of clozapine: A new class of D1 dopamine receptor subtype selective antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 16:4543-4547
- Publication Year :
- 2006
- Publisher :
- Elsevier BV, 2006.
-
Abstract
- Acylated and aroylated hydrazinoclozapines are highly potent dopamine D1 antagonists that show remarkable selectivity over other dopamine receptors. The most potent compound in this series is the 2,6-dimethoxybenzhydrazide 33 with a D1 Ki of 1.6 nM and 212-fold selectivity over D2 receptor.
- Subjects :
- Clinical Biochemistry
Pharmaceutical Science
Pharmacology
Biochemistry
Chemical synthesis
Structure-Activity Relationship
Dopamine
Dopamine receptor D2
Drug Discovery
medicine
Clozapine
Molecular Biology
Molecular Structure
Receptors, Dopamine D2
Chemistry
Receptors, Dopamine D1
Organic Chemistry
Antagonist
In vitro
Dopamine D2 Receptor Antagonists
Hydrazines
Dopamine receptor
Dopamine Antagonists
Molecular Medicine
Selectivity
medicine.drug
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....f2a1fa2549bd7d7c463641e9c2c93277
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.06.022