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Novel H3 receptor antagonists with improved pharmacokinetic profiles
- Source :
- Bioorganic & Medicinal Chemistry Letters. 18:4133-4136
- Publication Year :
- 2008
- Publisher :
- Elsevier BV, 2008.
-
Abstract
- A new series of H 3 antagonists derived from the natural product Conessine are presented. Several compounds from these new series retain the potency and selectivity of earlier diamine based analogs while exhibiting improved PK characteristics. One compound ( 3u ) demonstrated functional antagonism of the H 3 receptor in an in vivo pharmacological model.
- Subjects :
- Central Nervous System
Stereochemistry
Chemistry, Pharmaceutical
Clinical Biochemistry
Histamine Antagonists
Pharmaceutical Science
Pharmacology
Binding, Competitive
Biochemistry
Chemical synthesis
Structure-Activity Relationship
chemistry.chemical_compound
Alkaloids
Pharmacokinetics
In vivo
Drug Discovery
Animals
Receptors, Histamine H3
Potency
Receptor
Molecular Biology
Natural product
Molecular Structure
Organic Chemistry
Rats
Kinetics
Conessine
Models, Chemical
chemistry
Drug Design
Molecular Medicine
Histamine H3 receptor
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 18
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....8a3e31fcd35211c56f91ff3a94e95619
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.05.086