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8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands
- Publication Year :
- 2016
-
Abstract
- The novel 8-piperazinyl-2,3-dihydropyrroloisoquinoline template was synthesized in nine steps. The template was N-substituted to give a series of compounds showing binding to human cloned 5-HT1A, 5-HT1B and 5-HT1D receptors with pKi’s greater than 9 and selectivities up to 1000-fold against other serotonin, dopamine and adrenergic receptors. Several compounds were shown to possess weak partial agonist activity in cloned receptors, which translated to antagonism in in vitro studies.
- Subjects :
- Adrenergic receptor
Stereochemistry
medicine.drug_class
Clinical Biochemistry
Administration, Oral
Biological Availability
Pharmaceutical Science
Ligands
Biochemistry
Partial agonist
Structure-Activity Relationship
Dopamine
Drug Discovery
medicine
Animals
Receptor
Molecular Biology
5-HT receptor
Brain Chemistry
Chemistry
Organic Chemistry
Isoquinolines
Receptor antagonist
Rats
Serotonin Receptor Agonists
Receptor, Serotonin, 5-HT1D
Receptors, Serotonin
Receptor, Serotonin, 5-HT1A
Receptor, Serotonin, 5-HT1B
Molecular Medicine
5-HT1 receptor
Serotonin Antagonists
Serotonin
medicine.drug
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....86421f00e16772e71fb543436a7895c9