isamoltane
Sign in to saveAlso known as CGP-361A, isamoltan, (±)-isamoltane
Isamoltane (developmental code name CGP-361A) is a beta blocker (β-adrenergic receptor antagonist) with additional serotonin 5-HT1A and 5-HT1B receptor antagonist activity. It has about 5-fold higher affinity for the serotonin 5-HT1B receptor (Ki = 21nM) over the serotonin 5-HT1A receptor (Ki = 112nM). It has anxiolytic effects in rodents. The drug was under development by Novartis and AstraZeneca for the treatment of anxiety disorders in the 1990s but was never marketed.
Research
60 papers- The 5-HT1B receptors.Annals of the New York Academy of Sciences · 1990
- Serotonin 5-HT1D receptors.Annals of the New York Academy of Sciences · 1990
- Assessment of beta-adrenergic receptor blockade after isamoltane, a 5-HT1-receptor active compound, in healthy volunteers.Clinical pharmacology and therapeutics · 1993
- Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1 receptor subtypes in the rat brain.Naunyn-Schmiedeberg's archives of pharmacology · 1988
- Biochemical and behavioural effects of isamoltane, a beta-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain.Naunyn-Schmiedeberg's archives of pharmacology · 1991
via PubMed
Wikidata facts
- Mass
- 310.144805656
Show 3 more facts
- chemical formula
- C₁₆H₂₃ClN₂O₂
- canonical SMILES
- CC(C)NCC(COC1=CC=CC=C1N2C=CC=C2)O.Cl
- Commons category
- Isamoltane
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Article
2 sectionsContents
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- References
Isamoltane (developmental code name CGP-361A) is a beta blocker (β-adrenergic receptor antagonist) with additional serotonin 5-HT1A and 5-HT1B receptor antagonist activity. It has about 5-fold higher affinity for the serotonin 5-HT1B receptor (Ki = 21nM) over the serotonin 5-HT1A receptor (Ki = 112nM). It has anxiolytic effects in rodents. The drug was under development by Novartis and AstraZeneca for the treatment of anxiety disorders in the 1990s but was never marketed.
==See also== List of investigational anxiety disorder drugs