Chemistry:Isamoltane

From HandWiki

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.[1][2] It has about 5-fold higher affinity for the serotonin 5-HT1B receptor (Ki = 21 nM) over the serotonin 5-HT1A receptor (Ki = 112 nM).[3] It has anxiolytic effects in rodents.[4] The drug was under development by Novartis and AstraZeneca for the treatment of anxiety disorders in the 1990s but was never marketed.[1]

See also

References

  1. ↑ 1.0 1.1 "Isamoltan". 7 April 1999. https://adisinsight.springer.com/drugs/800000697. 
  2. ↑ "Structural analysis by the comparative molecular field analysis method of the affinity of beta-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptors". Eur. J. Pharmacol. 244 (1): 77–87. 1993. doi:10.1016/0922-4106(93)90061-d. PMID 8093601. 
  3. ↑ "Biochemical and behavioural effects of isamoltane, a beta-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain.". Naunyn-Schmiedeberg's Arch Pharmacol 343 (1): 1–6. 1991. doi:10.1007/bf00180669. PMID 1674359. 
  4. ↑ "Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1 receptor subtypes in the rat brain.". Naunyn-Schmiedeberg's Arch Pharmacol 337 (6): 609–620. 1988. doi:10.1007/bf00175785. PMID 2905765. 



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