Article · Wikipedia archive · Last revised Jun 22, 2026

Isamoltane

Isamoltane is a beta blocker with additional serotonin 5-HT1A and 5-HT1B receptor antagonist activity. It has about 5-fold higher affinity for the serotonin 5-HT1B receptor over the serotonin 5-HT1A receptor. 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.

Last revised
Jun 22, 2026
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Isamoltane
Clinical data
Other namesIsamoltan; CGP-361A; CGP361A
Drug classBeta blocker; Serotonin 5-HT1A receptor antagonist; Serotonin 5-HT1B receptor antagonist
ATC code
  • None
Identifiers
  • 1-(propan-2-ylamino)-3-(2-pyrrol-1-ylphenoxy)propan-2-ol
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H22N2O2
Molar mass274.364 g·mol−1
3D model (JSmol)
  • OC(CNC(C)C)COc1ccccc1n2cccc2

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.12 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

See also

References

References

  1. "Isamoltan". AdisInsight. 7 April 1999. Retrieved 11 December 2024.
  2. Langlois M, Brémont B, Rousselle D, Gaudy F (1993). "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. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.
  3. Rényi L, Larsson LG, Berg S, Svensson BE, Thorell G, Ross SB (1991). "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. doi:10.1007/bf00180669. PMID 1674359. S2CID 23397251.
  4. Waldmeier PC, Williams M, Baumann PA, Bischoff S, Sills MA, Neale RF (1988). "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. doi:10.1007/bf00175785. PMID 2905765. S2CID 23742271.