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]
 | |
| Clinical data | |
|---|---|
| Other names | Isamoltan; CGP-361A; CGP361A |
| Drug class | Beta blocker; Serotonin 5-HT1A receptor antagonist; Serotonin 5-HT1B receptor antagonist |
| ATC code |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C16H22N2O2 |
| Molar mass | 274.364 g·mol−1 |
| 3D model (JSmol) | |
| |
See also
editReferences
edit- 1 2 "Isamoltan". AdisInsight. 7 April 1999. Retrieved 11 December 2024.
- ↑ 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.
- ↑ 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.
- ↑ 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.