Isamoltane

Isamoltane (CGP-361A) is a drug used in scientific research. It acts as an antagonist at the β-adrenergic, 5-HT1A, and 5-HT1B receptors.[1] It has about five times the potency for the 5-HT1B receptor (21 nmol/l) over the 5-HT1A receptor (112 nmol/l).[2] It has anxiolytic effects in rodents.[3]

Isamoltane
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H22N2O2
Molar mass274.364 g·mol−1
3D model (JSmol)

References
  1. 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.
  2. 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 Schmiedebergs Arch Pharmacol. 343 (1): 1–6. doi:10.1007/bf00180669. PMID 1674359. S2CID 23397251.
  3. 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 Schmiedebergs Arch Pharmacol. 337 (6): 609–620. doi:10.1007/bf00175785. PMID 2905765. S2CID 23742271.
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