Isamoltane Explained

Iupac Name:1-(propan-2-ylamino)-3-(2-pyrrol-1-ylphenoxy)propan-2-ol
Cas Number:99740-06-4
Unii:214SP5P1EX
Atc Prefix:none
Pubchem:127403
Chemspiderid:113051
C:16
H:22
N:2
O:2
Smiles:OC(CNC(C)C)COc1ccccc1n2cccc2

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]

Notes and References

  1. Langlois M, Brémont B, Rousselle D, Gaudy F . 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 . 8093601 . 10.1016/0922-4106(93)90061-d.
  2. Rényi L, Larsson LG, Berg S, Svensson BE, Thorell G, Ross SB . 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 . 1674359 . 10.1007/bf00180669. 23397251 .
  3. Waldmeier PC, Williams M, Baumann PA, Bischoff S, Sills MA, Neale RF . 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 . 2905765 . 10.1007/bf00175785. 23742271 .