Isamoltane

Isamoltane
Clinical data
Other names	Isamoltan; CGP-361A; CGP361A
Drug class	Beta blocker; Serotonin 5-HT1A receptor antagonist; Serotonin 5-HT1B receptor antagonist
ATC code	None;
Identifiers
	IUPAC name 1-(propan-2-ylamino)-3-(2-pyrrol-1-ylphenoxy)propan-2-ol;
CAS Number	99740-06-4;
PubChem CID	127403;
ChemSpider	113051;
UNII	214SP5P1EX;
CompTox Dashboard (EPA)	DTXSID00912513 ;
Chemical and physical data
Formula	C16H22N2O2
Molar mass	274.364 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES OC(CNC(C)C)COc1ccccc1n2cccc2;

Isamoltane (developmental code name CGP-361A) is a beta blocker (β-adrenergic receptor antagonist) with additional serotonin 5-HT_1A and 5-HT_1B receptor antagonist activity.^[1]^[2] It has about 5-fold higher affinity for the serotonin 5-HT_1B receptor (K_i = 21 nM) over the serotonin 5-HT_1A receptor (K_i = 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]

References

^ ^a ^b "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.

[AdisInsight-1] "Isamoltan". AdisInsight. 7 April 1999. Retrieved 11 December 2024.

[pmid8093601-2] 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.

[pmid1674359-3] 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.

[pmid2905765-4] 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.

[1]

[2]

[3]

[4]

See also

References