Isamoltane

Drug used in scientific research
  • none
Identifiers
  • 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 Edit this at Wikidata
Chemical and physical dataFormulaC16H22N2O2Molar mass274.364 g·mol−13D model (JSmol)
  • Interactive image
  • 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]

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-Schmiedeberg's 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-Schmiedeberg's Arch Pharmacol. 337 (6): 609–620. doi:10.1007/bf00175785. PMID 2905765. S2CID 23742271.
  • v
  • t
  • e
Anxiolytics (N05B)
5-HT1ARTooltip 5-HT1A receptor agonists
GABAARTooltip GABAA receptor PAMsTooltip positive allosteric modulatorsHypnoticsGabapentinoids
(α2δ VDCC blockers)Antidepressants
AntipsychoticsSympatholytics
(Antiadrenergics)Others
  • v
  • t
  • e
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
  • See also: Receptor/signaling modulators
  • Dopaminergics
  • Serotonergics
  • Monoamine reuptake inhibitors
  • Monoamine releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins
  • v
  • t
  • e
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins