isamoltane

{{Short description|Drug used in scientific research}}

{{Infobox drug

| IUPAC_name = 1-(propan-2-ylamino)-3-(2-pyrrol-1-ylphenoxy)propan-2-ol

| image = Isamoltane.svg

| tradename =

| pregnancy_category =

| routes_of_administration =

| bioavailability =

| metabolism =

| elimination_half-life =

| excretion =

| CAS_number = 99740-06-4

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 214SP5P1EX

| ATC_prefix = none

| ATC_suffix =

| PubChem = 127403

| ChemSpiderID = 113051

| synonyms = Isamoltan; CGP-361A

| 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-HT_1A, and 5-HT_1B receptors.{{cite web | title=Isamoltan | website=AdisInsight | date=7 April 1999 | url=https://adisinsight.springer.com/drugs/800000697 | access-date=11 December 2024}}{{cite journal | vauthors = Langlois M, Brémont B, Rousselle D, Gaudy F | title = Structural analysis by the comparative molecular field analysis method of the affinity of beta-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptors | journal = Eur. J. Pharmacol. | volume = 244 | issue = 1 | pages = 77–87 | year = 1993 | pmid = 8093601 | doi = 10.1016/0922-4106(93)90061-d}} It has about five times the potency for the 5-HT_1B receptor (21 nmol/L) over the 5-HT_1A receptor (112 nmol/L).{{cite journal |vauthors=Rényi L, Larsson LG, Berg S, Svensson BE, Thorell G, Ross SB | title = Biochemical and behavioural effects of isamoltane, a beta-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain. | journal = Naunyn-Schmiedeberg's Arch Pharmacol | volume = 343 | issue = 1 | pages = 1–6 | year = 1991 | pmid = 1674359 | doi=10.1007/bf00180669| s2cid = 23397251 }} It has anxiolytic effects in rodents.{{cite journal |vauthors=Waldmeier PC, Williams M, Baumann PA, Bischoff S, Sills MA, Neale RF | title = Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1 receptor subtypes in the rat brain. | journal = Naunyn-Schmiedeberg's Arch Pharmacol | volume = 337 | issue = 6 | pages = 609–620 | year = 1988 | pmid = 2905765 | doi=10.1007/bf00175785| s2cid = 23742271 }}