Synonym
Isamoltane; CGP361A; CGP-361A; CGP 361A
IUPAC/Chemical Name
2-Propanol, 1-((1-methylethyl)amino)-3-(2-(1H-pyrrol-1-yl)phenoxy)-, monohydrochloride
InChi Key
DCOXRJZVVPMXLY-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H22N2O2.ClH/c1-13(2)17-11-14(19)12-20-16-8-4-3-7-15(16)18-9-5-6-10-18;/h3-10,13-14,17,19H,11-12H2,1-2H3;1H
SMILES Code
OC(COC1=CC=CC=C1N2C=CC=C2)CNC(C)C.[H]Cl
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
310.82
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: 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 Schmiedebergs Arch Pharmacol. 1988 Jun;337(6):609-20. doi: 10.1007/BF00175785. PMID: 2905765.
2: Bauer K, Dietersdorfer F, Kaik G. Assessment of beta-adrenergic receptor blockade after isamoltane, a 5-HT1-receptor active compound, in healthy volunteers. Clin Pharmacol Ther. 1993 Jun;53(6):675-83. doi: 10.1038/clpt.1993.89. PMID: 8099863.
3: 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 Schmiedebergs Arch Pharmacol. 1991 Jan;343(1):1-6. doi: 10.1007/BF00180669. PMID: 1674359.
4: Hoyer D, Schoeffter P, Waeber C, Palacios JM. Serotonin 5-HT1D receptors. Ann N Y Acad Sci. 1990;600:168-81; discussion 181-2. doi: 10.1111/j.1749-6632.1990.tb16880.x. PMID: 2252308.
5: Middlemiss DN, Hutson PH. The 5-HT1B receptors. Ann N Y Acad Sci. 1990;600:132-47; discussion 347-48. doi: 10.1111/j.1749-6632.1990.tb16878.x. PMID: 2252306.
6: Lian L, Xu Y, Zhang J, Yu Y, Zhu N, Guan X, Huang H, Chen R, Chen J, Shi G, Pan J. Antidepressant-like effects of a novel curcumin derivative J147: Involvement of 5-HT1A receptor. Neuropharmacology. 2018 Jun;135:506-513. doi: 10.1016/j.neuropharm.2018.04.003. Epub 2018 Apr 5. PMID: 29626566.
7: Dawson LA, Nguyen HQ. The role of 5-HT(1A) and 5-HT(1B/1D) receptors on the modulation of acute fluoxetine-induced changes in extracellular 5-HT: the mechanism of action of (+/-)pindolol. Neuropharmacology. 2000 Apr 3;39(6):1044-52. doi: 10.1016/s0028-3908(99)00192-6. PMID: 10727715.
8: Nogueira RL, Graeff FG. 5-HT mediation of the antiaversive effect of isamoltane injected into the dorsal periaqueductal grey. Behav Pharmacol. 1991 Feb;2(1):73-77. doi: 10.1097/00008877-199102000-00010. PMID: 11224050.
9: Chia JSM, Omar Farouk AA, Mohamad AS, Sulaiman MR, Perimal EK. Zerumbone alleviates chronic constriction injury-induced allodynia and hyperalgesia through serotonin 5-HT receptors. Biomed Pharmacother. 2016 Oct;83:1303-1310. doi: 10.1016/j.biopha.2016.08.052. Epub 2016 Aug 27. PMID: 27570173.
10: Davidson C, Stamford JA. Synergism of 5-HT 1B/D antagonists with paroxetine on serotonin efflux in rat ventral lateral geniculate nucleus slices. Brain Res Bull. 1997;43(4):405-9. doi: 10.1016/s0361-9230(97)00026-9. PMID: 9241443.
