Robalzotan ( NAD-299 , AZD-7371 ) is a selective antagonist of 5-HT 1A receptors . [1] It is able to completely eliminate the inhibition of serotonin release caused by autoreceptors, observed at the beginning of exposure to SSRIs , such as escitalopram , in rodent experiments. [2] It was investigated by Astra Zeneca as a potential antidepressant , but, like many other 5-HT 1A agonists and antagonists, its further development was discontinued. [3] Robalzotan was later investigated for other purposes, such as irritable bowel syndrome , but was again rejected. [four]
| Robalsotan | |
|---|---|
 | |
| Chemical compound | |
| IUPAC | (3 R ) -3- [di (cyclobutyl) amino] -8-fluoro-3,4-dihydro-2 H -chromene-5-carboxamide |
| Gross formula | C 18 H 23 FN 2 O 2 |
| Molar mass | 318.174 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| Route of administration | |
| Oral | |
See also
- Ebalzotan
- UH-301
- Tianeptine
Notes
- ↑ Jerning E., Svantesson GT, Mohell N. Receptor binding characteristics of [3H] NAD-299, a new selective 5-HT1A receptor antagonist. (English) // Eur J Pharmacol. : journal. - 1998. - Vol. 360 , no. 2-3 . - P. 219-225 . - DOI : 10.1016 / S0014-2999 (98) 00667-0 . - PMID 9851589 .
- ↑ Arborelius L., Wallsten C., Ahlenius S., Svensson TH. The 5-HT (1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing. (English) // Eur J Pharmacol. : journal. - 1999. - Vol. 382 , no. 2 . - P. 133-138 . - DOI : 10.1016 / S0014-2999 (99) 00592-0 . - PMID 10528148 .
- ↑ Mucke HA. Robalzotan AstraZeneca. (neopr.) // Curr Opin Investig Drugs .. - 2000. - T. 1 , No. 2 . - S. 236-240 . - PMID 11249580 .
- ↑ Drossman DA, Danilewitz M., Naesdal J., Hwang C., Adler J., Silberg DG Randomized, double-blind, placebo-controlled trial of the 5-HT1A receptor antagonist AZD7371 tartrate monohydrate (robalzotan tartrate monohydrate) in patients with irritable bowel syndrome (eng.) // The American Journal of Gastroenterology : journal. - 2008 .-- October ( vol. 103 , no. 10 ). - P. 2562-2569 . - DOI : 10.1111 / j.1572-0241.2008.02115.x . - PMID 18775020 .