Robalzotan

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Robalzotan
Robalzotan.png
Systematic (IUPAC) name
(3R)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2H-chromene-5-carboxamide
Clinical data
Legal status
  • Uncontrolled
Routes Oral
Identifiers
CAS number 169758-66-1 YesY
ATC code None
PubChem CID 3055171
ChemSpider 2316732
UNII I18M56OGME YesY
Chemical data
Formula C18H23FN2O2 
Mol. mass 318.174 g/mol
 YesY (what is this?)  (verify)

Robalzotan (NAD-299, AZD-7371) is a selective antagonist at the 5-HT1A receptor.[1] It was shown to completely reverse the autoreceptor-mediated inhibition of serotonin release induced by the administration of selective serotonin reuptake inhibitors like citalopram in rodent studies.[2] It was subsequently investigated by AstraZeneca as a potential antidepressant but like many other 5-HT1A ligands was discontinued.[3] Later on it was researched for other indications such as irritable bowel syndrome but was dropped once again.[4]

See also[edit]

References[edit]

  1. ^ Jerning E, Svantesson GT, Mohell N. (1998). "Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist.". Eur J Pharmacol. 360 (2-3): 219–225. doi:10.1016/S0014-2999(98)00667-0. PMID 9851589. 
  2. ^ Arborelius L, Wallsten C, Ahlenius S, Svensson TH. (1999). "The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing.". Eur J Pharmacol. 382 (2): 133–138. doi:10.1016/S0014-2999(99)00592-0. PMID 10528148. 
  3. ^ Mucke HA. (2000). "Robalzotan AstraZeneca.". Curr Opin Investig Drugs. 1 (2): 236–240. PMID 11249580. 
  4. ^ Drossman DA, Danilewitz M, Naesdal J, Hwang C, Adler J, Silberg DG (October 2008). "Randomized, double-blind, placebo-controlled trial of the 5-HT1A receptor antagonist AZD7371 tartrate monohydrate (robalzotan tartrate monohydrate) in patients with irritable bowel syndrome". The American Journal of Gastroenterology 103 (10): 2562–9. doi:10.1111/j.1572-0241.2008.02115.x. PMID 18775020.