Robalzotan (NAD-299, AZD-7371) is a selective antagonist at the 5-HT1A receptor. 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. It was subsequently investigated by AstraZeneca as a potential antidepressant but like many other 5-HT1A ligands was discontinued. Later on it was researched for other indications such as irritable bowel syndrome but was dropped once again.
- ↑ 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.
- ↑ 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.
- ↑ Mucke HA. (2000). "Robalzotan AstraZeneca.". Curr Opin Investig Drugs. 1 (2): 236–240. PMID 11249580.
- ↑ 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.