Robalzotan Explained

Robalzotan (NAD-299, AZD-7371) is a selective antagonist at the 5-HT_1A 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-HT_1A 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

• Ebalzotan
• UH-301

Notes and References

1. 10.1016/S0014-2999(98)00667-0 . Jerning E, Svantesson GT, Mohell N . Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. . Eur J Pharmacol . 360 . 2–3 . 219–225 . 1998 . 9851589 .
2. 10.1016/S0014-2999(99)00592-0 . Arborelius L, Wallsten C, Ahlenius S, Svensson TH . The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing. . Eur J Pharmacol . 382 . 2 . 133–138 . 1999 . 10528148 .
3. Mucke HA. . Robalzotan AstraZeneca. . Curr Opin Investig Drugs . 1 . 2 . 236–240 . 2000 . 11249580 .
4. 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 . The American Journal of Gastroenterology . 103 . 10 . 2562–9 . October 2008 . 18775020 . 10.1111/j.1572-0241.2008.02115.x .