Робалзотан

Робалзотан
Изображение химической структуры
Химическое соединение
ИЮПАК (3R)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2H-chromene-5-carboxamide
Брутто-формула C18H23FN2O2
Молярная масса 318.174 г/моль
CAS 169758-66-1
PubChem 3055171
DrugBank DB06538
Состав
Способы введения
Oral

Робалзотан (NAD-299, AZD-7371) — селективный антагонист 5-HT1A-рецепторов.[1] Он способен полностью снимать вызываемое ауторецепторами угнетение выброса серотонина, наблюдаемое в начале воздействия СИОЗС, таких, как эсциталопрам, в экспериментах на грызунах.[2] Он исследовался фирмой «Астра Зенека» в качестве потенциального антидепрессанта, но, подобно многим другим 5-HT1A-агонистам и антагонистам, его дальнейшая разработка была прекращена.[3] Позже робалзотан исследовался для других целей, таких, как синдром раздраженного кишечника, но был снова отвергнут.[4]

См. также

Примечания

  1. ↑ Jerning E., Svantesson G.T., Mohell N. Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. (англ.) // Eur J Pharmacol.[англ.] : journal. — 1998. — Vol. 360, no. 2—3. — P. 219—225. — doi:10.1016/S0014-2999(98)00667-0. — PMID 9851589.
  2. ↑ Arborelius L., Wallsten C., Ahlenius S., Svensson TH. The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing. (англ.) // Eur J Pharmacol.[англ.] : journal. — 1999. — Vol. 382, no. 2. — P. 133—138. — doi:10.1016/S0014-2999(99)00592-0. — PMID 10528148.
  3. ↑ Mucke HA. Robalzotan AstraZeneca. (неопр.) // Curr Opin Investig Drugs.. — 2000. — Т. 1, № 2. — С. 236—240. — PMID 11249580.
  4. ↑ Drossman D.A., Danilewitz M., Naesdal J., Hwang C., Adler J., Silberg D.G. Randomized, double-blind, placebo-controlled trial of the 5-HT1A receptor antagonist AZD7371 tartrate monohydrate (robalzotan tartrate monohydrate) in patients with irritable bowel syndrome (англ.) // The American Journal of Gastroenterology[англ.] : journal. — 2008. — October (vol. 103, no. 10). — P. 2562—2569. — doi:10.1111/j.1572-0241.2008.02115.x. — PMID 18775020.

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