Eptapiron
Eptapiron (F-11,440) je veoma potentan i visoko selektivan pun agonist 5-HT1A receptora iz azapironske klase.[1][2] Njegov afinitet za 5-HT1A receptor je 4.8 nM (Ki) ili 8.33 (pKi), a njegova intrinsična aktivnost je 100%, i.e. jednaka je sa serotoninom.[1]
 | |
| IUPAC ime | |
|---|---|
4-metil-2-[4-(4-pirimidin-2-ilpiperazin-1-il)butil]-1,2,4-triazin-3,5-dion | |
| Klinički podaci | |
| Način primene | Oralno |
| Pravni status | |
| Pravni status |
|
| Farmakokinetički podaci | |
| Poluvreme eliminacije | ~2 sata |
| Identifikatori | |
| CAS broj | 179756-85-5  |
| ATC kod | none |
| PubChem | CID 208928 |
| ChemSpider | 181024 |
| UNII | 3M824XRO8N |
| Hemijski podaci | |
| Formula | C16H23N7O2 |
| Molarna masa | 345,40 g/mol |
Eptapiron i srodna jedinjenja, poput F-13,640 i F-15,599, su razvijena jer se smatralo da je visoka efikasnost aktivacije receptora neohodna da bi se proizvela maksimalna terapeutska korist stimulacije 5-HT1A receptora.[1][2][3][4]
References
уреди- ^ а б в Koek W; Patoiseau JF; Assié MB; et al. (1998). „F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential”. The Journal of Pharmacology and Experimental Therapeutics. 287 (1): 266—83. PMID 9765347.
- ^ а б Prinssen EP, Colpaert FC, Koek W (2002). „5-HT1A receptor activation and anti-cataleptic effects: high-efficacy agonists maximally inhibit haloperidol-induced catalepsy”. European Journal of Pharmacology. 453 (2-3): 217—21. PMID 12398907. doi:10.1016/S0014-2999(02)02430-5.
- ^ Koek W; Vacher B; Cosi C; et al. (2001). „5-HT1A receptor activation and antidepressant-like effects: F 13714 has high efficacy and marked antidepressant potential”. European Journal of Pharmacology. 420 (2-3): 103—12. PMID 11408031. doi:10.1016/S0014-2999(01)01011-1.
- ^ Maurel JL, Autin JM, Funes P, Newman-Tancredi A, Colpaert F, Vacher B (2007). „High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity”. Journal of Medicinal Chemistry. 50 (20): 5024—33. PMID 17803293. doi:10.1021/jm070714l.
