Eptapiron

Eptapiron
(IUPAC) ime
	4-metil-2-[4-(4-pirimidin-2-ilpiperazin-1-il)butil]-1,2,4-triazin-3,5-dion
Klinički podaci
Identifikatori
CAS broj	179756-85-5
ATC kod	nije dodeljen
PubChem	208928
ChemSpider	181024
UNII	3M824XRO8N
Hemijski podaci
Formula	C16H23N7O2
Mol. masa	345,40 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C16H23N7O2/c1-20-14(24)13-19-23(16(20)25)8-3-2-7-21-9-11-22(12-10-21)15-17-5-4-6-18-15/h4-6,13H,2-3,7-12H2,1H3 ; Key: NMYAHEULKSYAPP-UHFFFAOYSA-N
Farmakokinetički podaci
Poluvreme eliminacije	~2 sata
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Uncontrolled
Način primene	Oralno

Eptapiron (F-11,440) je veoma potentan i visoko selektivan pun agonist 5-HT_1A receptora iz azapironske klase.^[4]^[5] Njegov afinitet za 5-HT_1A receptor je 4.8 nM (K_i) ili 8.33 (pK_i), a njegova intrinsična aktivnost je 100%, i.e. jednaka je sa serotoninom.^[4]

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-HT_1A receptora.^[4]^[5]^[6]^[7]

References uredi

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ ^4,0 ^4,1 ^4,2 Koek W, Patoiseau JF, Assié MB, et al. (October 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.
↑ ^5,0 ^5,1 Prinssen EP, Colpaert FC, Koek W (October 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. DOI:10.1016/S0014-2999(02)02430-5. PMID 12398907.
↑ Koek W, Vacher B, Cosi C, et al. (May 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. DOI:10.1016/S0014-2999(01)01011-1. PMID 11408031.
↑ Maurel JL, Autin JM, Funes P, Newman-Tancredi A, Colpaert F, Vacher B (October 2007). „High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity”. Journal of Medicinal Chemistry 50 (20): 5024–33. DOI:10.1021/jm070714l. PMID 17803293.

Vidi još uredi

Spoljašnje veze uredi

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[pmid9765347-4] 4,0 ^4,1 ^4,2 Koek W, Patoiseau JF, Assié MB, et al. (October 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.

[pmid12398907-5] 5,0 ^5,1 Prinssen EP, Colpaert FC, Koek W (October 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. DOI:10.1016/S0014-2999(02)02430-5. PMID 12398907.

[pmid11408031-6] Koek W, Vacher B, Cosi C, et al. (May 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. DOI:10.1016/S0014-2999(01)01011-1. PMID 11408031.

[pmid17803293-7] Maurel JL, Autin JM, Funes P, Newman-Tancredi A, Colpaert F, Vacher B (October 2007). „High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity”. Journal of Medicinal Chemistry 50 (20): 5024–33. DOI:10.1021/jm070714l. PMID 17803293.

[4]

[5]

[1]

[2]

[3]

[6]

[7]