SB-242,084
(IUPAC ) ime
6-hloro-5-metil-N -{6-[(2-metilpiridin-3-il)oksi]piridin-3-il]indolin-1-karboksamid
Klinički podaci
Identifikatori
CAS broj
181632-25-7
ATC kod
nije dodeljen
PubChem [ 1] [ 2]
3644637
ChEMBL [ 3]
CHEMBL14563
Hemijski podaci
Formula
C 21 H 19 Cl N 4 O 2
Mol. masa
394,853 g/mol
SMILES
eMolekuli & PubHem
InChI
InChI=1S/C21H19ClN4O2/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27) Y Key: GIUZEIJUFOPTMR-UHFFFAOYSA-N Y
Farmakoinformacioni podaci
Trudnoća
?
Pravni status
SB-242,084 je psihoaktivni lek i istraživačka hemikalija koja deluje kao selektivni antagonist za 5HT2C receptor .[ 4] On ima anksiolitičko dejstvo,[ 5] i pojačava dopaminsku signalizaciju u limbičnom sistemu .[ 6] On takođe ima kompleksno dejstvo na otpuštanje dopamina proizvedeno kokainom , povećavajući ga u pojedinim delovima mozga[ 7] [ 8] i snižavajući ga u drugim.[ 9] [ 10] Pokazano je da povišava efektivnost selektivnih inhibitora preuzimanja serotonina (SSRI), i da redukuje njihove nuspojave.[ 11] [ 12] U životinjskim studijama, SB-242,084 proizvodi stimulansnu aktivnost, koja je donekle slična ali znatno slabija od kokaina i amfetamina.[ 13]
↑ 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 .
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI :10.1093/nar/gkr777 . PMID 21948594 . edit
↑ Kennett, GA; Wood, MD; Bright, F; Trail, B; Riley, G; Holland, V; Avenell, KY; Stean, T i dr.. (1997). „SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist”. Neuropharmacology 36 (4–5): 609–20. DOI :10.1016/S0028-3908(97)00038-5 . PMID 9225286 .
↑ Martin, JR; Ballard, TM; Higgins, GA (2002). „Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety” . Pharmacology, Biochemistry, and Behavior 71 (4): 615–25. DOI :10.1016/S0091-3057(01)00713-4 . PMID 11888553 .
↑ Di Matteo, V; Di Giovanni, G; Di Mascio, M; Esposito, E (1999). „SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system” . Neuropharmacology 38 (8): 1195–205. DOI :10.1016/S0028-3908(99)00047-7 . PMID 10462132 .
↑ Navailles, S; De Deurwaerdère, P; Porras, G; Spampinato, U (2004). „In vivo evidence that 5-HT2C receptor antagonist but not agonist modulates cocaine-induced dopamine outflow in the rat nucleus accumbens and striatum”. Neuropsychopharmacology 29 (2): 319–26. DOI :10.1038/sj.npp.1300329 . PMID 14560323 .
↑ Navailles, S; Moison, D; Ryczko, D; Spampinato, U (2006). „Region-dependent regulation of mesoaccumbens dopamine neurons in vivo by the constitutive activity of central serotonin2C receptors”. Journal of Neurochemistry 99 (4): 1311–9. DOI :10.1111/j.1471-4159.2006.04188.x . PMID 17018023 .
↑ Navailles, S; Moison, D; Cunningham, KA; Spampinato, U (2008). „Differential regulation of the mesoaccumbens dopamine circuit by serotonin2C receptors in the ventral tegmental area and the nucleus accumbens: an in vivo microdialysis study with cocaine”. Neuropsychopharmacology 33 (2): 237–46. DOI :10.1038/sj.npp.1301414 . PMID 17429406 .
↑ Leggio, GM; Cathala, A; Moison, D; Cunningham, KA; Piazza, PV; Spampinato, U (2009). „Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens” . Neuropharmacology 56 (2): 507–13. DOI :10.1016/j.neuropharm.2008.10.005 . PMC 3130963 . PMID 18977370 .
↑ Cremers, TI; Giorgetti, M; Bosker, FJ; Hogg, S; Arnt, J; Mørk, A; Honig, G; Bøgesø, KP i dr.. (2004). „Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade”. Neuropsychopharmacology 29 (10): 1782–9. DOI :10.1038/sj.npp.1300474 . PMID 15138437 .
↑ Burghardt, NS; Bush, DE; McEwen, BS; Ledoux, JE (2007). „Acute SSRIs Increase Conditioned Fear Expression: Blockade with a 5-HT2C Receptor Antagonist” . Biological Psychiatry 62 (10): 1111–8. DOI :10.1016/j.biopsych.2006.11.023 . PMC 2129095 . PMID 17524369 .
↑ Manvich, D. F.; Kimmel, H. L.; Cooper, D. A.; Howell, L. L. (2012). „The Serotonin 2C Receptor Antagonist SB 242084 Exhibits Abuse-Related Effects Typical of Stimulants in Squirrel Monkeys”. Journal of Pharmacology and Experimental Therapeutics . DOI :10.1124/jpet.112.195156 . PMID 22685342 .
Agonisti :
Azapironi :
Alnespiron •
Binospiron •
Buspiron •
Enilospiron •
Eptapiron •
Gepiron •
Ipsapiron •
Perospiron •
Revospiron •
Tandospiron •
Tiospiron •
Umespiron •
Zalospiron ;
Antidepresivi :
Etoperidon •
Nefazodon •
Trazodon ;
Antipsihotici :
Aripiprazol •
Asenapin •
Klozapin •
Kvetiapin •
Ziprasidon ;
Ergolini :
Dihidroergotamin •
Ergotamin •
Lisurid •
Metisergid •
LSD ;
Triptamini :
5-CT •
5-MeO-DMT •
5-MT •
Bufotenin •
DMT •
Indorenat •
Psilocin •
Psilocibin ;
Drugi :
8-OH-DPAT •
Adatanserin •
Bay R 1531 •
Befiradol •
BMY-14802 •
Kanabidiol •
Dimemebfe •
Ebalzotan •
Eltoprazin •
F-11,461 •
F-12,826 •
F-13,714 •
F-14,679 •
F-15,063 •
F-15,599 •
Flesinoksan •
Flibanserin •
Lesopitron •
Lu AA21004 •
LY-293,284 •
LY-301,317 •
MKC-242 •
NBUMP •
Osemozotan •
Oksaflozan •
Pardoprunoks •
Piklozotan •
Rauvolscin •
Repinotan •
Roksindol •
RU-24,969 •
S 14,506 •
S-14,671 •
S-15,535 •
Sarizotan •
SSR-181,507 •
Sunepitron •
U-92,016-A •
Urapidil •
Vilazodon •
Ksaliproden •
Johimbin Antagonisti :
Antipsihotici :
Iloperidon •
Risperidon •
Sertindol ;
Beta blokatori :
Alprenolol •
Cianopindolol •
Jodocianopindolol •
Oksprenolol •
Pindobind •
Pindolol •
Propranolol •
Tertatolol ;
Drugi :
AV965 •
BMY-7,378 •
CSP-2503 •
Dotarizin •
Flopropion •
GR-46611 •
Isamoltan •
Lekozotan •
Metitepin/Metiotepin •
MPPF •
NAN-190 •
PRX-00023 •
Robalzotan •
S-15535 •
SB-649,915 •
SDZ 216-525 •
Spiperon •
Spiramid •
Spiroksatrin •
UH-301 •
WAY-100,135 •
WAY-100,635 •
Ksilamidin Agonisti :
Lisergamidi :
Dihidroergotamin •
Metisergid ;
Triptani :
Almotriptan •
Avitriptan •
Eletriptan •
Frovatriptan •
Naratriptan •
Rizatriptan •
Sumatriptan •
Zolmitriptan ;
Triptamini :
5-CT •
5-Etil-DMT •
5-MT •
5-(Noniloksi)triptamin ;
Drugi :
CP-135,807 •
CP-286,601 •
GR-46611 •
L-694,247 •
L-772,405 •
PNU-109,291 •
PNU-142,633 Antagonisti :
Lisergamidi :
Metergolin ;
Drugi :
Alniditan •
BRL-15,572 •
Elzasonan •
GR-127,935 •
Ketanserin •
LY-310,762 •
LY-367,642 •
LY-456,219 •
LY-456,220 •
Metitepin/Metiotepin •
Ritanserin •
Johimbin •
Ziprasidon
Agonisti :
Fenetilamini :
2C-B •
2C-E •
2C-I •
2C-T-2 •
2C-T-7 •
2C-T-21 •
DOB •
DOC •
DOI •
DOM •
MDA •
MDMA •
Meskalin ;
Piperazini :
Aripiprazol •
mCPP •
TFMPP ;
Triptamini :
5-CT •
5-MeO-α-ET •
5-MeO-α-MT •
5-MeO-DET •
5-MeO-DiPT •
5-MeO-DMT •
5-MeO-DPT •
5-MT •
α-ET •
α-Metil-5-HT •
α-MT •
Bufotenin •
DET •
DiPT •
DMT •
DPT •
Psilocin •
Psilocibin ;
Drugi :
A-372,159 •
AL-38022A •
CP-809,101 •
Dimemebfe •
Lorkaserin •
Medifoksamin •
MK-212 •
Org 12,962 •
ORG-37,684 •
Oksaflozan •
PNU-22394 •
Ro60-0175 •
Ro60-0213 •
Vabicaserin •
WAY-629 •
WAY-161,503 •
YM-348 Antagonisti :
Atipični antipsihotici :
Klozapin •
Iloperidon •
Melperon •
Olanzapin •
Paliperidon •
Pimozid •
Hetiapin •
Risperidon •
Sertindol •
Ziprasidon •
Zotepin ;
Tipični antipsihotici :
Hlorpromazin •
Loksapin •
Pipamperon ;
Antidepresivi :
Agomelatin •
Amitriptilin •
Amoksapin •
Aptazapin •
Etoperidon •
Fluoksetin •
Mianserin •
Mirtazapin •
Nefazodon •
Nortriptilin •
Trazodon ;
Drugi :
Adatanserin •
Cinanserin •
Ciproheptadin •
Deramciklan •
Dotarizin •
Eltoprazin •
Esmirtazapin •
FR-260,010 •
Ketanserin •
Ketotifen •
Latrepirdin •
Lu AA24530 •
Metitepin/Metiotepin •
Metisergid •
Pizotifen •
Ritanserin •
RS-102,221 •
S-14,671 •
SB-200,646 •
SB-206,553 •
SB-221,284 •
SB-228,357 •
SB-242,084 •
SB-243,213 •
SDZ SER-082 •
Ksilamidin
Agonisti :
Lisergamidi :
Dihidroergotamin •
Ergotamin •
Lisurid •
LSD •
Mesulergin •
Metergolin •
Metisergid ;
Triptamini :
2-Metil-5-HT •
5-BT •
5-CT •
5-MT •
Bufotenin •
E-6801 •
E-6837 •
EMD-386,088 •
EMDT •
LY-586,713 •
N -Metil-5-HT •
Triptamin ;
Drugi :
WAY-181,187 •
WAY-208,466 Antagonisti :
Antidepresanti :
Amitriptilin •
Amoksapin •
Klomipramin •
Doksepin •
Mianserin •
Nortriptilin ;
Atipični antipsihotici :
Aripiprazol •
Asenapin •
Klozapin •
Fluperlapin •
Iloperidon •
Olanzapin •
Tiospiron ;
Tipični antipsihotici :
Hlorpromazin •
Loksapin ;
Drugi :
BGC20-760 •
BVT-5182 •
BVT-74316 •
EGIS-12,233 •
GW-742,457 •
Ketanserin •
Latrepirdin •
Lu AE58054 •
Metitepin/Metiotepin •
MS-245 •
PRX-07034 •
Ritanserin •
Ro04-6790 •
Ro 63-0563 •
SB-258,585 •
SB-271,046 •
SB-357,134 •
SB-399,885 •
SB-742,457 Agonisti :
Lisergamidi :
LSD ;
Triptamini :
5-CT •
5-MT •
Bufotenin ;
Drugi :
8-OH-DPAT •
AS-19 •
Bifeprunoks •
LP-12 •
LP-44 •
RU-24,969 •
Sarizotan Antagonisti :
Lisergamidi :
2-Bromo-LSD •
Bromokriptin •
Dihidroergotamin •
Ergotamin •
Mesulergin •
Metergolin •
Metisergid ;
Antidepresanti :
Amitriptilin •
Amoksapin •
Klomipramin •
Imipramin •
Maprotilin •
Mianserin ;
Atipični antipsihotici :
Amisulprid •
Aripiprazol •
Klozapin •
Olanzapin •
Risperidon •
Sertindol •
Tiospiron •
Ziprasidon •
Zotepin ;
Tipični antipsihotici :
Hlorpromazin •
Loksapin ;
Drugi :
Butaklamol •
EGIS-12,233 •
Ketanserin •
LY-215,840 •
Metitepin/Metiotepin •
Pimozid •
Ritanserin •
SB-258,719 •
SB-258,741 •
SB-269,970 •
SB-656,104 •
SB-656,104-A •
SB-691,673 •
SLV-313 •
SLV-314 •
Spiperon •
SSR-181,507