С Википедије, слободне енциклопедије
Pelanserin (TR2515) je antagonist 5-HT2 i α1-adrenergičkog receptora.[3]
Sinteza:[4][5] ~86%:[6] 40%:[7] NA:[8] Patenti:[9][10] Upotrebni patent:[11]
Reakcija između izatoičkog anhidrida (1) i 1-(3-aminopropil)-4-fenilpiperazina [20529-19-5] (2) sa fosgenom kompletira sintezu pelanserina (3).
- ^ 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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди
- ^ 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.
- ^ Villalobos-Molina, R; Ibarra, M; Hong, E (1995). „The 5-HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro”. European Journal of Pharmacology. 277 (2–3): 181—5. PMID 7493607. doi:10.1016/0014-2999(95)00074-u.
- ^ Hayao, Shin; Havera, Herbert J.; Strycker, Wallace G.; Leipzig, T. J.; Kulp, Richard A.; Hartzler, Harold E. (1965). „New Sedative and Hypotensive 3-Substituted 2,4(1H,3H)-Quinazolinediones”. Journal of Medicinal Chemistry. 8 (6): 807—811. PMID 5885076. doi:10.1021/jm00330a017.
- ^ Havera, Herbert J. (1979). „Derivatives of 1,3-disubstituted 2,4(1H,3H)-quinazolinediones as possible peripheral vasodilators or antihypertensive agents”. Journal of Medicinal Chemistry. 22 (12): 1548—1550. doi:10.1021/jm00198a024.
- ^ Garcia, J. D.; Somanathan, R.; Rivero, I. A.; Aguirre, G.; Hellberg, L. H. (2000). „Synthesis of Deuterium-Labeled Antihypertensive 3-(4-Phenyl-1′-Piperazinyl)-Propyl-2,4-Quinazolinedione”. Synthetic Communications. 30 (15): 2707—2711. doi:10.1080/00397910008086895.
- ^ Li, Xin; Lee, Yong-Rok; Kim, Sung-Hong (2011). „Concise Synthesis of Pelanserine, Goshuyuamide II, and Wuchuyuamide II with Quinazolinedione Nuclei”. Bulletin of the Korean Chemical Society. 32 (9): 3480—3482. doi:10.5012/bkcs.2011.32.9.3480.
- ^ Cortez, R.; Rivero, I. A.; Somanathan, R.; Aguirre, G.; Ramirez, F.; Hong, E. (1991). „Synthesis of Quinazolinedione Using Triphosgene”. Synthetic Communications. 21 (2): 285—292. doi:10.1080/00397919108020823.
- ^ AT 269143B, "Verfahren zur Herstellung von neuen Chinazolindionderivaten und ihrer Säureadditionssalze bzw. ihrer entsprechenden Piperaziniumverbindungen [Process for the preparation of new quinazolinedione derivatives and their acid addition salts or their corresponding piperazinium compounds]", published 1969-03-10, assigned to Miles Laboratories, Inc.
- ^ Hayao Shin, U.S. Patent 3.274.194 (1966 to Bayer Corp).
- ^ Horacio Vidrio, U.S. Patent 3.919.425 (1975 to Bayer Corp).
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α1 |
- Agonisti: 5-FNE
- 6-FNE
- Amidefrin
- Anisodamin
- Anisodin
- Cirazolin
- Dipivefrin
- Dopamin
- Efedrin
- Epinefrin (Adrenalin)
- Etilefrin
- Etilnorepinefrin
- Indanidin
- Levonordefrin
- Metaraminol
- Metoksamin
- Metildopa
- Midodrin
- Nafazolin
- Norepinefrin (Noradrenalin)
- Oktopamin
- Oksimetazolin
- Fenilefrin
- Fenilpropanolamin
- Pseudoefedrin
- Sinefrin
- Tetrahidrozolin
Antagonisti: Abanohil
- Adimolol
- Ajmalicin
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoksatian
- Buflomedil
- Bunazosin
- Karvedilol
- CI-926
- Korinantin
- Dapiprazol
- DL-017
- Domesticin
- Doksazosin
- Eugenodilol
- Fenspirid
- GYKI-12,743
- GYKI-16,084
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- Mefendioksan
- Metazosin
- Monatepil
- Moksisilit (Timoksamin)
- Naftopidil
- Nantenin
- Neldazosin
- Nicergolin
- Niguldipin
- Pelanserin
- Fendioksan
- Fenoksibenzamin
- Fentolamin
- Piperoksan
- Prazosin
- Hinazosin
- Ritanserin
- RS-97,078
- SGB-1,534
- Silodosin
- SL-89.0591
- Spiperon
- Talipeksol
- Tamsulosin
- Terazosin
- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazolin
- Trimazosin
- Upidosin
- Urapidil
- Zolertin
* Mnogi TCA, TeCA, antipsihotici, ergolini, i neki piperazini kao što su buspiron, trazodon, nefazodon, etoperidon, i mepiprazol takođe antagoniziraju α1-adrenergičke receptore, što doprinosi njihovim nuspojavama.
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5-HT1A | 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 • 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-14,671 • S-15,535 • Sarizotan • SSR-181,507 • Sunepitron • U-92,016-A • Urapidil • Vilazodon • Ksaliproden • JohimbinAntagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol • Oksprenolol • Pindobind • Pindolol • Propranolol • Tertatolol; Drugi: BMY-7,378 • CSP-2503 • Dotarizin • Flopropion • GR-46611 • Isamoltan • Lekozotan • Metitepin/Metiotepin • MPPF • NAN-190 • PRX-00023 • Robalzotan • S-15535 • SB-649,915 • Spiperon • Spiramid • Spiroksatrin • UH-301 • WAY-100,135 • WAY-100,635 • Ksilamidin |
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5-HT2B | |
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5-HT2C | 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-348Antagonisti: 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 |
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