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Piperoksan (benodain ) je lek koji je bio privi otkriveni antihistaminik .[5] [6] Ovo jedinjenje je izvedeno iz benzodioksana tokom ranih 1930-ih .[5] [6] Inicijalno je ispitivano kao blokator α-adrenergičkog receptora . Kasnije je pokazano da ono takođe deluje kao antagonist histaminom indukovanog bronhospazma kod morskih prasića .[7] [8] [9] Bovet je nagrađen Nobelovom nagradom za fiziologiju ili medicinu 1957 . za njegov doprinos.[10] Jedan od njegovih studenata je objavio prvu SAR studiju antihistamina 1939 . godine.[7]
↑ 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 . http://www.sciencedirect.com/science/article/pii/S1359644610007737 . 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 . http://www.jcheminf.com/content/2/1/3 . edit
↑ 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
↑ 5,0 5,1 Scriabine, Alexander; Landau, Ralph; Achilladelis, Basil (1999). Pharmaceutical innovation: revolutionizing human health . Philadelphia: Chemical Heritage Press. ISBN 0-941901-21-1 . http://books.google.com/books?id=IH4lPs6S1bMC&lpg=PA230&dq=piperoxan%20anthistamine&pg=PA230#v=onepage&q&f=false .
↑ 6,0 6,1 Williams, David H.; Lemke, Thomas L.; Foye, William O. (2008). Foye's principles of medicinal chemistry . Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 0-7817-6879-9 . http://books.google.com/books?id=R0W1ErpsQpkC&lpg=PA1010&dq=piperoxan%20anthistamine&pg=PA1010#v=onepage&q&f=false .
↑ 7,0 7,1 Scriabine, Alexander; Landau, Ralph; Achilladelis, Basil (1999). Pharmaceutical innovation: revolutionizing human health . Philadelphia: Chemical Heritage Press. ISBN 0-941901-21-1 . http://books.google.com/books?id=IH4lPs6S1bMC&lpg=PA230&dq=piperoxan%20anthistamine&pg=PA230#v=onepage&q&f=false .
↑ Williams, David H.; Lemke, Thomas L.; Foye, William O. (2008). Foye's principles of medicinal chemistry . Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 0-7817-6879-9 . http://books.google.com/books?id=R0W1ErpsQpkC&lpg=PA1010&dq=piperoxan%20anthistamine&pg=PA1010#v=onepage&q&f=false .
↑ Fourneau, Ernest; Bovet, Daniel (1933). „Recherches sur l'action sympathicolytique d'un nouveau dérivé du dioxane”. Archives Internationales de Pharmacodynamie et de Thérapie 46 : 178-91. ISSN 0003-9780 .
↑ „Daniel Bovet - Biography” . http://nobelprize.org/nobel_prizes/medicine/laureates/1957/bovet-bio.html .
Williams, David H.; Lemke, Thomas L.; Foye, William O. (2008). Foye's principles of medicinal chemistry . Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 0-7817-6879-9 . http://books.google.com/books?id=R0W1ErpsQpkC&lpg=PA1010&dq=piperoxan%20anthistamine&pg=PA1010#v=onepage&q&f=false .
Scriabine, Alexander; Landau, Ralph; Achilladelis, Basil (1999). Pharmaceutical innovation: revolutionizing human health . Philadelphia: Chemical Heritage Press. ISBN 0-941901-21-1 . http://books.google.com/books?id=IH4lPs6S1bMC&lpg=PA230&dq=piperoxan%20anthistamine&pg=PA230#v=onepage&q&f=false .
Williams, David H.; Lemke, Thomas L.; Foye, William O. (2008). Foye's principles of medicinal chemistry . Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 0-7817-6879-9 . http://books.google.com/books?id=R0W1ErpsQpkC&lpg=PA1010&dq=piperoxan%20anthistamine&pg=PA1010#v=onepage&q&f=false .
Scriabine, Alexander; Landau, Ralph; Achilladelis, Basil (1999). Pharmaceutical innovation: revolutionizing human health . Philadelphia: Chemical Heritage Press. ISBN 0-941901-21-1 . http://books.google.com/books?id=IH4lPs6S1bMC&lpg=PA230&dq=piperoxan%20anthistamine&pg=PA230#v=onepage&q&f=false .
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.
Receptor
Agonisti :
2-Piridiletilamin • Betahistin • Histamin • HTMT • UR-AK49 Antagonisti :
1. generacija :
4-Metildifenhidramin • Alimemazin • Antazolin • Azatadin • Bamipin • Benzatropin/Benztropin • Bepotastin • Bromazin • Bromfeniramin • Buklizin • Kaptodiam • Karbinoksamin • Hlorciklizin • Hloropiramin • Hloroten • Hlorfenamin • Hlorfenoksamin • Cinarizin • Klemastin • Klobenzepam • Klocinizin • Ciklizin • Ciproheptadin • Dacemazin • Deptropin • Deksbromfeniramin • Dekshlorfeniramin • Dimenhidrinat • Dimetinden • Difenhidramin • Difenilpiralin • Doksilamin • Embramin • Etodroksizin • Etibenzatropin/Etilbenztropin • Etimemazin • Flunarizin • Histapirodin • Homohlorciklizin • Hidroksietilprometazin • Hidroksizin • Izoprometazin • Izotipendil • Meklozin • Mepiramin/Pirilamin • Mehitazin • Metafurilen • Metapirilen • Metdilazin • Moksastin • Niaprazin • Orfenadrin • Oksatomid • Oksomemazin • Fenindamin • Feniramin • Feniltoloksamin • Pimetiksen • Piperoksan • Pipoksizin • Prometazin • Propiomazin • Pirobutamin • Talastin • Tenalidin • Tenildiamin • Tiazinamijum • Tonzilamin • Tolpropamin • Tripelenamin • Triprolidin
2. generacija : Akrivastin • Alinastin • Astemizol • Azelastin • Bamirastin • Barmastin • Bepiastin • Bepotastin • Bilastin • Kabastinen • Karebastin • Ketirizin • Klemastin • Klemizol • Klobenztropin • Dorastin • Ebastin • Emedastin • Epinastin • Flezelastin • Ketotifen • Latrepirdin • Levokabastin • Linetastin • Loratadin • Mapinastin • Mebhidrolin • Mizolastin • Moksastin • Noberastin • Oktastin • Olopatadin • Perastin • Piklopastin • Rokastin • Rupatadin • Setastin • Talastin • Temelastin • Terfenadin • Zepastin
3. generacija : Desloratadin • Feksofenadin • Cetirizin • Levocetirizin
Negrupisani : Belarizin • Efletirizin • Elbanizin • Flotrenizin • Medrilamin • Napaktadin • Pibaksizin • Tagorizin • Trelnarizin • Trenizin • Vapitadin
Razni :
Triciklični antidepresanti (
amitriptilin ,
• doksepin ,
• trimipramin , itd)
• Tetraciklični antidepresanti (
mianserin ,
• mirtazapin , itd)
• Tipični antipsihotici (
hlorpromazin ,
• tioridazin , itd)
• Atipični antipsihotici (
klozapin ,
• olanzapin ,
• hetiapin , itd)
Transporter
Enzim
Drugi