Buclizine: Wikis

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Categories: Organochlorides > Piperazines

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Updated live from Wikipedia, last check: May 30, 2012 15:18 UTC (36 seconds ago)

From Wikipedia, the free encyclopedia

Buclizine
Systematic (IUPAC) name

(RS)-1-[(4-chlorophenyl)- phenyl-methyl]-4- [(4-tert-butylphenyl) methyl] piperazine
Identifiers
CAS number	82-95-1
ATC code	R06AE01
PubChem	6729
DrugBank	APRD00723
Chemical data
Formula	C₂₈H₃₃Cl N₂
Mol. mass	433.028 g/mol
Therapeutic considerations
Pregnancy cat.	?
Legal status
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Buclizine is an antihistamine and anticholinergic of the piperazine derivative family. It is considered to be an antiemetic, similar to meclizine.

In the United Kingdom, buclizine is one of three drugs contained in Migraleve tablets, marketed by McNeil Healthcare at migraine sufferers.

References

Cholinergics

Receptor
Ligands

mAChR	Agonists: 77-LH-28-1 • AC-42 • AC-260,584 • Aceclidine • Acetylcholine • AF30 • AF150(S) • AF267B • AFDX-384 • Alvameline • AQRA-741 • Arecoline • Bethanechol • Butyrylcholine • Carbachol • CDD-0034 • CDD-0078 • CDD-0097 • CDD-0098 • CDD-0102 • Cevimeline • cis-Dioxolane • Ethoxysebacylcholine • LY-593,039 • L-689,660 • LY-2,033,298 • McNA343 • Methacholine • Milameline • Muscarine • NGX-267 • Ocvimeline • Oxotremorine • PD-151,832 • Pilocarpine • RS86 • Sabcomeline • SDZ 210-086 • Sebacylcholine • Suberylcholine • Talsaclidine • Thiopilocarpine • Vedaclidine • VU-0029767 • VU-0090157 • VU-0152099 • VU-0152100 • VU-0238429 • WAY-132,983 • Xanomeline • YM-796 Antagonists: 3-Quinuclidinyl Benzilate • 4-DAMP • Anisodamine • Anisodine • Atropine • Atropine Methonitrate • Benactyzine • Benzatropine (Benztropine) • Benzydamine • BIBN 99 • Biperiden • Bornaprine • CAR-226,086 • CAR-301,060 • CAR-302,196 • CAR-302,282 • CAR-302,368 • CAR-302,537 • CAR-302,668 • CS-27349 • Cyclobenzaprine • Cyclopentolate • Darifenacin • DAU-5884 • Dimethindene • Dexetimide • DIBD • Dicyclomine (Dicycloverine) • Ditran • EA-3167 • EA-3443 • EA-3580 • EA-3834 • Elemicin • Etanautine • Etybenzatropine (Ethylbenztropine) • Flavoxate • Himbacine • HL-031,120 • Ipratropium • J-104,129 • Hyoscyamine • Mamba Toxin 3 • Mamba Toxin 7 • Mazaticol • Mebeverine • Methoctramine • Metixene • Myristicin • N-Ethyl-3-Piperidyl Benzilate • N-Methyl-3-Piperidyl Benzilate • Orphenadrine • Otenzepad • Oxybutynin • PBID • PD-102,807 • Phenglutarimide • Phenyltoloxamine • Pirenzepine • Piroheptine • Procyclidine • Profenamine • RU-47,213 • SCH-57,790 • SCH-72,788 • SCH-217,443 • Scopolamine (Hyoscine) • Solifenacin • Telenzepine • Tiotropium • Tolterodine • Trihexyphenidyl • Tripitamine • Tropatepine • Tropicamide • WIN-2299 • Zamifenacin; Others: 1st Generation Antihistamines (Brompheniramine • Chlorpheniramine, Cyclizine, Cyproheptadine, Dimenhydrinate, Diphenhydramine, Doxylamine, Hydroxyzine, Meclizine, Mepyramine/Pyrilamine, Phenindamine, Pheniramine, Tripelennamine, Triprolidine, etc) • Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic Antidepressants (Amoxapine, Maprotiline, etc) • Typical Antipsychotics (Chlorpromazine, Thioridazine, etc) • Atypical Antipsychotics (Clozapine, Olanzapine, Quetiapine, etc)

nAChR	Agonists: 5-HIAA • A-84,543 • A-366,833 • A-582,941 • A-867,744 • ABT-202 • ABT-418 • ABT-560 • ABT-894 • Acetylcholine • Altinicline • Anabasine • AR-R17779 • Butyrylcholine • Carbachol • Cotinine • Cytisine • Decamethonium • Desformylflustrabromine • Dianicline • Dimethylphenylpiperazinium • Epibatidine • Epiboxidine • Ethoxysebacylcholine • EVP-4473 • EVP-6124 • Galantamine • GTS-21 • Ispronicline • Lobeline • MEM-63,908 (RG-3487) • Nicotine • NS-1738 • PHA-543,613 • PHA-709,829 • PNU-120,596 • PNU-282,987 • Pozanicline • Rivanicline • Sazetidine A • Sebacylcholine • SIB-1508Y • SIB-1553A • SSR-180,711 • Suberylcholine • TC-1698 • TC-1734 • TC-1827 • TC-2216 • TC-5214 • TC-5619 • TC-6683 • Tebanicline • Tropisetron • UB-165 • Varenicline • WAY-317,538 • XY-4083 Antagonists: 18-Methoxycoronaridine • α-Bungarotoxin • α-Conotoxin • Alcuronium • Anatruxonium • Atracurium • Bupropion (Amfebutamone) • Chandonium • Chlorisondamine • Cisatracurium • Coclaurine • Coronaridine • Dacuronium • Decamethonium • Dextromethorphan • Dextropropoxyphene • Dextrorphan • Diadonium • DHβE • Dimethyltubocurarine (Metocurine) • Dipyrandium • Dizocilpine (MK-801) • Doxacurium • Duador • Esketamine • Fazadinium • Gallamine • Hexafluronium • Hexamethonium (Benzohexonium) • Ibogaine • Ketamine • Kynurenic Acid • Levacetylmethadol • Malouetine • Mecamylamine • Memantine • Methadone • Methorphan (Racemethorphan) • Methyllycaconitine • Metocurine • Mivacurium • Morphanol (Racemorphanol) • Neramexane • Pancuronium • Pempidine • Pentamine • Pentolinium • Phencyclidine • Pipecuronium • Radafaxine • Rapacuronium • Rocuronium • Surugatoxin • Suxamethonium (Succinylcholine) • Toxiferine • Trimethaphan • Tropeinium • Tubocurarine • Vecuronium

Reuptake
Inhibitors

Plasmalemmal

CHT Inhibitors

Hemicholinium-3 (Hemicholine)

VAChT Inhibitors

ChAT Inhibitors

1-(-Benzoylethyl)pyridinium • 2-(α-Naphthoyl)ethyltrimethylammonium • 3-Chloro-4-stillbazole • 4-(1-Naphthylvinyl)pyridine • Acetylseco Hemicholinium-3 • Acryloylcholine • AF64A • B115 • BETA • CM-54,903 • N,N-Dimethylaminoethylacrylate • N,N-Dimethylaminoethylchloroacetate

Catabolism

AChE Inhibitors	Reversible: Carbamates: Aldicarb • Bendiocarb • Bufencarb • Carbaryl • Carbendazim • Carbetamide • Carbofuran • Chlorbufam • Chloropropham • Ethienocarb • Ethiofencarb • Fenobucarb • Fenoxycarb • Formetanate • Furadan • Ladostigil • Methiocarb • Methomyl • Miotine • Oxamyl • Phenmedipham • Pinmicarb • Pirimicarb • Propamocarb • Propham • Propoxur; Stigmines: Ganstigmine • Neostigmine • Phenserine • Physostigmine • Pyridostigmine • Rivastigmine; Others: Ambenonium • Donepezil • Edrophonium • Galantamine • Huperzine A (Huperzia Serrata) • Minaprine • Tacrine • Zanapezil Irreversible: Organophosphates: Acephate • Azinphos-Methyl • Bensulide • Cadusafos • Chlorethoxyfos • Chlorfenvinphos • Chlorpyrifos • Chlorpyrifos-Methyl • Coumaphos • Cyclosarin (GF) • Demeton • Demeton-S-Methyl • Diazinon • Dichlorvos • Dicrotophos • Diisopropyl Fluorophosphate (Guthion) • Diisopropylphosphate • Dimethoate • Dioxathion • Disulfoton • EA-3148 • Echothiophate • Ethion • Ethoprop • Fenamiphos • Fenitrothion • Fenthion • Fosthiazate • GV • Isofluorophate • Isoxathion • Malaoxon • Malathion • Methamidophos • Methidathion • Metrifonate • Mevinphos • Monocrotophos • Naled • Novichok Agent • Omethoate • Oxydemeton-Methyl • Paraoxon • Parathion • Parathion-Methyl • Phorate • Phosalone • Phosmet • Phostebupirim • Phoxim • Pirimiphos-Methyl • Sarin (GB) • Soman (GD) • Tabun (GA) • Temefos • Terbufos • Tetrachlorvinphos • Tribufos • Trichlorfon • VE • VG • VM • VR • VX; Others: Demecarium • Onchidal (Onchidella Binneyi)

BChE Inhibitors	Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.

Others

Precursors	Choline (Lecithin) • Citicoline • Dimethylethanolamine (DMAE; Deanol) • Glycerophosphocholine • Phosphatidylcholine • Phosphatidylethanolamine • Phosphorylcholine • Pirisudanol

Cofactors	Acetic Acid • Acetyl-L-Carnitine • Acetyl-Coenzyme A • Vitamin B5 (Pantothenic Acid, Pantethine, Pantetheine, Panthenol)

Others	Acetylcholine Releasing Agents: α-Latrotoxin • β-Bungarotoxin; Acetylcholine Release Inhibitors: Botulinum Toxin (Botox); Acetylcholinesterase Reactivators: Pralidoxime • obidoxime

Histaminergics

Receptor
Ligands

H₁	Agonists: 2-Pyridylethylamine • Betahistine • Histamine • HTMT • UR-AK49 Antagonists: 1st Generation: 4-Methyldiphenhydramine • Alimemazine • Antazoline • Azatadine • Bamipine • Benzatropine (Benztropine) • Bepotastine • Bromazine • Brompheniramine • Buclizine • Captodiame • Carbinoxamine • Chlorcyclizine • Chloropyramine • Chlorothen • Chlorpheniramine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimenhydrinate • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etybenzatropine (Ethylbenztropine) • Etymemazine • Histapyrrodine • Hydroxyethylpromethazine • Hydroxyzine • Isopromethazine • Isothipendyl • Meclizine • Mepyramine (Pyrilamine) • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • Phenindamine • Pheniramine • Phenyltoloxamine • Pimethixene • Promethazine • Propiomazine • Pyrrobutamine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; 2nd Generation: Acrivastine • Astemizole • Azelastine • Cetirizine • Clemizole • Clobenztropine • Dimebolin • Ebastine • Emedastine • Epinastine • Ketotifen • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Rupatadine • Setastine • Terfenadine; 3rd Generation: Desloratadine • Fexofenadine • Levocetirizine; Miscellaneous: Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic Antidepressants (Mianserin, Mirtazapine, etc) • Serotonin Antagonists and Reuptake Inhibitors (Trazodone, Nefazodone) • Typical Antipsychotics (Chlorpromazine, Thioridazine, etc) • Atypical Antipsychotics (Clozapine, Olanzapine, Quetiapine, etc)

H₂	Agonists: Amthamine • Betazole • Dimaprit • Histamine • HTMT • Impromidine • UR-AK49 Antagonists: Cimetidine • Famotidine • Lafutidine • Metiamide • Niperotidine • Nizatidine • Ranitidine • Roxatidine

H₃	Agonists: α-Methylhistamine • Cipralisant • Histamine • Imetit • Immepip • Immethridine • Methimepip • Proxyfan Antagonists: A-349,821 • A-423,579 • ABT-239 • Betahistine • Burimamide • Ciproxifan • Clobenpropit • Conessine • GSK-189,254 • Impentamine • Iodophenpropit • JNJ-5,207,852 • MK-0249 • NNC-38-1,049 • SCH-79,687 • Thioperamide • Tiprolisant • VUF-5,681

H₄	Agonists: 4-Methylhistamine • Histamine • VUF-8,430 Antagonists: JNJ-7,777,120 • Thioperamide • VUF-6,002

Reuptake
Inhibitors

Plasmalemmal

.....

Vesicular

VMAT Inhibitors

Ibogaine • Reserpine • Tetrabenazine

Enzyme
Inhibitors

Anabolism

HDC Inhibitors

α-FMH • Brocresine • Catechin • Cyanidanol-3 • McN-A-1293 • ME • Meciadanol • Naringenin • Thiazol-4-yimethoxyamine • Tritoqualine • Zy-15,029

Catabolism

HNMT Inhibitors	Amodiaquine • BW-301U • Diphenhydramine • Harmaline • Metoprine • Quinacrine • SKF-91,488 • Tacrine

DAO Inhibitors	1,4-Diamino-2-butyne • Aminoguanidine

Others

Precursors	L-Histidine

Cofactors	Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal Phosphate)

Piperazines

1-Cyclohexylpiperazine • 2C-B-BZP • Acaprazine • Almitrine • Alnespirone • Aminoethylpiperazine • Amoxapine • Antrafenine • Aripiprazole • Atevirdine • Azaperone • Azimilide • Befuraline • Bifeprunox • Binospirone • BRL-15572 • Buclizine • Buspirone • BZP • Chlorbenzoxamine • Chlorcyclizine • Cinepazet • Cinnarizine • Ciprofloxacin • Clocinizine • Clopenthixol • Clozapine • CPPene • Cyclizine • Dapiprazole • Dasatinib • DBL-583 • DBZP • Dibenzylpiperazine • Diethylcarbamazine • Dimethylphenylpiperazinium • Dotarizine • DPI-3290 • Dropropizine • EGIS-12233 • Eltoprazine • Enilospirone • Ensaculin • Etoperidone • Fipexide • Flesinoxan • Flibanserin • Flupentixol • Fluphenazine • Fluprazine • GBR-12935 • Gepirone • HEPPS • Hexocyclium • Hydroxyzine • Imatinib • Indinavir • Ipsapirone • Itraconazole • JNJ-7777120 • Ketoconazole • Levodropropizine • Lidoflazine • Loxapine • Lurasidone • Manidipine • MBZP • mCPP • MDBZP • Meclizine • MeOPP • Nefazodone • Niaprazine • Olanzapine • Opipramol • Oxatomide • Oxypertine • PB28 • Perazine • Perospirone • Perphenazine • pFPP • Piberaline • Piperazine • PIPES • Pirenzepine • Piribedil • Posaconazole • Prochlorperazine • PRX-00023 • Quipazine • Ranolazine • Revospirone • S-15535 • SA 4503 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885 • Sildenafil • Tandospirone • TFMPP • Thiethylperazine • Thiothixene • Tirilazad • Trazodone • Trelibet • Trifluoperazine • Trimazosin • Trimetazidine • Umespirone • Vanoxerine • Vardenafil • Vesnarinone • Vilazodone • VUF-6002 • WAY-100,135 • WAY-100,635 • Zalospirone • Zipeprol • Ziprasidone • Zuclopenthixol

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