- 関
- thiethylperazine、thiethylperazine maleate
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/04/15 02:23:03」(JST)
[Wiki en表示]
Thiethylperazine
|
Systematic (IUPAC) name |
2-(ethylthio)-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine |
Clinical data |
AHFS/Drugs.com |
Micromedex Detailed Consumer Information |
Legal status |
? |
Pharmacokinetic data |
Protein binding |
60% |
Identifiers |
CAS number |
1420-55-9 Y |
ATC code |
R06AD03 |
PubChem |
CID 5440 |
DrugBank |
DB00372 |
ChemSpider |
5245 Y |
UNII |
8ETK1WAF6R Y |
KEGG |
D02354 Y |
ChEBI |
CHEBI:9544 Y |
ChEMBL |
CHEMBL1378 Y |
Chemical data |
Formula |
C22H29N3S2 |
Mol. mass |
399.618 g/mol |
SMILES
- S(c2cc1N(c3c(Sc1cc2)cccc3)CCCN4CCN(C)CC4)CC
|
InChI
-
InChI=1S/C22H29N3S2/c1-3-26-18-9-10-22-20(17-18)25(19-7-4-5-8-21(19)27-22)12-6-11-24-15-13-23(2)14-16-24/h4-5,7-10,17H,3,6,11-16H2,1-2H3 Y
Key:XCTYLCDETUVOIP-UHFFFAOYSA-N Y
|
Y (what is this?) (verify) |
Thiethylperazine (Torecan) is an antiemetic of the phenothiazine class. Though it was never licensed or used as an antipsychotic, it may have such effects.
Thiethylperazine activates the transport protein ABCC1 that clears beta-amyloid from brains of mice. [1]
References
- ^ Science Daily (September 1, 2011). "Alzheimer Disease: Transport Protein ABCC1 Plays Key Role in Clearing Beta-Amyloid from Brains of Mice.". Retrieved September 1, 2011.
- Bourquin, J. P.; Schwarb, G.; Gamboni, G.; Rischer, R.; Ruesch, L.; Uldimann, S. G.; Theuss, U.; Schenke, E.; Renz, J.; Helv. Chim. Acta 1958, 41, 1072.
Antiemetics (A04)
|
|
5-HT3 Serotonin ion
channel antagonists |
- Alosetron
- Azasetron
- Bemesetron
- Cilansetron
- Clozapine
- Dazopride
- Dolasetron
- Granisetron
- Lerisetron
- Metoclopramide
- Mianserin
- Mirtazapine
- Olanzapine
- Ondansetron
- Palonosetron
- Quetiapine
- Ramosetron
- Ricasetron
- Tropisetron
- Zatosetron
|
|
5-HT Serotonin G-protein
receptor antagonists |
- Clozapine
- Cyproheptadine
- Hydroxyzine
- Olanzapine
- Risperidone
- Ziprasidone
|
|
CB1 Agonists
(Cannabinoids) |
- Dronabinol
- Nabilone
- Nonabine
- Tetrahydrocannabinol
|
|
D2/D3 Antagonists |
- Alizapride
- Bromopride
- Chlorpromazine
- Clebopride
- Domperidone
- Haloperidol
- Hydroxyzine
- Itopride
- Metoclopramide
- Metopimazine
- Prochlorperazine
- Thiethylperazine
|
|
H1 antagonists
(Antihistamines) |
- Cyclizine
- Dimenhydrinate
- Diphenhydramine
- Hydroxyzine
- Meclozine
- Promethazine
|
|
mACh antagonists
(Anticholinergics) |
- Atropine
- Diphenhydramine
- Hydroxyzine (very mild)
- Hyoscyamine
- Scopolamine
|
|
NK1 Antagonists |
- Aprepitant
- Casopitant
- Ezlopitant
- Fosaprepitant
- Maropitant
- Vestipitant
|
|
Others |
- Cerium oxalate
- Dexamethasone
- Lorazepam
- Midazolam
- Propofol
- Trimethobenzamide
|
|
|
anat (t, g, p)/phys/devp/enzy
|
noco/cong/tumr, sysi/epon
|
proc, drug (A2A/2B/3/4/5/6/7/14/16), blte
|
|
|
|
Antipsychotics (neuroleptics) (N05A)
|
|
Typical |
- Benzamides
- Levosulpiride
- Nemonapride
- Sulpiride
- Sultopride
- Tiapride
- Veralipride
- Butyrophenones
- Azaperone
- Benperidol
- Bromperidol
- Droperidol
- Fluanisone
- Haloperidol #
- Lenperone
- Moperone
- Pipamperone
- Spiperone
- Timiperone
- Trifluperidol
- Diphenylbutylpiperidines
- Clopimozide
- Fluspirilene
- Penfluridol
- Pimozide
- Phenothiazines
- Acepromazine
- Acetophenazine
- Butaperazine
- Carphenazine
- Chloracizine
- Chlorproethazine
- Chlorpromazine
- Cyamemazine
- Dixyrazine
- Fluacizine
- Fluphenazine
- Levomepromazine/Methotrimeprazine
- Mesoridazine
- Perazine
- Pericyazine
- Perphenazine
- Piperacetazine
- Pipotiazine
- Prochlorperazine
- Promazine
- Promethazine
- Propiomazine
- Sulforidazine
- Thiethylperazine
- Thiopropazate
- Thioproperazine
- Thioridazine
- Trifluoperazine
- Triflupromazine
- Thioxanthenes
- Chlorprothixene
- Clopenthixol
- Flupentixol
- Thiothixene
- Zuclopenthixol
- Tricyclics
- Butaclamol
- Fluotracen
- Loxapine
- Trimipramine
- Others
- Prothipendyl
|
|
Atypical |
- Benzamides
- Amisulpride
- Remoxipride‡
- Butyrophenones
- Cinuperone
- Melperone
- Setoperone
- Benzo(iso)oxazolepiperidines
- Iloperidone
- Ocaperidone
- Paliperidone
- Risperidone #
- Benzo(iso)thiazolepiperazines
- Lurasidone
- Perospirone
- Revospirone
- Tiospirone
- Ziprasidone
- Diphenylbutylpiperazines
- Amperozide
- Phenylpiperazines
- Aripiprazole
- Bifeprunox
- Brexpiprazole†
- Elopiprazole
- Umespirone
- Tricyclics
- Amoxapine
- Asenapine
- Carpipramine
- Clocapramine
- Clorotepine
- Clotiapine
- Clozapine #
- Fluperlapine
- Gevotroline
- Metitepine
- Mosapramine
- NDMC
- Olanzapine
- Piquindone
- Quetiapine
- Tenilapine
- Zotepine
- Others
- Blonanserin
- Cariprazine
- Molindone
- Pimavanserin
- Roxindole
- Sarizotan
- Sertindole
- Spiramide
- Zicronapine†
|
|
Others |
- Alstonine
- Azacyclonol
- Cannabidiol
- Mazapertine§
- Mifepristone
- Oxypertine
- Reserpine
- Rimcazole
- Secretin
- Talnetant§
- Tetrabenazine
- Vabicaserin
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
dsrd (o, p, m, p, a, d, s), sysi/epon, spvo
|
proc (eval/thrp), drug (N5A/5B/5C/6A/6B/6D)
|
|
|
|
Antihistamines (R06)
|
|
Aminoalkyl ethers |
- Bromazine (bromodiphenhydramine)
- Carbinoxamine
- Clemastine
- Chlorphenoxamine
- Diphenylpyraline
- Diphenhydramine
- Doxylamine
- Orphenadrine
- Phenyltoloxamine
|
|
Substituted alkylamines |
- Brompheniramine
- Chlorphenamine
- Dexbrompheniramine (+pseudoephedrine)
- Dexchlorpheniramine (+betamethasone)
- Dimetindene
- Pheniramine
- Talastine
|
|
Substituted ethylenediamines |
- Chloropyramine
- Histapyrrodine
- Mepyramine
- Methapyrilene
- Tripelennamine (pyribenzamine)
|
|
Phenothiazine derivatives |
- Alimemazine
- Hydroxyethylpromethazine
- Isothipendyl
- Mequitazine
- Methdilazine
- Oxomemazine
- Promethazine
|
|
Piperazine derivatives |
- Buclizine
- Cetirizine
- Chlorcyclizine
- Cinnarizine
- Cyclizine
- Hydroxyzine
- Levocetirizine
- Meclizine
- Niaprazine
- Oxatomide
|
|
Others for systemic use |
- Antazoline
- Azatadine
- Bamipine
- Cyproheptadine
- Deptropine
- Ebastine
- Emedastine
- Epinastine
- Ketotifen
- Latrepirdine
- Mebhydrolin
- Mizolastine
- Olopatadine
- Phenindamine
- Pimethixene
- Pyrrobutamine
- Quifenadine
- Rupatadine
- Triprolidine
- selective (Acrivastine
- Astemizole
- Azelastine
- Bilastine
- Desloratadine
- Fexofenadine
- Loratadine
- Terfenadine)
|
|
For topical use |
- Bamipine
- Chloropyramine
- Chlorphenoxamine
- Clemastine
- Dimetindene
- Diphenhydramine
- Isothipendyl
- Mepyramine
- Promethazine
- Thenalidine
|
|
Dopaminergics
|
|
Receptor ligands
|
|
Agonists
|
- Adamantanes: Amantadine
- Memantine
- Rimantadine; Aminotetralins: 7-OH-DPAT
- 8-OH-PBZI
- Rotigotine
- UH-232; Benzazepines: 6-Br-APB
- Fenoldopam
- SKF-38,393
- SKF-77,434
- SKF-81,297
- SKF-82,958
- SKF-83,959; Ergolines: Bromocriptine
- Cabergoline
- Dihydroergocryptine
- Epicriptine
- Lisuride
- LSD
- Pergolide; Dihydrexidine derivatives: 2-OH-NPA
- A-86,929
- Ciladopa
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine; Others: A-68,930
- A-77636
- A-412,997
- ABT-670
- ABT-724
- Aplindore
- Apomorphine
- Aripiprazole
- Bifeprunox
- BP-897
- CY-208,243
- Dizocilpine
- Etilevodopa
- Flibanserin
- Ketamine
- Melevodopa
- Modafinil
- Pardoprunox
- Phencyclidine
- PD-128,907
- PD-168,077
- PF-219,061
- Piribedil
- Pramipexole
- Propylnorapomorphine
- Pukateine
- Quinagolide
- Quinelorane
- Quinpirole
- RDS-127
- Ro10-5824
- Ropinirole
- Rotigotine
- Roxindole
- Salvinorin A
- SKF-89,145
- Sumanirole
- Terguride
- Umespirone
- WAY-100,635
|
|
Antagonists
|
- Typical antipsychotics: Acepromazine
- Azaperone
- Benperidol
- Bromperidol
- Clopenthixol
- Chlorpromazine
- Chlorprothixene
- Droperidol
- Flupentixol
- Fluphenazine
- Fluspirilene
- Haloperidol
- Levosulpiride
- Loxapine
- Mesoridazine
- Methotrimeprazine
- Nemonapride
- Penfluridol
- Perazine
- Periciazine
- Perphenazine
- Pimozide
- Prochlorperazine
- Promazine
- Sulforidazine
- Sulpiride
- Sultopride
- Thioridazine
- Thiothixene
- Trifluoperazine
- Triflupromazine
- Trifluperidol
- Zuclopenthixol; Atypical antipsychotics: Amisulpride
- Asenapine
- Blonanserin
- Cariprazine
- Carpipramine
- Clocapramine
- Clorotepine
- Clozapine
- Gevotroline
- Iloperidone
- Lurasidone
- Melperone
- Molindone
- Mosapramine
- Olanzapine
- Paliperidone
- Perospirone
- Piquindone
- Quetiapine
- Remoxipride
- Risperidone
- Sertindole
- Tiospirone
- Zicronapine
- Ziprasidone
- Zotepine; Antiemetics: AS-8112
- Alizapride
- Bromopride
- Clebopride
- Domperidone
- Metoclopramide
- Thiethylperazine; Others: Amoxapine
- Buspirone
- Butaclamol
- Ecopipam
- EEDQ
- Eticlopride
- Fananserin
- Hydroxyzine
- L-745,870
- Nafadotride
- Nuciferine
- PNU-99,194
- Raclopride
- Sarizotan
- SB-277,011-A
- SCH-23,390
- SKF-83,959
- Sonepiprazole
- Spiperone
- Spiroxatrine
- Stepholidine
- Tetrahydropalmatine
- Tiapride
- UH-232
- Yohimbine
|
|
|
|
Reuptake inhibitors
|
|
Plasmalemmal
|
DAT inhibitors
|
- Piperazines: DBL-583
- GBR-12,935
- Nefazodone
- Vanoxerine; Piperidines: BTCP
- Desoxypipradrol
- Dextromethylphenidate
- Difemetorex
- Ethylphenidate
- Methylnaphthidate
- Methylphenidate
- Phencyclidine
- Pipradrol; Pyrrolidines: Diphenylprolinol
- MDPV
- Naphyrone
- Prolintane
- Pyrovalerone; Tropanes: Altropane
- Brasofensine
- CFT
- Cocaine
- Dichloropane
- Difluoropine
- FE-β-CPPIT
- FP-β-CPPIT
- Ioflupane (123I)
- Iometopane
- RTI-112
- RTI-113
- RTI-121
- RTI-126
- RTI-150
- RTI-177
- RTI-229
- RTI-336
- Tenocyclidine
- Tesofensine
- Troparil
- Tropoxane
- WF-11
- WF-23
- WF-31
- WF-33; Others: Adrafinil
- Armodafinil
- Amfonelic acid
- Amphetamine
- Amineptine
- Benzatropine
- Bromantane
- BTQ
- BTS-74,398
- Bupropion
- Ciclazindol
- Diclofensine
- Dimethocaine
- Diphenylpyraline
- Dizocilpine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- Etybenzatropine
- EXP-561
- Fencamine
- Fencamfamine
- Fezolamine
- Fluorenol
- GYKI-52,895
- Indatraline
- Ketamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Mazindol
- Medifoxamine
- Mesocarb
- Modafinil
- Nefopam
- Nomifensine
- NS-2359
- O-2172
- Pridefrine
- Propylamphetamine
- Radafaxine
- SEP-225,289
- SEP-227,162
- Sertraline
- Sibutramine
- Tametraline
- Tedatioxetine
- Tripelennamine
|
|
|
Vesicular
|
VMAT inhibitors
|
- Deserpidine
- Ibogaine
- Reserpine
- Tetrabenazine
|
|
|
|
|
|
|
Allosteric modulators
|
|
- Quinazolinamines: SoRI-9804
- SoRI-20040
- SoRI-20041
|
|
|
Enzyme inhibitors
|
|
Anabolism
|
PAH inhibitors
|
|
|
TH inhibitors
|
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
|
|
AAAD/DDC inhibitors
|
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
|
|
|
Catabolism
|
MAO inhibitors
|
- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Brofaromine
- Cimoxatone
- Clorgiline
- Eprobemide
- Esuprone
- Harmala alkaloids
- Methylene Blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective: D-Deprenyl
- Ethanol
- L-Deprenyl (Selegiline)
- Ladostigil
- Lazabemide
- Milacemide
- Nicotine
- Pargyline
- Rasagiline
- Safinamide
|
|
COMT inhibitors
|
- Entacapone
- Nitecapone
- Tolcapone
|
|
DBH inhibitors
|
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Tropolone
|
|
|
|
|
Others
|
|
Precursors
|
- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa)
|
|
Cofactors
|
- Ferrous iron (Fe2+)
- Tetrahydrobiopterin
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
|
|
Others
|
- Activity enhancers: BPAP * PPAP; Toxins: 6-OHDA; Steroids: Anabolic-androgenic steroids
|
|
|
|
List of dopaminergic drugs
|
|
Piperazines
|
|
Simple piperazines
(no additional rings) |
- 1-Cyclohexylpiperazine
- Aminoethylpiperazine
- Diethylcarbamazine
- HEPPS
- Midafotel
- Piperazine
- PIPES
|
|
Phenylpiperazines |
- Acaprazine
- Antrafenine
- Aripiprazole
- Batoprazine
- Bifeprunox
- BRL-15,572
- Ciprofloxacin
- CSP-2503
- Dapiprazole
- DCPP
- DMPP
- Diphenylpiperazine
- Dropropizine
- EGIS-12,233
- Elopiprazole
- Eltoprazine
- Enpiprazole
- Ensaculin
- Etoperidone
- Flesinoxan
- Flibanserin
- Fluprazine
- Itraconazole
- Ketoconazole
- Levodropropizine
- Lorpiprazole
- mCPP
- Mefway
- MeOPP
- Mepiprazole
- Naftopidil
- Naluzotan
- Naphthylpiperazine
- Nefazodone
- Niaprazine
- Oxypertine
- Pardoprunox
- pCPP
- pFPP
- Posaconazole
- S-14,506
- S-14,671
- S-15,535
- SB-258,585
- SB-271,046
- SB-357,134
- SB-399,885
- Sonepiprazole
- TFMPP
- Tolpiprazole
- Trazodone
- Urapidil
- Vesnarinone
- Vilazodone
- Vortioxetine
- WAY-100,135
- WAY-100,635
|
|
Benzylpiperazines |
- 2C-B-BZP
- Befuraline
- Bifeprunox
- Buclizine
- BZP
- Chlorbenzoxamine
- DBZP
- Fipexide
- Imatinib
- MBZP
- MDBZP
- Meclozine
- Piberaline
- Piribedil
- Trimetazidine
- Vesnarinone
|
|
Diphenylalkylpiperazines
(benzhydrylalkylpiperazines) |
- Almitrine
- Amperozide
- BRL-15,572
- Buclizine
- BW373U86
- Cetirizine
- Chlorbenzoxamine
- Chlorcyclizine
- Cinnarizine
- Clocinizine
- Cyclizine
- DBL-583
- Diphenylmethylpiperazine
- Dotarizine
- DPI-221
- DPI-287
- DPI-3290
- GBR-12,783
- GBR-12,935
- GBR-13,069
- GBR-13,098
- GBR-13,119
- Hydroxyzine
- Lidoflazine
- Manidipine
- Meclozine
- Oxatomide
- SNC-80
- Vanoxerine
|
|
Pyrimidinylpiperazines |
- Buspirone
- Dasatinib
- Eptapirone
- Gepirone
- Ipsapirone
- Piribedil
- Prazitone
- Pyrimidinylpiperazine
- Revospirone
- Tandospirone
- Tirilazad
- Trimazosin
- Umespirone
- Zalospirone
|
|
Pyridinylpiperazines |
- Atevirdine
- Azaperone
- Mirtazapine
- Pyridinylpiperazine
|
|
Benzo(iso)thiazolylpiperazines |
- Lurasidone
- Perospirone
- Revospirone
- Tiospirone
- Ziprasidone
|
|
Tricyclics
(piperazine attached via side chain) |
- Amoxapine
- Clopenthixol
- Clorotepine
- Clozapine
- Cyanothepin
- Doclothepin
- Docloxythepin
- Flupentixol
- Fluphenazine
- Isofloxythepin
- Loxapine
- Meperathiepin
- Metitepine
- Octomethothepin
- Olanzapine
- Opipramol
- Oxyclothepin
- Oxyprothepin
- Peradithiepin
- Perathiepin
- Perazine
- Perphenazine
- Pirenzepine
- Prochlorperazine
- Thiethylperazine
- Thiothixene
- Trifluoperazine
- Trifluthepin
- Zuclopenthixol
|
|
Others/Uncategorized |
- 6-Nitroquipazine
- Azimilide
- Cinepazet
- Cyclohexylpiperazine
- Hexocyclium
- Indinavir
- JNJ-7777120
- Lodenafil
- Mirodenafil
- PB-28
- Quipazine
- Ranolazine
- SA-4503
- Sildenafil
- Tadalafil
- Vardenafil
- VUF-6002
- Zipeprol
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- [Noncardiogenic pulmonary edema in the course of poisoning with clozapine, ketoprofen and thiethylperazine].
- Majewska M, Kołodziej M, Szponar J, Drelich G, Danielewicz P, Kostek H.Author information Samodzielny Publiczny Szpital Wojewódzki im. Jana Bozego w Lublinie, Regionalny Ośrodek Toksykologii Klinicznej.AbstractPulmonary edema is a severe, potentially fatal clinical condition. It happens, when interstitial fluid is accumulating in the alveoli, impeding proper gas exchange. Typically we distinguish cardiogenic and noncardiogenic pulmonary edema. The article describes the case of severe pulmonary edema, which occurred in a young woman, free of cardiac diseases, about 30 hours after a suicidal drug poisoning (clozapine, ketoprofen, thiethylperazine). Both clozapine and ketoprofen intoxication, may be severe. Complications in these poisonings affect not only the central nervous system, but also the circulatory or respiratory system and may even occur several hours after the overdose of these drugs. The study considered the causes and possible mechanisms of pulmonary edema in poisoning with these drugs.
- Przegla̧d lekarski.Przegl Lek.2012;69(8):618-20.
- Pulmonary edema is a severe, potentially fatal clinical condition. It happens, when interstitial fluid is accumulating in the alveoli, impeding proper gas exchange. Typically we distinguish cardiogenic and noncardiogenic pulmonary edema. The article describes the case of severe pulmonary edema, whic
- PMID 23243946
- Cerebral amyloid-β proteostasis is regulated by the membrane transport protein ABCC1 in mice.
- Krohn M, Lange C, Hofrichter J, Scheffler K, Stenzel J, Steffen J, Schumacher T, Brüning T, Plath AS, Alfen F, Schmidt A, Winter F, Rateitschak K, Wree A, Gsponer J, Walker LC, Pahnke J.Author information Department of Neurology, Neurodegeneration Research Laboratory, University of Rostock, Rostock, Germany.AbstractIn Alzheimer disease (AD), the intracerebral accumulation of amyloid-β (Aβ) peptides is a critical yet poorly understood process. Aβ clearance via the blood-brain barrier is reduced by approximately 30% in AD patients, but the underlying mechanisms remain elusive. ABC transporters have been implicated in the regulation of Aβ levels in the brain. Using a mouse model of AD in which the animals were further genetically modified to lack specific ABC transporters, here we have shown that the transporter ABCC1 has an important role in cerebral Aβ clearance and accumulation. Deficiency of ABCC1 substantially increased cerebral Aβ levels without altering the expression of most enzymes that would favor the production of Aβ from the Aβ precursor protein. In contrast, activation of ABCC1 using thiethylperazine (a drug approved by the FDA to relieve nausea and vomiting) markedly reduced Aβ load in a mouse model of AD expressing ABCC1 but not in such mice lacking ABCC1. Thus, by altering the temporal aggregation profile of Aβ, pharmacological activation of ABC transporters could impede the neurodegenerative cascade that culminates in the dementia of AD.
- The Journal of clinical investigation.J Clin Invest.2011 Oct;121(10):3924-31. doi: 10.1172/JCI57867. Epub 2011 Sep 1.
- In Alzheimer disease (AD), the intracerebral accumulation of amyloid-β (Aβ) peptides is a critical yet poorly understood process. Aβ clearance via the blood-brain barrier is reduced by approximately 30% in AD patients, but the underlying mechanisms remain elusive. ABC transporters have been impli
- PMID 21881209
- Enhancement of vancomycin activity by phenothiazines against vancomycin-resistant Enterococcus faecium in vitro.
- Rahbar M, Mehrgan H, Hadji-nejad S.Author information Department of Microbiology, Reference Health Laboratories, Ministry of Health, Tehran, Iran.AbstractThe antimicrobial and resistance-reversal activities of seven phenothiazine derivatives were evaluated against vancomycin-sensitive Enterococcus faecalis ATCC 29212, vancomycin resistant E. faecalis ATCC 51299 and ten vancomycin-resistant E. faecium strains originating from human infections. Minimum inhibitory concentrations (MIC) of the compounds were determined by agar dilution method, and synergy between phenothiazines and vancomycin was investigated using Checkerboard (microbroth dilution) technique. We found that all enterococci strains, regardless of their susceptibility to vancomycin, were inhibited by phenothiazines at concentrations varying from 8 to 256 microg/ml, with thiethylperazine being the most potent inhibitory agent. Besides, all the phenothiazines showed partial synergy with vancomycin and could lessen MIC of vancomycin from 512 to 8 microg/ml at their sub-inhibitory concentrations. The highest reduction in MIC was observed with chlorpromazine (32 times); however, thiethylperazine and promethazine stood next (24 times). Although resistance modification was observed at concentrations higher than those that phenothiazines reach in vivo, the potential offered by non-antibiotics justify further animal experiments as well as clinical trials to establish their clinical relevance.
- Basic & clinical pharmacology & toxicology.Basic Clin Pharmacol Toxicol.2010 Aug;107(2):676-9. doi: 10.1111/j.1742-7843.2010.00558.x. Epub 2010 Mar 28.
- The antimicrobial and resistance-reversal activities of seven phenothiazine derivatives were evaluated against vancomycin-sensitive Enterococcus faecalis ATCC 29212, vancomycin resistant E. faecalis ATCC 51299 and ten vancomycin-resistant E. faecium strains originating from human infections. Minimum
- PMID 20353486
Related Links
- thiethylperazine malate, the malate salt of thiethylperazine, having the same actions and uses as the base. It is administered intramuscularly.
- Thiethylperazine: A dopamine antagonist that is particularly useful in treating the nausea and vomiting associated with anesthesia, mildly emetic cancer chemotherapy agents, radiation therapy, and toxins. This piperazine ...
- (thiethylperazine malate) Injection, USP (for intramuscular use only) Prescribing Information Rx only DESCRIPTION TORECAN ® (thiethylperazine) is a phenothiazine. Thiethylperazine is characterized by a substituted thioethyl ...
Related Pictures
★リンクテーブル★
[★]
- 英
- thiethylperazine、thiethylperazine malate、thiethylperazine maleate
- 関
- リンゴ酸チエチルペラジン、マレイン酸チエチルペラジン
[★]
- 関
- thiethylperazine、thiethylperazine malate
[★]
- 英
- thiethylperazine malate
- 関
- チエチルペラジン
[★]
チエチルペラジン
- 関
- thiethylperazine malate、thiethylperazine maleate