タリペキソール
- 関
- talipexole hydrochloride
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/12/26 17:23:59」(JST)
[Wiki en表示]
Talipexole
|
|
Clinical data |
Trade names |
Domin |
AHFS/Drugs.com |
International Drug Names |
Routes of
administration |
Oral |
ATC code |
none |
Legal status |
Legal status |
|
Identifiers |
IUPAC name
- 6-allyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[4,5-d]azepin-2-amine
|
Synonyms |
Alefexole |
CAS Number |
36085-73-1 N |
PubChem (CID) |
5374 |
IUPHAR/BPS |
5442 |
ChemSpider |
5181 N |
UNII |
7AM2J46Z1Y N |
ChEMBL |
CHEMBL1289023 N |
Chemical and physical data |
Formula |
C10H15N3S |
Molar mass |
209.31 g/mol |
3D model (Jmol) |
Interactive image |
SMILES
-
n1c2c(sc1N)CCN(CC2)C\C=C
C=CCN1CCC2=C(CC1)SC(=N2)N
|
InChI
-
InChI=1S/C10H15N3S/c1-2-5-13-6-3-8-9(4-7-13)14-10(11)12-8/h2H,1,3-7H2,(H2,11,12) N
-
Key:DHSSDEDRBUKTQY-UHFFFAOYSA-N N
|
NY (what is this?) (verify) |
Talipexole (B-HT920, Domnin) is a dopamine agonist that is marketed as a treatment for Parkinson's Disease in Japan by Boehringer Ingelheim; it was introduced in 1996.[1] As of December 2014 it was not approved for marketing in the US nor in Europe.[2]
Talipexole is a D2 dopamine receptor agonist and interacts both pre- and post-synaptic receptors. It also is an α2-adrenergic agonist.[3]
The main side effects are drowsiness, dizziness, hallucinations and minor gastrointestinal complaints.[3] In 2008 the Japanese Ministry of Health, Labour, and Welfare mandated that Boehringer add a warning to the label concerning the risk of sudden onset of sleep.[4]:15
References
- ^ PharmaLetter 22 July 1996 First Launch In Japan For Talipexole
- ^ EvaluatePharma Database. Page accessed 9 December 2014
- ^ a b Benkert O, et al. Dopamine agonists in schizophrenia: a review. Eur Neuropsychopharmacol. 1995;5 Suppl:43-53. PMID 8775758
- ^ Japanese Ministry of Health, Labour and Welfare March 2008 Pharmaceuticals and Medical Devices Safety Information No. 245
Antiparkinson agents (N04)
|
|
Dopaminergics |
DA precursors/prodrugs |
|
|
DA receptor agonists |
- Apomorphine
- Bromocriptine
- Cabergoline
- Dihydroergocryptine
- Lisuride
- Pergolide
- Piribedil
- Pramipexole
- Ropinirole
- Rotigotine
|
|
MAO-B inhibitors |
|
|
COMT inhibitors |
|
|
AAAD inhibitors |
|
|
|
Anticholinergics |
- Benzatropine
- Biperiden#
- Bornaprine
- Chlorphenoxamine
- Cycrimine
- Dexetimide
- Diphenhydramine
- Etanautine
- Etybenzatropine
- Mazaticol
- Metixene
- Orphenadrine
- Phenglutarimide
- Piroheptine
- Procyclidine
- Profenamine
- Trihexyphenidyl
- Tropatepine
|
|
Others |
- Amantadine
- Budipine
- Methylxanthines (e.g., caffeine)
- Rimantadine
|
|
-
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
Adrenergic receptor modulators
|
|
α1 |
- Agonists
- 6-FNE
- Amidephrine
- Anisodine
- Buspirone
- Cirazoline
- Corbadrine
- Dexisometheptene
- Dipivefrine
- Dopamine
- Droxidopa (L-DOPS)
- Ephedrine
- Epinephrine
- Etilefrine
- Etilevodopa
- Ethylnorepinephrine
- Indanidine
- Isometheptene
- L-DOPA (levodopa)
- L-Phenylalanine
- L-Tyrosine
- Melevodopa
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine (drug)
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetryzoline
- Tiamenidine
- XP21279
- Xylometazoline
|
|
- Antagonists
- Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Anisodamine
- Arotinolol
- Atiprosin
- Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- Corynanthine
- Dapiprazole
- Domesticine
- Doxazosin
- Ergolines (e.g., ergotamine, dihydroergotamine, lisuride, terguride)
- Etoperidone
- Eugenodilol
- Fenspiride
- Hydroxyzine
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- mCPP
- Mepiprazole
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Nefazodone
- Neldazosin
- Niaprazine
- Nicergoline
- Niguldipine
- Pardoprunox
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- Silodosin
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tiodazosin
- Tolazoline
- Trazodone
- Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin)
- Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine)
- Trimazosin
- Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
- Urapidil
- WB-4101
- Zolertine
|
|
|
α2 |
- Agonists
- (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Corbadrine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Droxidopa (L-DOPS)
- Etilevodopa
- Ephedrine
- Ergotamine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- L-DOPA (levodopa)
- L-Phenylalanine
- L-Tyrosine
- Lofexidine
- Medetomidine
- Melevodopa
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tiamenidine
- Tizanidine
- Tolonidine
- Urapidil
- XP21279
- Xylazine
- Xylometazoline
|
|
- Antagonists
- 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- Atypical antipsychotics (e.g., asenapine, clozapine, lurasidone, paliperidone, quetiapine, risperidone, zotepine)
- Azapirones (e.g., buspirone, tandospirone)
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- Idazoxan
- mCPP
- Mianserin
- Mirtazapine
- NAN-190
- Olanzapine
- Pardoprunox
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
- Yohimbine
|
|
|
β |
- Agonists
- Abediterol
- Alifedrine
- Amibegron
- Arbutamine
- Arformoterol
- Arotinolol
- BAAM
- Bambuterol
- Befunolol
- Bitolterol
- Broxaterol
- Buphenine
- Carbuterol
- Carmoterol
- Cimaterol
- Clenbuterol
- Corbadrine
- Denopamine
- Dipivefrine
- Dobutamine
- Dopamine
- Dopexamine
- Droxidopa (L-DOPS)
- Ephedrine
- Epinephrine
- Etafedrine
- Etilefrine
- Etilevodopa
- Ethylnorepinephrine
- Fenoterol
- Formoterol
- Hexoprenaline
- Higenamine
- Indacaterol
- Isoetarine
- Isoprenaline
- Isoxsuprine
- L-DOPA (levodopa)
- L-Phenylalanine
- L-Tyrosine
- Levosalbutamol
- Mabuterol
- Melevodopa
- Methoxyphenamine
- Methyldopa
- Mirabegron
- Norepinephrine
- Orciprenaline
- Oxyfedrine
- PF-610355
- Phenylpropanolamine
- Pirbuterol
- Prenalterol
- Ractopamine
- Procaterol
- Pseudoephedrine
- Reproterol
- Rimiterol
- Ritodrine
- Salbutamol
- Salmeterol
- Solabegron
- Terbutaline
- Tretoquinol
- Tulobuterol
- Vilanterol
- Xamoterol
- XP21279
- Zilpaterol
- Zinterol
|
|
- Antagonists
- Acebutolol
- Adaprolol
- Adimolol
- Afurolol
- Alprenolol
- Alprenoxime
- Amosulalol
- Ancarolol
- Arnolol
- Arotinolol
- Atenolol
- Befunolol
- Betaxolol
- Bevantolol
- Bisoprolol
- Bopindolol
- Bornaprolol
- Brefonalol
- Bucindolol
- Bucumolol
- Bufetolol
- Bufuralol
- Bunitrolol
- Bunolol
- Bupranolol
- Butaxamine
- Butidrine
- Butofilolol
- Capsinolol
- Carazolol
- Carpindolol
- Carteolol
- Carvedilol
- Celiprolol
- Cetamolol
- Cicloprolol
- Cinamolol
- Cloranolol
- Cyanopindolol
- Dalbraminol
- Dexpropranolol
- Diacetolol
- Dichloroisoprenaline
- Dihydroalprenolol
- Dilevalol
- Diprafenone
- Draquinolol
- Ecastolol
- Epanolol
- Ericolol
- Ersentilide
- Esatenolol
- Esprolol
- Eugenodilol
- Exaprolol
- Falintolol
- Flestolol
- Flusoxolol
- Hydroxycarteolol
- Hydroxytertatolol
- ICI-118,551
- Idropranolol
- Indenolol
- Indopanolol
- Iodocyanopindolol
- Iprocrolol
- Isoxaprolol
- Isamoltane
- Labetalol
- Landiolol
- Levobetaxolol
- Levobunolol
- Levomoprolol
- Medroxalol
- Mepindolol
- Metipranolol
- Metoprolol
- Moprolol
- Nadolol
- Nadoxolol
- Nebivolol
- Nifenalol
- Nipradilol
- Oxprenolol
- Pacrinolol
- Pafenolol
- Pamatolol
- Pargolol
- Penbutolol
- Pindolol
- Practolol
- Primidolol
- Procinolol
- Pronethalol
- Propafenone
- Propranolol
- Ridazolol
- Ronactolol
- Soquinolol
- Sotalol
- Spirendolol
- SR 59230A
- Sulfinalol
- Talinolol
- Tazolol
- Tertatolol
- Tienoxolol
- Tilisolol
- Timolol
- Tiprenolol
- Tolamolol
- Toliprolol
- Xibenolol
- Xipranolol
|
|
|
- See also: Dopaminergics
- Melatonergics
- Serotonergics
- Monoamine reuptake and release modulators
- Monoamine metabolism modulators
- Monoamine neurotoxins
|
Dopamine receptor modulators
|
|
D1-like |
Agonists |
- Benzazepines
- 6-Br-APB
- Fenoldopam
- SKF-38,393
- SKF-77,434
- SKF-81,297
- SKF-82,958
- SKF-83,959
- Trepipam
|
|
- Ergolines
- Cabergoline
- CY-208,243
- Dihydroergocryptine
- LEK-8829
- Lisuride
- Pergolide
- Terguride
|
|
- Dihydrexidine derivatives
- A-77636
- A-86929
- Adrogolide (ABT-431, DAS-431)
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine
|
|
- Phenethylamines
- Deoxyepinephrine (N-methyldopamine, epinine)
- Dopexamine
- Etilevodopa
- Ibopamine
- L-DOPA (levodopa)
- Melevodopa
- L-Phenylalanine
- L-Tyrosine
- XP21279
|
|
- Others
- A-68930
- Apomorphine
- Isocorypalmine
- Nuciferine
- Propylnorapomorphine
- Rotigotine
- SKF-89,145
- SKF-89,626
- Stepholidine
- Tetrahydropalmatine
|
|
|
Antagonists |
- Typical antipsychotics
- Butaclamol
- Chlorpromazine
- Chlorprothixene
- Flupentixol (flupenthixol) (+melitracen)
- Fluphenazine
- Loxapine
- Perphenazine (+amitriptyline)
- Pifluthixol
- Thioridazine
- Thiothixene
- Trifluoperazine (+tranylcypromine)
- Zuclopenthixol
|
|
- Atypical antipsychotics
- Asenapine
- Clorotepine
- Clotiapine
- Clozapine
- DHA-clozapine
- Fluperlapine
- Iloperidone
- Norclozapine
- Norquetiapine
- Olanzapine (++fluoxetine)
- Paliperidone
- Quetiapine
- Risperidone
- Tefludazine
- Zicronapine
- Ziprasidone
- Zotepine
|
|
- Others
- Ecopipam
- EEDQ
- Metitepine (methiothepin)
- SCH-23390
|
|
|
|
D2-like |
Agonists |
- Adamantanes
- Amantadine
- Memantine
- Rimantadine
|
|
- Aminotetralins
- 5-OH-DPAT
- 7-OH-DPAT
- 8-OH-PBZI
- Rotigotine
- UH-232
|
|
- Ergolines
- Bromocriptine
- Cabergoline
- Dihydroergocryptine
- Epicriptine
- Lisuride
- LSD
- Pergolide
- Terguride
|
|
- Dihydrexidine derivatives
- 2-OH-NPA
- Ciladopa
- Dihydrexidine
- Dinoxyline
- N,N-Propyldihydrexidine
|
|
- Phenethylamines
- Deoxyepinephrine (N-methyldopamine, epinine)
- Dopexamine
- Etilevodopa
- Ibopamine
- L-DOPA (levodopa)
- L-Phenylalanine
- L-Tyrosine
- Melevodopa
- XP21279
|
|
- Atypical antipsychotics
- Alentemol (U-66444B)
- Aripiprazole (+sertraline)
- Aripiprazole lauroxil
- Bifeprunox
- Brexpiprazole
- Cariprazine
- F-15063
- Lumateperone
- Norclozapine
- RP5063
|
|
- Others
- A-412,997
- ABT-670
- ABT-724
- Adrafinil
- Aplindore
- Apomorphine
- Arketamine
- Armodafinil
- BP-897
- Captodiame
- CP-226,269
- Dizocilpine
- Esketamine
- Flibanserin
- GSK-789,472
- Ketamine
- Mesulergine
- Modafinil
- OSU-6162
- Pardoprunox
- Phencyclidine
- PD-128,907
- PD-168,077
- PF-219,061
- PF-592,379
- Piribedil
- Pramipexole
- Propylnorapomorphine
- Pukateine
- Quinagolide
- Quinelorane
- Quinpirole
- RDS-127
- Ro10-5824
- Ropinirole
- Roxindole
- Salvinorin A
- SKF-83,959
- Sumanirole
- Talipexole
- Umespirone
- WAY-100,635
|
|
|
Antagonists |
- Typical antipsychotics
- Acepromazine
- Acetophenazine
- Azaperone
- Benperidol
- Bromperidol
- Butaclamol
- Butaperazine
- Chloracizine
- Clopenthixol
- Chlorproethazine
- Chlorpromazine
- Chlorprothixene
- Ciclindole
- Clothixamide
- Clopimozide
- Droperidol
- Fluacizine
- Fluanisone
- Flucindole
- Fluotracen
- Flupentixol (flupenthixol) (+melitracen)
- Fluphenazine
- Fluprothixene
- Fluspirilene
- Haloperidol
- Homopipramol
- Lenperone
- Levomepromazine (methotrimeprazine)
- Levosulpiride
- Loxapine
- Mesoridazine
- Moperone
- Naranol
- Nemonapride
- Penfluridol
- Perathiepin
- Perazine
- Pericyazine (periciazine)
- Perphenazine (+amitriptyline)
- Piflutixol (pifluthixol)
- Pimozide
- Pipamperone
- Prochlorperazine
- Promazine
- Prothipendyl
- Spiperone (spiroperidol)
- Sulforidazine
- Sulpiride
- Sultopride
- Teflutixol
- Thiopropazate
- Thioproperazine
- Thioridazine
- Thiothixene
- Timiperone
- Trifluoperazine (+tranylcypromine)
- Triflupromazine
- Trifluperidol
- Zetidoline
- Zuclopenthixol
|
|
- Atypical antipsychotics
- Amisulpride
- Asenapine
- BL-1020
- Blonanserin
- Carpipramine
- Cinuperone
- Clocapramine
- Clorotepine
- Clotiapine (clothiapine)
- Clozapine
- Cyamemazine
- DHA-clozapine
- Dixyrazine
- Elopiprazole
- Flumezapine
- Fluperlapine
- Gevotroline
- Iloperidone
- Lurasidone
- Mazapertine
- Melperone
- Molindone
- Mosapramine
- Ocaperidone
- Olanzapine (+fluoxetine)
- Paliperidone
- Perospirone
- Piperacetazine
- Pipotiazine
- Piquindone
- Quetiapine
- Remoxipride
- Risperidone
- Sertindole
- Tefludazine
- Tenilapine
- Tiospirone
- Veralipride
- Zicronapine
- Ziprasidone
- Zotepine
|
|
- Antiemetics/gastroprokinetics/sedatives
- Aceprometazine
- AS-8112
- Alimemazine
- Alizapride
- Benzquinamide
- Bromopride
- Clebopride
- Domperidone
- Eticlopride
- Hydroxyzine
- Itopride
- Metoclopramide
- Metopimazine
- Promethazine
- Thiethylperazine
- Trimethobenzamide
|
|
- Antidepressants
- Amoxapine
- Nefazodone
- Opipramol
- Propiomazine
- Trimipramine
|
|
- Others
- Azapride
- Buspirone
- Desmethoxyfallypride
- EEDQ
- F-15063
- Fallypride
- Fananserin
- Fenfluramine
- GSK-789,472
- Iodobenzamide
- Isocorypalmine
- L-741,626
- L-745,870
- Levofenfluramine
- LEK-8829
- Metergoline
- Metitepine (methiothepin)
- N-Methylspiperone
- Nafadotride
- Nuciferine
- PNU-99,194
- Pridopidine
- Raclopride
- Sarizotan
- SB-277,011-A
- Seridopidine
- Sonepiprazole
- Spiroxatrine
- Stepholidine
- SV-293
- Tetrahydropalmatine
- Tiapride
- UH-232
- Yohimbine
|
|
|
|
- See also: Adrenergics
- Melatonergics
- Serotonergics
- Monoamine reuptake and release modulators
- Monoamine metabolism modulators
- Monoamine neurotoxins
|
English Journal
- [The therapeutic plasma concentrations of antiparkinson dopamine agonists and their in vitro pharmacology at dopamine receptors].
- Tadori Y, Kobayashi H.
- Nihon shinkei seishin yakurigaku zasshi = Japanese journal of psychopharmacology.Nihon Shinkei Seishin Yakurigaku Zasshi.2014 Nov;34(5-6):127-32.
- This review discusses the relationship between therapeutic plasma concentrations of antiparkinson dopamine agonists (rotigotine, pergolide, cabergoline, apomorphine, bromocriptine, ropinirole, pramipexole, and talipexole) and their in vitro pharmacology at dopamine D1, D2 and D3 receptors. A signifi
- PMID 25536763
- Drug-induced hypothermia as beneficial treatment before and after cerebral ischemia.
- Johansen FF1, Hasseldam H, Rasmussen RS, Bisgaard AS, Bonfils PK, Poulsen SS, Hansen-Schwartz J.
- Pathobiology : journal of immunopathology, molecular and cellular biology.Pathobiology.2014;81(1):42-52. doi: 10.1159/000352026. Epub 2013 Aug 23.
- OBJECTIVES: Hypothermia is still unproven as beneficial treatment in human stroke, although in animal models, conditioning the brain with hypothermia has induced tolerance to insults. Here, we delineate the feasibility of drug-induced mild hypothermia in reducing ischemic brain damage when condition
- PMID 23989388
- Do dopamine agonists prevent or reduce the severity of ovarian hyperstimulation syndrome in women undergoing assisted reproduction? A systematic review and meta-analysis.
- Baumgarten M1, Polanski L, Campbell B, Raine-Fenning N.
- Human fertility (Cambridge, England).Hum Fertil (Camb).2013 Sep;16(3):168-74. doi: 10.3109/14647273.2013.833348.
- Controlled ovarian stimulation is an integral part of assisted reproduction treatment. This can result in ovarian hyperstimulation syndrome (OHSS), which is associated with significant morbidity and potentially mortality. Recent approaches to ovarian stimulation have led to a reduction in the preval
- PMID 24047196
Japanese Journal
- An anti-Parkinson drug ropinirole depletes orexin from rat hypothalamic slice culture
- 薬物療法 主な治療薬の種類と特徴 ドパミン受容体作動薬--概要,薬理作用,用法・用量,有用性,副作用とその対策 タリペキソール (パーキンソン病--基礎・臨床研究のアップデート) -- (治療)
Related Links
- Talipexole (B-HT920) is a dopamine agonist that has been proposed as an antiparkinsonian agent. ... "Protective effects of the antiparkinsonian drugs talipexole and pramipexole against 1-methyl-4-phenylpyridinium-induced apoptotic death ...
★リンクテーブル★
[★]
- 英
- antiparkinson agent, antiparkinsonism drug
- 関
- パーキンソン病、薬理学
ドパミン前駆体
ドパミン受容体作動薬
ドパミン放出促進
中枢性抗コリン作用
ノルアドレナリン前駆体
[★]
- 英
- talipexole
- 化
- 塩酸タリペキソール talipexole hydrochloride
- 商
- ドミン
- 関
- パーキンソン病
[★]
- 関
- talipexole