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Pimozid

Pimozide Struktur
2062-78-4
CAS-Nr.
2062-78-4
Bezeichnung:
Pimozid
Englisch Name:
Pimozide
Synonyma:
orap;OPIRAN;R 6238;Pimochi;PIMOZIDE;PriMozide;NSC 170984;mcn-jr-6238;Pimozide CRS;PIMOZIDE USP
CBNumber:
CB7290660
Summenformel:
C28H29F2N3O
Molgewicht:
461.55
MOL-Datei:
2062-78-4.mol

Pimozid Eigenschaften

Schmelzpunkt:
214-218°
Dichte
1.1763 (estimate)
storage temp. 
2-8°C
L?slichkeit
DMSO: 18 mg/mL
Aggregatzustand
White solid
pka
7.32(at 25℃)
Farbe
Off-White to Light Orange
Wasserl?slichkeit
2.9mg/L(30 ºC)
InChIKey
YVUQSNJEYSNKRX-UHFFFAOYSA-N
SMILES
O=C1NC2=CC=CC=C2N1C3CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3
CAS Datenbank
2062-78-4(CAS DataBase Reference)
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher Xn
R-S?tze: 22
S-S?tze: 36
RIDADR  3249
WGK Germany  3
RTECS-Nr. DE1750000
HazardClass  6.1(b)
PackingGroup  III
HS Code  2933399090
Speicherklasse 11 - Combustible Solids
Hazard Classifications Acute Tox. 4 Oral
Bildanzeige (GHS) Exclamation Mark (GHS07)
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung P264, P270, P301+P312, P330, P501
Sicherheit

Pimozid Chemische Eigenschaften,Einsatz,Produktion Methoden

R-S?tze Betriebsanweisung:

R22:Gesundheitssch?dlich beim Verschlucken.

S-S?tze Betriebsanweisung:

S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

Beschreibung

Pimozide is a dopamine receptor antagonist (Kis = 2.4, 0.3, and 1.8 nM for D2, D3, and D4 receptors, respectively). It also binds to eight additional receptors (Kds = 25-3,100 nM for the human receptors) and inhibits the voltage-gated sodium channel Nav1.2 and the voltage-gated potassium channel Kv11.1 (IC50s = 42 and 340 nM, respectively). Pimozide (0.5, 1, and 2 mg/kg) decreases the number of licks and reduces fluid intake of a sweetened solution in rats. It decreases the number of threats and attacks and increases immobility time in the neutral arena aggression test, indicating increased passiveness, in male mice when administered at a dose of 0.75 mg/kg for 10 days. Formulations containing pimozide have been used in the treatment of Tourette syndrome.

Chemische Eigenschaften

White or almost white powder.

Verwenden

Pimozide is a D2 dopamine receptor antagonist that binds to the cloned 5-HT7 receptor with high affinity (1,2,3,4). Pimozide is also a Ca2+ channel antagonist. Pimozide is used as an antipsychotic.

Definition

ChEBI: Pimozide is a member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. It has a role as a H1-receptor antagonist, a serotonergic antagonist, a first generation antipsychotic, an antidyskinesia agent and a dopaminergic antagonist. It is a member of benzimidazoles, an organofluorine compound and a heteroarylpiperidine.

Allgemeine Beschreibung

Pimozide, 1-[1-[4,4-bis(p-fluorophenyl)butyl]-4-piperidyl]-2-benzimidazolinone (Orap), isa white to creamy white solid (pKa=9.42). Pimozide is 50%absorbed after oral administration. It is metabolized byCYP450 enzymes, in particular the CYP3A4 and CYP1A2isozymes, to inactive metabolites. Pimozide is excreted in theurine and to a lesser extent in the feces. Toxic effects may beproduced with pimozide in the presence of inducers or inhibitorsof CYP3A4 and CYP1A2. Pimozide is also a stronginhibitor of CYP2D6 without appearing to be an importantsubstrate of this isoform.99 The use of pimozide in the UnitedStates is small, but it is a critical drug for many patients withGilles de la Tourette disorder who cannot tolerate haloperidol.

Biologische Aktivit?t

Dopamine D 2 -receptor antagonist and antipsychotic which binds with very high affinity to the cloned rat 5-HT 7 receptor (K i = 0.5 nM).

Pimozid Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Pimozid Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 157)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21587 55
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49979 58
TargetMol Chemicals Inc.
+1-781-999-5354; +17819995354
marketing@targetmol.com United States 32466 58
Hefei TNJ Chemical Industry Co.,Ltd.
+86-0551-65418671 +8618949823763
sales@tnjchem.com China 34563 58
AFINE CHEMICALS LIMITED
+86-0571-85134551
sales@afinechem.com China 15075 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471;
sales@sarms4muscle.com China 10473 58
CR Corporation Limited
+8613062833949
fred.wen@crcorporation.cn China 8645 58
Shaanxi Didu New Materials Co. Ltd
+86-86-17392712697 +8617792793228
1069@dideu.com China 8585 58
Shanghai Acmec Biochemical Technology Co., Ltd.
+86-18621343501; +undefined18621343501
product@acmec-e.com China 33324 58
Aladdin Scientific

tp@aladdinsci.com United States 57505 58

2062-78-4(Pimozid)Verwandte Suche:


  • PIMOZIDE
  • 1-(1-(4,4-bis(p-fluorophenyl)butyl)-4-piperidyl)-2-benzimidazolinon
  • 1-(1-(4,4-bis(p-fluorophenyl)butyl)-4-piperidyl)-2-benzimidazolinone
  • 1-(4,4-bis(p-fluorophenyl)butyl)-4-(2-oxo-1-benzimidazolinyl)piperidine
  • mcn-jr-6238
  • 1-[1-(4,4-BIS[4-FLUOROPHENYL]BUTYL)-4-PIPERIDINYL]-1,3-DIHYDRO-2H-BENZ-IMIDAZOL-2-ONE
  • 3-(1-(4,4-bis(4-fluorophenyl)butyl)-4-piperidyl)-1H-benzimidazol-2-one
  • 2H-Benzimidazol-2-one, 1-1-4,4-bis(4-fluorophenyl)butyl-4-piperidinyl-1,3-dihydro-
  • OPIRAN
  • 1-[1-[4,4-Bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazole-2-one
  • 1-[1-[4,4-Bis(4-fluorophenyl)butyl]-4-piperidyl]-1,3-dihydro-2H-benzimidazol-2-one
  • R 6238
  • 3-[1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl]-1H-benzimidazol-2-one
  • Pimozide (200 mg)
  • NSC 170984
  • PriMozide
  • 1-(1-(4,4-bis(4-fluorophenyl)butyl)piperidin-4-yl)-1H-benzo[d]iMidazol-2(3H)-one
  • STAT5 Inhibitor III, Pimozide
  • STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem
  • Pimozide CRS
  • PIMOZIDE USP/EP/BP
  • Pimozide (10mM in DMSO)
  • Pimozide D4Q: What is Pimozide D4 Q: What is the CAS Number of Pimozide D4 Q: What is the storage condition of Pimozide D4
  • Pimozide (1539508)
  • orap
  • Pyridine,2,3,6-trichloro-9-nitro-
  • Pimochi
  • Pimozide in methanol
  • PIMOZIDE USP
  • Pimozide solution
  • Pimozide for system suitability CRS
  • Pimozide (Standard)
  • 2062-78-4
  • 2062-78-2
  • C28H29F2N3O
  • Inhibitors
  • ORAP
  • Organics
  • Dopamine receptor
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