Prochlorperazinmaleat

Bezeichnung:Prochlorperazinmaleat

CAS-Nr84-02-6

Englisch Name:PROCHLORPERAZINE MALEATE

CBNumberCB2439552

SummenformelC28H32ClN3O8S

Molgewicht606.09

MOL-Datei84-02-6.mol

Synonyma

Prochlorperazinmaleat

Prochlorperazinmaleat physikalisch-chemischer Eigenschaften

Schmelzpunkt	1750C
storage temp.	2-8°C
Löslichkeit	Very slightly soluble in water and in ethanol (96 per cent).
pka	pKa 8.1(H2O,t =24±1) (Uncertain)
Farbe	White
maximale Wellenlänge (λmax)	313nm(MeOH)(lit.)
Merck	14,7761
Stabilität	Stable for 2 years as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	20/21/22
S-Sätze:	36
WGK Germany	3
RTECS-Nr.	SO3150000
HS Code	2934302300
Toxizität	LD50 in mice (mg/kg): 400 s.c.; 120 i.p.; 90 i.v., 400 orally (Courvoisier)

Gefahreninformationscode (GHS)

PROCHLORPERAZINE MALEATE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Prochlorperazine maleate (84-02-6) inhibits dynamin and clathrin-mediated endocytosis (CME) with an IC50=5.8 μM for CME.1?Increases tumor cell antigen presentation enhancing the efficacy of anti-tumor mAbs.2?A clinically useful antipsychotic agent3?with antimigraine4?and antiemetic activity5.
Chemische Eigenschaften
Off-White Powder
Verwenden
Antiemetic;Dopamine antagonist
Verwenden
Antiemetic.
Trademarks
Compazine (GlaxoSmithKline).
Allgemeine Beschreibung
Prochlorperazinemaleate, 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazinemaleate (Compazine), is in the piperazine subgroupof the phenothiazines, characterized by high-milligramantipsychotic potency, a high prevalence of EPS, and lowsedative and autonomic effects. Prochlorperazine is more potenton a milligram basis than its alkylamino counterpart,chlorpromazine. Because of the high prevalence of EPS, however,it is used mainly for its antiemetic effect, not for its antipsychoticeffect.
Biologische Aktivität
D 2 receptor antagonist. Also interacts with 5-HT 3 and nAChR. Displays antipsychotic, antispasmodic, antiemetic and antinociceptive activity in vivo .
Biochem/physiol Actions
Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic
Einzelnachweise
References/Citations 1) Daniel?et al.?(2015),?Phenothiazine-derived antipsychotic drugs inhibit dynamin and clathrin-mediated endocytosis; Traffic,?16?635 2) Chew?et al.?(2020),?Endocytosis Inhibition in Humans to Improve Responses to ADCC-Mediating Antibodies; Cell,?180?895 3) Hollister?et al.?(1969),?Clinical use of psychotherapeutic drugs: current status;?Clin. Pharmacol. Ther.,?10?170 4) Cook and Newberry (2018),?Emergency Department Use of Intravenous Prochlorperazine for Acute Migraine; Adv. Emerg. Nurs. J.,?40?148 5) Van den Berg?et al.?(1996),?The prophylactic antiemetic efficacy of prochlorperazine and ondansetron in nasal septal surgery: a randomized double-blind comparison; Anaesth. Intensive Care,?24?538

Prochlorperazinmaleat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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