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Brexpiprazole

Brexpiprazole Struktur
913611-97-9
CAS-Nr.
913611-97-9
Englisch Name:
Brexpiprazole
Synonyma:
OPC-34712;Brexpiprazole impurity a;7-[4-(4-(Benzo[b]thien-4-yl)-piperazin-1-yl)butoxy]-1H-quinolin-2-one;7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one;7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one;CS-1678;ipiprazole;Epiprazole;Brexpiprazole;Brexipiprazole
CBNumber:
CB52681994
Summenformel:
C25H27N3O2S
Molgewicht:
433.57
MOL-Datei:
913611-97-9.mol

Brexpiprazole Eigenschaften

Schmelzpunkt:
179 - 181oC
Siedepunkt:
675.2±55.0 °C(Predicted)
Dichte
1.245±0.06 g/cm3(Predicted)
storage temp. 
Refrigerator
L?slichkeit
Dichloromethane (Slightly), Chloroform (Slightly), Methanol (Slightly)
pka
11.22±0.70(Predicted)
Aggregatzustand
Solid
Farbe
White to Off-White
InChI
InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29)
InChIKey
ZKIAIYBUSXZPLP-UHFFFAOYSA-N
SMILES
N1C2=C(C=CC(OCCCCN3CCN(C4=C5C=CSC5=CC=C4)CC3)=C2)C=CC1=O
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
H351 Kann vermutlich Krebs verursachen. Karzinogenit?t Kategorie 2 Warnung P201, P202, P281, P308+P313, P405,P501
H360 Kann die Fruchtbarkeit beeintr?chtigen oder das Kind im Mutterleib sch?digen. Fertility (Fruchtbarkeit) Kategorie 1 Achtung GHS hazard pictogramssrc="/GHS08.jpg" width="20" height="20" />
H362 Kann S?uglinge über die Muttermilch sch?digen. Reproductive toxicity, effects on or via lactation Additional category P201, P260, P263, P264, P270,P308+P313
H372 Sch?digt bei Hautkontakt und Verschlucken die Organe bei l?ngerer oder wiederholter Exposition. Spezifische Zielorgan-Toxizit?t (wiederholte Exposition) Kategorie 1 Achtung GHS hazard pictogramssrc="/GHS08.jpg" width="20" height="20" /> P260, P264, P270, P314, P501
H400 Sehr giftig für Wasserorganismen. Kurzfristig (akut) gew?ssergef?hrdend Kategorie 1 Warnung GHS hazard pictogramssrc="/GHS09.jpg" width="20" height="20" /> P273, P391, P501
H410 Sehr giftig für Wasserorganismen mit langfristiger Wirkung. Langfristig (chronisch) gew?ssergef?hrdend Kategorie 1 Warnung GHS hazard pictogramssrc="/GHS09.jpg" width="20" height="20" /> P273, P391, P501
Sicherheit
P201 Vor Gebrauch besondere Anweisungen einholen.
P202 Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.
P260 Dampf/Aerosol/Nebel nicht einatmen.
P263 Kontakt w?hrend der Schwangerschaft /und der Stillzeit vermeiden.
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P270 Bei Gebrauch nicht essen, trinken oder rauchen.
P273 Freisetzung in die Umwelt vermeiden.
P281 Vorgeschriebene pers?nliche Schutzausrüstung verwenden.
P308+P313 BEI Exposition oder falls betroffen: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen.
P314 Bei Unwohlsein ?rztlichen Rat einholen / ?rztliche Hilfe hinzuziehen.
P405 Unter Verschluss aufbewahren.
P501 Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Brexpiprazole Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Brexpiprazole is a novel antipsychotic drug which serves as a serotonin ® dopamine activity modulator and has demonstrated efficacy as an adjunctive treatment in patients with major depressive disorder (MDD). The drug exhibits a unique pharmacological profile, acting as a partial agonist of serotonin 5-HT1A and dopamine D2 receptors and as a full antagonist of 5-HT2A and noradrenaline α1B/2C receptors, with similar subnanomolar binding affinity. The drug, which was developed by Otsuka and Lundbeck, was approved in 2015 by the FDA for the treatment of schizophrenia and as an adjunctive treatment for depression. Brexpiprazole is widely considered to be a successor to Otsuka’s antipsychotic drug aripiprazole (trade name Abilify) whose patent expired in August 2014.

Verwenden

Brexpiprazole is a kind of atypical antipsychotic. It is a dopamine D2 receptor partial agonist. As a novel serotonin-dopamine activity modulator, it can be used for the treatment of schizophrenia, and for the adjunctive treatment for depression. It can also provide efficacy and tolerability over established adjunctive treatments formajor depressive disorder(MDD).Recent study has also suggested it can ameliorate PCP-induced cognitive deficits in mice via 5-HT1A receptors.

Definition

ChEBI: Brexpiprazole(913611-97-9) is a N-arylpiperazine. It is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. Brexpiprazole is a drug candidate useful in treatment and prevention of mental disorders including CNS disorders.

Synthese

Commercially available fluorobenzaldehyde (60) underwent a substitution reaction with commercial tert-butyl piperazine-1- carboxylate (61) under basic conditions to afford the piperazinyl benzaldehyde 62 in excellent yield. Next, the construction of the benzothiophene was affected by initial condensation of thioglycolic acid ethyl ester 63 with ochlorobenzaldehyde 62 under mildly basic conditions at elevated temperatures. Treatment with aqueous base and adjustment of pH to roughly 5 through the use of 4 N HCl furnished the 2-carboxylic acid benzothiophene 64 in 80% yield across the three-step operation. Next, decarboxylation through the use of cuprous oxide using conditions slightly modified from those originally described by Goosen followed by acidic removal of the Boc protecting group on the terminal piperazine nitrogen secured the key piperazinyl benzothiophene subunit 65 as the corresponding hydrochloride salt.
The hydroxyquinolone and linker component synthesis began with alkylation of commercially available quinolone 66 with 1,4-bromochlorobutane (67) under basic conditions to furnish chloroalkoxyquinolone 68. A subsequent alkylation with hydrochloride salt 65 using potassium carbonate and warm aqueous ethanol followed by recrystallizative workup resulted in clean conversion to brexpiprazole (VIII) in 78% yield from 68.

Synthesis_913611-97-9

Enzyminhibitor

This serotonin-dopamine activity modulator, or SDAM (FW = 433.60 g/mol; CAS 913611-97-9), also known as OPC-34712, Rexulti, 7-{4-[4-(1- benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one, is an atypical antipsychotic drug that acts as a dopamine D2L (Ki = 1.1 nM) and D3 (Ki = 0.3 nM) receptor partial agonist and a partial agonist of 5-HT1A receptors (Ki = 0.12 nM). Brexpiprazole is also an antagonist of the 5-HT2A (Ki = 0.47 nM), 5-HT2B (Ki = 1.9 nM), 5-HT7 (Ki = nM), α1B-adrenergic (Ki = 0.17 nM), α2C-adrenergic (Ki = 0.59 nM), and histamine H1 receptors (Ki = 19 nM). It has negligible affinity for the mACh receptors. Rexulti is an FDA-approved add-on medication for major depressive disorder in adults. See Aripiprazole

Mode of action

Brexpiprazole's suggested mechanism of action is based on its impact on dopamine and serotonin receptors. As a serotonin-dopamine activity modulator (SDAM), it acts as a novel partial agonist for D2 dopamine and serotonin 1A receptors while effectively blocking the serotonin 2A receptors, as well as noradrenergic alpha 1B and 2C receptors.

Einzelnachweise

https://en.wikipedia.org/wiki/Brexpiprazole
https://www.drugbank.ca/drugs/DB09128
Maeda, K, et al. "Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator." Journal of Pharmacology & Experimental Therapeutics 350.3(2014):589-604.
Maeda, K, et al. "Brexpiprazole II: antipsychotic-like and procognitive effects of a novel serotonin-dopamine activity modulator." Journal of Pharmacology & Experimental Therapeutics 350.3(2014):605.
Yoshimi, N, et al. "Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors. " Pharmacology Biochemistry & Behavior 124(2014):245.

Brexpiprazole Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Brexpiprazole Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 369)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Huadong Medicine (Xi'an)Bodyguard Pharmaceutical Co.,Ltd.
+86-029-86185165 +8618629664246
guoyuan@eastchinapharm.com China 1615 58
Changzhou Rokechem Technology Co., Ltd.
18758118018
sales001@rokechem.com China 255 58
Seasons Biotechnology Co., Ltd.
+86-0576-89232655 +86-13566878689
info@seasonsbio.com China 47 58
TAIZHOU YUXIN BIOTECHNOLOGY CO,.LTD
+86-576-88902229;+86-0576-88902229 +8613968687450
yuxin@yuxchem.com China 167 58
Beijing Hope Pharmaceutical Co., Ltd.
+86-010-67886402 +8613611125266
market@hopelife.cn China 71 58
Shijiazhuang Dingmin Pharmaceutical Sciences Co., Ltd.
+86-0311-67591193 +8613931880626
sales02@dingminpharma.com China 252 58
Dorne Chemical Technology co. LTD
+86-86-13583358881 +8618560316533
Ethan@dornechem.com China 3106 58
shandong perfect biotechnology co.ltd
+86-53169958659; +8618596095638
sales@sdperfect.com China 294 58
Zibo Hangyu Biotechnology Development Co., Ltd
+86-0533-2185556 +8617865335152
Mandy@hangyubiotech.com China 10986 58
Shandong Hanjiang Chemical Co., Ltd
+86-0533-2066820 +8618369939125
hanson@sdhanjiang.com China 999 58

913611-97-9()Verwandte Suche:


  • Brexpiprazole
  • 7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]- 2(1H)-Quinolinone
  • 7-[4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one
  • CS-1678
  • OPC 34712; OPC34712; OPC-34712
  • Brexpiprazole(OPC34712)
  • OPC-34712;OPC34712
  • 2(1H)-Quinolinone, 7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]-
  • Epipiprazole Impurities
  • Epipiprazole863
  • Epipiprazole864
  • Epipiprazole860
  • Impurities of Epipiprazole1
  • BrexpiprazoleQ: What is Brexpiprazole Q: What is the CAS Number of Brexpiprazole Q: What is the storage condition of Brexpiprazole
  • TIANFU CHEM---Brexpiprazole
  • 7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one
  • Brexpiprazole impurity a
  • 7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one
  • OPC-34712
  • 7-[4-(4-(Benzo[b]thien-4-yl)-piperazin-1-yl)butoxy]-1H-quinolin-2-one
  • 7-[4-[4-(4-Benzothienyl)-1-piperazinyl]butoxy]quinolin-2(1H)-one
  • Brexpiprazole Crude
  • Brexpiprazole 7-[4-(4-Benzo[b]thien-4-yl-1-piperazinyl)butoxy]-2(1H)- quinolinone
  • ipiprazole
  • Epiprazole
  • Brexipiprazole
  • 913611-97-9
  • Dopamine D2 receptor partial agonist
  • API
  • Inhibitors
  • 913611-97-9
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