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147416-96-4

中文名稱 替侖西平二鹽酸鹽
英文名稱 TELENZEPINE DIHYDROCHLORIDE
CAS 147416-96-4
分子式 C19H22N4O2S
分子量 370.47
MOL 文件 147416-96-4.mol
147416-96-4 結(jié)構(gòu)式 147416-96-4 結(jié)構(gòu)式

基本信息

中文別名
替侖西平二鹽酸鹽
英文別名
TelenzepineHydrochloride
Telenzepine dihydrochloide
TELENZEPINE DIHYDROCHLORIDE
JTQJFSQQHGPLOX-UHFFFAOYSA-N
Telenzepine hydrate dihydrochloride
TELENZEPINE DIHYDROCHLORIDE SELECTIVE M1 MUSCARIN
4,9-Dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl)-(10H)
4,9-Dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl)-(10H)thieno[3,4-b][1,5]benzodiazepin-10-onedihydrochloride
4,9-DIHYDRO-3-METHYL-4-[(4-METHYL-1-PIPERAZINYL)ACETYL]-10H-THIENO[3,4-B][1,5] BENZODIAZEPIN-10-ONE DIHYDROCHLORIDE

物理化學(xué)性質(zhì)

儲(chǔ)存條件Store at RT
溶解度H2O: >10 mg/mL
溶解度H2O: >10 mg/mL
形態(tài)solid
顏色white
水溶解性溶于水至100mM

安全數(shù)據(jù)

WGK Germany3
WGK Germany3
替侖西平二鹽酸鹽價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/02/08HY-B1789A替侖西平二鹽酸鹽
Telenzepine dihydrochloride
147416-96-45 mg580元
2025/02/08HY-B1789A替侖西平二鹽酸鹽
Telenzepine dihydrochloride
147416-96-410 mg925元
2025/02/08HY-B1789A替侖西平二鹽酸鹽
Telenzepine dihydrochloride
147416-96-425 mg1850元

常見問題列表

生物活性
Telenzepine dihydrochloride 是一種選擇性和具有口服活性的毒蕈堿 M1 受體拮抗劑,Ki 為 0.94 nM。Telenzepine dihydrochloride 抑制胃酸分泌并具有抗?jié)冏饔谩?/span>
靶點(diǎn)

Ki: 0.94 nM (Muscarinic M1 receptor), 17.8 nM (Muscarinic M2 receptor)

體外研究

At submicromolar concentrations (100 nM), Telenzepine abolishes responses to either muscarine or the muscarinic component of the acetylcholine response. The excitatory effect of muscarine at postsynaptic M1 receptors is dose dependently inhibited by Telenzepine (0.1-1000 nM) at concentrations.
The threshold dose of Telenzepine as an antagonist of the muscarinic depolarization in AH/type 2 neurons is in the range of 0.1-1 nM. The IC 50 of Telenzepine needed to abolish the response is 8.5 nM.

體內(nèi)研究

Intravenous Telenzepine potently inhibits gastric acid secretion in the Ghosh-Schild rat (carbachol-stimulated), the chronic fistula rat (basal secretion), or, both intravenously and orally, in the modified Shay rat.
Telenzepine (2.7 μmol/kg; orally) treatment shows significantly longer duration antiulcer effects in the modified Shay rat.

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