(S)-Terazosin

• 常用名: (S)-Terazosin
• 英文名: Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(tetrahydro-2-furanyl)carbonyl]-, (S)
• CAS号: 109351-33-9
• 分子量: 387.43300
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₉H₂₅N₅O₄
• 熔点: N/A
• 闪点: N/A

(S)-Terazosin用途

(S)-Terazosin 是 Terazosin 的有活性的 S 型异构体,也是一种有效的,高亲和力的 α-肾上腺素受体拮抗剂,对 α1a,α1b 和 α1d-肾上腺素受体的 Ki 值分别为 3.91 nM,0.79 nM 和 1.16 nM。(S)-Terazosin 对 α2a,α2B 和 α2c-肾上腺素受体也具有高亲和力,Ki 值分别为 729 nM,3.5 nM 和 46.4 nM。

(S)-Terazosin名称

• 英文名: (S)-Terazosin

(S)-Terazosin生物活性

• 描述: (S)-Terazosin 是 Terazosin 的有活性的 S 型异构体,也是一种有效的,高亲和力的 α-肾上腺素受体拮抗剂,对 α1a,α1b 和 α1d-肾上腺素受体的 Ki 值分别为 3.91 nM,0.79 nM 和 1.16 nM。(S)-Terazosin 对 α2a,α2B 和 α2c-肾上腺素受体也具有高亲和力,Ki 值分别为 729 nM,3.5 nM 和 46.4 nM。
• 相关类别:
  研究领域 >> 内分泌
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
• 靶点实验:

  Ki: 3.91 nM (α1a-adrenoceptor), 0.79 nM (α1b-adrenoceptor) and 1.16 nM (α1d-adrenoceptor); 729 nM (α2a-adrenoceptor), 3.5 nM (α2Ba-adrenoceptor) and 46.4 nM (α2c-adrenoceptor)[1]

• 体外研究: 外消旋化合物及其对映体对低纳米摩尔范围内Ki值α1肾上腺素能受体亚型具有高度和明显的等亲和力,对离体组织中α1肾上腺素能受体具有较强的拮抗作用,在每个α1肾上腺素能受体亚型上对映体与外消旋体的亲和力近似相等。在α2b位点,(R)-特拉唑嗪的结合强度低于(S)-特拉唑嗪或外消旋体[1]。
• 体内研究: (S) -特拉唑嗪对大鼠心房α2B受体有拮抗作用,pEC30为6.93。(s) -特拉唑嗪对大鼠输精管α1A和α2A受体有拮抗作用,pA2值分别为8.3和6.12[1]。
• 参考文献:

  [1]. Hancock AA, et al. Actions of terazosin and its enantiomers at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro. J Recept Signal Transduct Res. 1995 Sep-Dec;15(7-8):863-85.

(S)-Terazosin物理化学性质

• 分子式: C₁₉H₂₅N₅O₄
• 分子量: 387.43300
• 精确质量: 387.19100
• PSA: 103.04000
• LogP: 1.64090
• InChIKey: VCKUSRYTPJJLNI-AWEZNQCLSA-N
• SMILES: COc1cc2nc(N3CCN(C(=O)C4CCCO4)CC3)nc(N)c2cc1OC

(S)-Terazosin靶点实验

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实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

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实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

实验名称：Absorbance-based primary biochemical high throughput screening assay to identify acti... 来源：The Scripps Research Institute Molecular Screening Center 靶标：caspase-3 preproprotein [Homo sapiens] External Id：PROCASPASE3_ACT_EPIABS_1536_1X%ACT PRUN

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(S)-Terazosin英文别名

• (-)-(S)-terazosin
• S(-)-terazosin
• S(-)-2-[4-[(tetrahydro-2-furanyl)carbonyl]-1-piperazinyl]-6,7-dimethoxy-4-quinazolinamine