四氢罂粟碱盐酸盐 T6423

Product Introduction
Bioactivity


英文名: BRL-15572 dihydrochloride

描述: BRL-15572 dihydrochloride (BRL 15573 dihydrochloride) 是一种 5-HT1D 受体拮抗剂，pKi 为 7.9，对 5-HT1A 和 5-HT2B 受体也显示出相当大的亲和力，其选择性是 5-HT1B 受体的 60 倍。

细胞实验: [35S]GTPγS binding studies. [35S]GTPγS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1 × 106 cells are preincubated at 30°C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 μ M), with or without BRL-15572. The reaction is started by the addition of 10 μL of [35S]GTPγS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30°C. Non-specific binding is determined by addition of unlabelled GTPγS (10 μM), prior to the addition of cells. The reaction is stopped by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Radioactivity is determined by liquid scintillation spectrometry.(Only for Reference)

体外活性: BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 μM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors. [1] In human atrial appendages, the electrically evoked tritium overflow is inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors). [2] The inhibitory effect of 5-HT on the K+-evoked overflow of glutamate is antagonized by the h5-HT1D receptor ligand BRL-15572. BRL-15572 (1 μM) is unable to modify the effect of 5-HT at the autoreceptor regulating [3H]5-HT release. [3] The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247. [4]

体内活性: In diabetic pithed rats, administration of the selective 5-HT1D receptor antagonist BRL-15572 (2 mg/kg) does not modify the decreased HR induced by vagal electrical stimulation. The effects of L-694,247 (50 μg/kg), a selective agonist for non-rodent 5-HT1B and 5-HT1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572. [5]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 89 mg/mL (185.5 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 38 mg/mL (79.2 mM)


关键字: h5-HT1D | BRL 15572 dihydrochloride | BRL-15573 | BRL15573 Dihydrochloride | BRL-15572 | BRL 15572 Dihydrochloride | BRL 15573 | BRL 15572 | 5-HT Receptor | BRL15572 | BRL-15573 Dihydrochloride | BRL15573 | Inhibitor | Serotonin Receptor | BRL15572 dihydrochloride | 5-hydroxytryptamine Receptor | inhibit | BRL 15573 Dihydrochloride | BRL15572 Dihydrochloride | BRL-15572 Dihydrochloride

相关产品: SB-224289 hydrochloride | Granisetron hydrochloride | RS 67333 hydrochloride | GR 46611 | LY-2624803 | (S)-Amisulpride | Jujuboside B1 | Iferanserin | (S)-Bexicaserin | Ondansetron

相关库: Anti-Neurodegenerative Disease Compound Library | Neurotransmitter Receptor Compound Library | Anti-Parkinson's Disease Compound Library | Angiogenesis related Compound Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Inhibitor Library | GPCR Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

四氢罂粟碱盐酸盐 T6423信息由TargetMol中国为您提供，如您想了解更多关于四氢罂粟碱盐酸盐 T6423报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途