(S)-5-Methoxy-N-propyl-2-aminotetraline hydrochloride - CAS 93601-86-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Dopamine Receptor
(S)-5-Methoxy-N-propyl-2-Aminotetraline hydrochloride is a dopamine receptor agonist.
Brife Description:
dopamine receptor agonist
White to Off-White Solid
(S)-5-Methoxy-N-propyl-1,2,3,4-tetrahydronaphthalen-2-amine hydrochloride; (S)-1,2,3,4-Tetrahydro-5-methoxy-N-propyl-2-naphthalenamine Hydrochloride; Aminotetraline hydrochloride, (S)-5-Methoxy-N-propyl-2-
Melting Point:
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1.TASP0434299: A novel pyridopyrimidin-4-one derivative as a radioligand for vasopressin V1B receptor.
Koga K1, Yoshinaga M1, Uematsu Y1, Nagai Y2, Miyakoshi N1, Shimoda Y2, Fujinaga M2, Minamimoto T2, Zhang MR2, Higuchi M2, Ohtake N1, Suhara T2, Chaki S3. J Pharmacol Exp Ther. 2016 Mar 30. pii: jpet.116.232942. [Epub ahead of print]
A novel pyridopyrimidin-4-one derivative, N-tert-butyl-2-[2-(3-methoxyphenyl)-6-[3-(morpholin-4-yl)propoxy]-4-oxopyrido[2,3-d]pyrimidin-3(4H)-yl]acetamide (TASP0434299), was characterized as a radioligand candidate for arginine vasopressin receptor 1B (V1B receptor). TASP0434299 exhibited high binding affinities for human and rat V1B receptors with IC50 values of 0.526 and 0.641 nM, respectively, and a potent antagonistic activity at human V1B receptor with an IC50 value of 0.639 nM without apparent binding affinities for other molecules at 1 μM. [3H]TASP0434299 bound to membranes expressing human V1B receptor as well as those prepared from the rat anterior pituitary in a saturable manner. The binding of [3H]TASP0434299 to the membranes was dose-dependently displaced by several ligands for V1B receptor. In addition, the intravenous administration of [3H]TASP0434299 to rats produced a saturable radioactive accumulation in the anterior pituitary where V1B receptor is enriched, and it was dose-dependently blocked by the oral administration of 2-[2-(3-chloro-4-fluorophenyl)-6-[3-(morpholin-4-yl)propoxy]-4-oxopyrido[2,3-d]pyrimidin-3(4H)-yl]-N-isopropylacetamide hydrochloride (TASP0390325), a V1B receptor antagonist, indicating that [3H]TASP0434299 can be used as an in vivo radiotracer to measure the occupancy of V1B receptor.
2.Effect of Sulindac and Erlotinib vs Placebo on Duodenal Neoplasia in Familial Adenomatous Polyposis: A Randomized Clinical Trial.
Samadder NJ1, Neklason DW2, Boucher KM3, Byrne KR4, Kanth P4, Samowitz W5, Jones D6, Tavtigian SV6, Done MW7, Berry T7, Jasperson K7, Pappas L7, Smith L7, Sample D7, Davis R7, Topham MK8, Lynch P9, Strait E10, McKinnon W11, Burt RW12, Kuwada SK13. JAMA. 2016 Mar 22-29;315(12):1266-75. doi: 10.1001/jama.2016.2522.
IMPORTANCE: Patients with familial adenomatous polyposis (FAP) are at markedly increased risk for duodenal polyps and cancer. Surgical and endoscopic management of duodenal neoplasia is difficult and chemoprevention has not been successful.
3.Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Waszkielewicz AM1, Gunia-Krzyżak A2, Powroźnik B3, Słoczyńska K3, Pękala E3, Walczak M4, Bednarski M5, Żesławska E6, Nitek W7, Marona H2. Bioorg Med Chem. 2016 Apr 15;24(8):1793-810. doi: 10.1016/j.bmc.2016.03.006. Epub 2016 Mar 3.
A series of thirty N-(phenoxy)alkyl or N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols has been designed, synthesized and evaluated for anticonvulsant activity in MES, 6Hz test, and pilocarpine-induced status epilepticus. Among the title compounds, the most promising seems R-(-)-2N-{2-[2-(2,6-dimethylphenoxy)ethoxy]ethyl}aminopropan-1-ol hydrochloride (22a) with proved absolute configuration with X-ray analysis and enantiomeric purity. The compound is effective in MES test with ED50=12.92mg/kg b.w. and its rotarod TD50=33.26mg/kg b.w. The activity dose is also effective in a neurogenic pain model-the formalin test. Within high throughput profile assay, among eighty one targets, the strongest affinity of the compound is observed towards σ receptors and 5-HT transporter and the compound does not bind to hERG. It also does not exhibit mutagenic properties in the Vibrio harveyi test. Moreover, murine liver microsomal assay and pharmacokinetics profile (mice, iv, p.
4.Preparation of Fe2O3-Clorprenaline/Tetraphenylborate Nanospheres and Their Application as Ion Selective Electrode for Determination of Clorprenaline in Pork.
Shao X1, Zhang J1, Li D1, Yue J2, Chen Z3. Nanoscale Res Lett. 2016 Dec;11(1):178. doi: 10.1186/s11671-016-1388-7. Epub 2016 Apr 5.
A novel modified ion selective electrode based on Fe2O3-clorprenaline/tetraphenylborate nanospheres (Fe2O3-CLPT NSs) as electroactive materials for the determination of clorprenaline hydrochloride (CLP) is described. The α-Fe2O3 nanoparticles (NPs) were prepared by hydrothermal synthesis, then self-assembled on CLP/tetraphenylborate (TPB) to form Fe2O3-CLPT NSs, which were used as a potentiometric electrode for analyte determination innovatively. The Fe2O3-CLPT NSs modified electrode exhibited a wider concentration range from 1.0 × 10(-7) to 1.0 × 10(-1) mol/L and a lower detection limit of 3.7 × 10(-8) mol/L compared with unmodified electrodes. The selectivity of the modified electrode was evaluated by fixed interference method. The good performance of the modified electrode such as wide pH range (2.4-6.7), fast response time (15 s), and adequate lifetime (14 weeks) indicate the utility of the modified electrode for evaluation of CLP content in various real samples.
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CAS 93601-86-6 (S)-5-Methoxy-N-propyl-2-aminotetraline hydrochloride

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