09/17/21 News Top Picks: new discover of 111635-08-6

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Chemical Research Letters, May 2021. Application In Synthesis of 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.111635-08-6, Name is 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, molecular formula is C10H14ClN. In a Article,once mentioned of 111635-08-6

Background Most of the currently used antidepressant drugs are monoamine-based compounds, acting by the inhibition of re-uptake or metabolism of noradrenaline (NA) and/or serotonin (5-HT), because these neurotransmitters play a key role in the pathophysiology of depression. The aim of this study was to investigate the potential antidepressant-like activity of an endogenous amine, 1,2,3,4-tetrahydroisoquinoline (TIQ) and its close derivative, 1-methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ). Methods The experiments were carried out on male C57BL6J mice. The antidepressant-like activity of TIQs was evaluated in the behavioral tests: the forced swim test (FST) and tail suspension test (TST) and neurochemical analysis. TIQ and 1MeTIQ were administrated in three differences doses of 10, 25 or 50 mg/kg. Imipramine (IMI; 15 or 30 mg/kg) was used as a reference drug. In the neurochemical ex vivo study, the levels of NA, 5-HT and their metabolites, the rate of monoamine metabolism and their neuronal activity in different mouse brain structures were determined by HPLC with electrochemical detection. Results The results of this study have demonstrated that TIQ and 1MeTIQ produced antidepressant-like effect in the FST and TST because they significantly decreased the immobility time comparably to IMI. Biochemical data have demonstrated that administration of TIQs led to the activation of NA and 5-HT systems. Conclusions The results reported in this paper indicate that TIQ and 1MeTIQ possess a distinct antidepressant activity. In the light of these findings, we suggest that both tested compounds may be effective for the depression therapy in a clinical setting with better tolerance of side effects.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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New research progress on 111635-08-6 in 2021. Recommanded Product: 111635-08-6, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 111635-08-6, molcular formula is C10H14ClN, introducing its new discovery.

Diuretic and saluretic tetrahydro-isoquinoline derivatives of the Formula (I) STR1 wherein R stands for hydrogen or chlorine, R1 and R2 are hydrogen, methoxy or ethoxy, and R3 and R4 are hydrogen or methyl, and a process for the preparation thereof as well as pharmaceutical compositions containing as active ingredients isoquinoline derivatives of the Formula (I). The compounds of Formula I are prepared by reacting a 2-amino-tetrahydro-isoquinoline derivative of the Formula (II) STR2 with a carboxylic acid derivative of the Formula (III) STR3 wherein x stands for chlorine, –OH, –OCH2 CN, –OCH3, –OC2 H5, –OCOOCH3 or –OCOOC2 H5 R5 and R6 stand for hydrogen or together from CHN(CH3)2 and in case of the Formula (Ia) STR4 splitting off the protective group in alkaline medium.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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A series of N-(4-chloro-3-sulfamoylbenzamido)-1,2,3,4-tetrahydroquinoline (IV-1) and isoquinoline (IV-2) have been synthesized and their diuretic and antihypertensive activities evaluated. While none of the test compounds was found to be provided with antihypertensive properties, most of them displayed a diuretic activity comparable to (IV-2 a) or higher (IV-1 a,b) (IV-2 c) than those of indapamide and clopamide, taken as reference drugs.

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Tetrahydroisoquinoline – Wikipedia,
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Compounds of the benzylamine (BA) class are potent inhibitors of phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28). Restriction of the aminomethyl side chain through its incorporation into a cyclic framework as in 1,2,3,4-tetrahydroisoquinoline (THIQ) or 2,3,4,5-tetrahydro-1H-2-benzazepine (THBA) results in enhanced potency as an inhibitor, suggesting a conformational effect in the binding of BAs to the active site; however, these ring systems still retain a high degree of flexibility. We have synthesized a series of conformationally defined analogues of benzylamine in order to probe the effect of conformation, as well as the influence of steric bulk, on PNMT inhibition by this class of ligands. In addition, 1-, 3-, and 4-methyl-substituted THIQs were synthesized and evaluated as flexible models for steric bulk tolerance about this ring system. Substitution by a methyl group on either benzylic position of THIQ results in diminished activity as a PNMT inhibitor; however, 3-methyl-THIQ (11) shows enhanced activity as an inhibitor vs THIQ itself. Full conformational restriction of the BA side chain in analogues 4-8 results in a dramatic loss in inhibitor potency. We attribute this effect to a negative steric interaction between the alkyl bridging units above (or below) the heterocyclic ring systems and an active-site amino acid residue. Conformational restriction of THIQ employing a bridging unit that is not located above (or below) the ring system (9) results in only slightly diminished activity compared to THIQ itself. The relative activities of 4-8 were examined in terms of the conformational descriptors tau1 and tau2. Although there is no correlation between tau1 and activity as a PNMT inhibitor, a qualitative relationship between tau2 (endo or exo) and activity with PNMT is apparent. We believe that the binding of the N-H and/or N-lone pair of electrons may influence the spatial orientation of these molecules at the active site, resulting in positive binding interactions for compounds 4 and 8 and negative interactions for analogues 5-7. The results from the current investigation are compared to those obtained from a similar study involving conformationally defined amphetamines.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.

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Tetrahydroisoquinoline – Wikipedia,
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Electric Literature of 111635-08-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.111635-08-6, Name is 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, molecular formula is C10H14ClN. In a Patent,once mentioned of 111635-08-6

TETRAHYDROISOQUINOLINE DERIVATIVES

The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.

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Tetrahydroisoquinoline – Wikipedia,
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Related Products of 111635-08-6, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 111635-08-6, molcular formula is C10H14ClN, introducing its new discovery.

Conformational and steric aspects of the inhibition of phenylethanolamine N-methyltransferase by benzylamines

Compounds of the benzylamine (BA) class are potent inhibitors of phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28). Restriction of the aminomethyl side chain through its incorporation into a cyclic framework as in 1,2,3,4-tetrahydroisoquinoline (THIQ) or 2,3,4,5-tetrahydro-1H-2-benzazepine (THBA) results in enhanced potency as an inhibitor, suggesting a conformational effect in the binding of BAs to the active site; however, these ring systems still retain a high degree of flexibility. We have synthesized a series of conformationally defined analogues of benzylamine in order to probe the effect of conformation, as well as the influence of steric bulk, on PNMT inhibition by this class of ligands. In addition, 1-, 3-, and 4-methyl-substituted THIQs were synthesized and evaluated as flexible models for steric bulk tolerance about this ring system. Substitution by a methyl group on either benzylic position of THIQ results in diminished activity as a PNMT inhibitor; however, 3-methyl-THIQ (11) shows enhanced activity as an inhibitor vs THIQ itself. Full conformational restriction of the BA side chain in analogues 4-8 results in a dramatic loss in inhibitor potency. We attribute this effect to a negative steric interaction between the alkyl bridging units above (or below) the heterocyclic ring systems and an active-site amino acid residue. Conformational restriction of THIQ employing a bridging unit that is not located above (or below) the ring system (9) results in only slightly diminished activity compared to THIQ itself. The relative activities of 4-8 were examined in terms of the conformational descriptors tau1 and tau2. Although there is no correlation between tau1 and activity as a PNMT inhibitor, a qualitative relationship between tau2 (endo or exo) and activity with PNMT is apparent. We believe that the binding of the N-H and/or N-lone pair of electrons may influence the spatial orientation of these molecules at the active site, resulting in positive binding interactions for compounds 4 and 8 and negative interactions for analogues 5-7. The results from the current investigation are compared to those obtained from a similar study involving conformationally defined amphetamines.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 111635-08-6, in my other articles.

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 111635-08-6, Name is 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, molecular formula is C10H14ClN

Diuretic agents related to indapamide: III – Synthesis and pharmacological activity of N-(4-chloro-3-sulfamoylbenzamido)-1,2,3,4-tetrahydroquinolines 1,2,3,4-tetrahydroisoquinolines.

A series of N-(4-chloro-3-sulfamoylbenzamido)-1,2,3,4-tetrahydroquinoline (IV-1) and isoquinoline (IV-2) have been synthesized and their diuretic and antihypertensive activities evaluated. While none of the test compounds was found to be provided with antihypertensive properties, most of them displayed a diuretic activity comparable to (IV-2 a) or higher (IV-1 a,b) (IV-2 c) than those of indapamide and clopamide, taken as reference drugs.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 111635-08-6, in my other articles.

Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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111635-08-6, Name is 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride, belongs to tetrahydroisoquinoline compound, is a common compound. Recommanded Product: 1-Methyl-1,2,3,4-tetrahydroisoquinoline hydrochlorideIn an article, once mentioned the new application about 111635-08-6.

Antidepressant-like effect of 1,2,3,4-tetrahydroisoquinoline and its methyl derivative in animal models of depression

Background Most of the currently used antidepressant drugs are monoamine-based compounds, acting by the inhibition of re-uptake or metabolism of noradrenaline (NA) and/or serotonin (5-HT), because these neurotransmitters play a key role in the pathophysiology of depression. The aim of this study was to investigate the potential antidepressant-like activity of an endogenous amine, 1,2,3,4-tetrahydroisoquinoline (TIQ) and its close derivative, 1-methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ). Methods The experiments were carried out on male C57BL6J mice. The antidepressant-like activity of TIQs was evaluated in the behavioral tests: the forced swim test (FST) and tail suspension test (TST) and neurochemical analysis. TIQ and 1MeTIQ were administrated in three differences doses of 10, 25 or 50?mg/kg. Imipramine (IMI; 15 or 30?mg/kg) was used as a reference drug. In the neurochemical ex vivo study, the levels of NA, 5-HT and their metabolites, the rate of monoamine metabolism and their neuronal activity in different mouse brain structures were determined by HPLC with electrochemical detection. Results The results of this study have demonstrated that TIQ and 1MeTIQ produced antidepressant-like effect in the FST and TST because they significantly decreased the immobility time comparably to IMI. Biochemical data have demonstrated that administration of TIQs led to the activation of NA and 5-HT systems. Conclusions The results reported in this paper indicate that TIQ and 1MeTIQ possess a distinct antidepressant activity. In the light of these findings, we suggest that both tested compounds may be effective for the depression therapy in a clinical setting with better tolerance of side effects.

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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2-amino-tetrahydro-isoquinolene derivatives and a process for the preparation thereof and pharmaceutical compositions containing same

Diuretic and saluretic tetrahydro-isoquinoline derivatives of the Formula (I) STR1 wherein R stands for hydrogen or chlorine, R1 and R2 are hydrogen, methoxy or ethoxy, and R3 and R4 are hydrogen or methyl, and a process for the preparation thereof as well as pharmaceutical compositions containing as active ingredients isoquinoline derivatives of the Formula (I). The compounds of Formula I are prepared by reacting a 2-amino-tetrahydro-isoquinoline derivative of the Formula (II) STR2 with a carboxylic acid derivative of the Formula (III) STR3 wherein x stands for chlorine, –OH, –OCH2 CN, –OCH3, –OC2 H5, –OCOOCH3 or –OCOOC2 H5 R5 and R6 stand for hydrogen or together from CHN(CH3)2 and in case of the Formula (Ia) STR4 splitting off the protective group in alkaline medium.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem