Tag: 371.9004

Ali, Fadia E. et al. published their research in Journal of Medicinal Chemistry in 1985 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Formula: C22H26ClNO2

Orally active and potent inhibitors of 纬-aminobutyric acid uptake was written by Ali, Fadia E.;Bondinell, William E.;Dandridge, Penelope A.;Frazee, James S.;Garvey, Eleanor;Girard, Gerald R.;Kaiser, Carl;Ku, Thomas W.;Lafferty, John J.. And the article was included in Journal of Medicinal Chemistry in 1985.Formula: C22H26ClNO2 This article mentions the following:

GABA聽聽[56-12-2]-uptake inhibitors that are more potent, more lipophilic, and in limited testing, at least as selective as the parent amino acids were obtained by alkylation of the appropriate butyric-, cyclohexane- and piperidinecarboxylic and pyrrolinidineacetic acids. The ability of these alkylated amino acids to inhibit Na-dependent, high-affinity GABA uptake was measured after preincubation for 15 min with rat brain synaptosomes. N-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic聽acid (I) [85375-85-5] is a specific GABA-uptake inhibitor more potent, more lipophilic and, as selective as the nonalkylated parent; I and its analogs also exhibited anticovulsant activity in rodents. Structure-activity relations are discussed. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Formula: C22H26ClNO2).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Formula: C22H26ClNO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Sato, Hitoshi et al. published their research in Tenkan Kenkyu in 1996 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Computed Properties of C22H26ClNO2

Anticonvulsant effects of GABA uptake inhibitors: their profile of action in the rat kindling model of epilepsy was written by Sato, Hitoshi;Morimoto, Kiyoshi;Suwaki, Hiroshi. And the article was included in Tenkan Kenkyu in 1996.Computed Properties of C22H26ClNO2 This article mentions the following:

GABA uptake inhibitors are newly developed antiepileptic drugs. In this study, we analyzed the antiepileptic profile of GABA uptake inhibitors, Tiagabine, SKF-89976A and NNC-711, in the rat kindling model, which is a chronic exptl. model of human complex partial seizures with secondary generalization. We examined the dose-dependent anticonvulsant effects of the GABA uptake inhibitors in amygdala (AM)- and hippocampal (HIPP)-kindled seizures, and compared their anticonvulsant and behavioral side effects with those of Valproate (VPA) and Carbamazepine (CBZ). In AM- and HIPP-kindled rats, i.p. administration of the GABA uptake inhibitors (2.50-20 mg/kg) significantly reduced the seizure stage and after-discharge (AD) duration in dose-dependent manners, compared with vehicle treatment. The anticonvulsant potencies of the 3 GABA uptake inhibitors were in the order: NNC-711 > Tiagabine >> SKF89976A, which was related to the in vitro GABA uptake efficacy, and they were similar between AM- and HIPP-kindled seizures. High doses of GABA uptake inhibitors (20-40 mg/kg) caused sedation, motor impairment and EEG paroxyms with myoclonus. When the correlation between the anticonvulsant and behavioral side effects was examined, GABA uptake inhibitors showed more potent anticonvulsant and less side effects, compared with VPA and CBZ. These results indicate the clin. usefulness of GABA uptake inhibitors in temporal lobe epilepsy. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Computed Properties of C22H26ClNO2).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Computed Properties of C22H26ClNO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

N’Goka, Victor et al. published their research in European Journal of Medicinal Chemistry in 2004 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of SKF-89976A Hydrochloride

Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids was written by N’Goka, Victor;Stenbol, Tine B.;Krogsgaard-Larsen, Povl;Schlewer, Gilbert. And the article was included in European Journal of Medicinal Chemistry in 2004.Application In Synthesis of SKF-89976A Hydrochloride This article mentions the following:

Nipecotic acid derivatives, I [R1 = Ph, 4-PhC6H4, 2-MeC6H4; R2 = Ph, 2-MeC6H4, H, 2-ClC6H4, 伪-thienyl; R1R2 = fluorenyl, dibenzosuberyl; R3 = H, Et], bearing an aryl iminoxymethyl side chain at the position 6 were synthesized and tested for their GABA uptake inhibitory properties. Contrarily to the N-substituted derivatives, the introduction of the oxime function in the side chain of analogs of the active nipecotic derivative does neither increase, nor maintain the activity. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Application In Synthesis of SKF-89976A Hydrochloride).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of SKF-89976A Hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Hirayama, Bruce A. et al. published their research in British Journal of Pharmacology in 2001 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Synthetic Route of C22H26ClNO2

Common mechanisms of inhibition for the Na+/glucose (hSGLT1) and Na+/Cl–/GABA (hGAT1) cotransporters was written by Hirayama, Bruce A.;Diez-Sampedro, Ana;Wright, Ernest M.. And the article was included in British Journal of Pharmacology in 2001.Synthetic Route of C22H26ClNO2 This article mentions the following:

1 Electrophysiol. methods were used to investigate the interaction of inhibitors with the human Na+/glucose (hSGLT1) and Na+/Cl–/GABA (hGAT1) cotransporters. Inhibitor constants were estimated from both inhibition of substrate-dependent current and inhibitor-induced changes in cotransporter conformation. 2 The competitive, non-transported inhibitors are substrate derivatives with inhibition constants from 200 nM (phlorizin) to 17 mM (esculin) for hSGLT1, and 300 nM (SKF89976A) to 10 mM (baclofen) for hGAT1. At least for hSGLT1, values determined using either method were proportional over 5-orders of magnitude. 3 Correlation of inhibition to structure of the inhibitors resulted in a pharmacophore for glycoside binding to hSGLT1: the aglycon is coplanar with the pyranose ring, and binds to a hydrophobic/aromatic surface of at least 7脳12脜. Important hydrogen bond interactions occur at five positions bordering this surface. 4 In both hSGLT1 and hGAT1 the data suggests that there is a large, hydrophobic inhibitor binding site 鈭?脜 from the substrate binding site. This suggests an architectural similarity between hSGLT1 and hGAT1. There is also structural similarity between non-competitive and competitive inhibitors, e.g., phloretin is the aglycon of phlorizin (hSGLT1) and nortriptyline resembles SKF89976A without nipecotic acid (hGAT1). 5 Our studies establish that measurement of the effect of inhibitors on presteady state currents is a valid non-radioactive method for the determination of inhibitor binding constants Furthermore, anal. of the presteady state currents provide novel insights into partial reactions of the transport cycle and mode of action of the inhibitors. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Synthetic Route of C22H26ClNO2).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Synthetic Route of C22H26ClNO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

N’Goka, Victor et al. published their research in European Journal of Medicinal Chemistry in 2004 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of SKF-89976A Hydrochloride

Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids was written by N’Goka, Victor;Stenbol, Tine B.;Krogsgaard-Larsen, Povl;Schlewer, Gilbert. And the article was included in European Journal of Medicinal Chemistry in 2004.Application In Synthesis of SKF-89976A Hydrochloride This article mentions the following:

Nipecotic acid derivatives, I [R1 = Ph, 4-PhC6H4, 2-MeC6H4; R2 = Ph, 2-MeC6H4, H, 2-ClC6H4, α-thienyl; R1R2 = fluorenyl, dibenzosuberyl; R3 = H, Et], bearing an aryl iminoxymethyl side chain at the position 6 were synthesized and tested for their GABA uptake inhibitory properties. Contrarily to the N-substituted derivatives, the introduction of the oxime function in the side chain of analogs of the active nipecotic derivative does neither increase, nor maintain the activity. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Application In Synthesis of SKF-89976A Hydrochloride).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of SKF-89976A Hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Hirayama, Bruce A. et al. published their research in British Journal of Pharmacology in 2001 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Synthetic Route of C22H26ClNO2

Common mechanisms of inhibition for the Na+/glucose (hSGLT1) and Na+/Cl–/GABA (hGAT1) cotransporters was written by Hirayama, Bruce A.;Diez-Sampedro, Ana;Wright, Ernest M.. And the article was included in British Journal of Pharmacology in 2001.Synthetic Route of C22H26ClNO2 This article mentions the following:

1 Electrophysiol. methods were used to investigate the interaction of inhibitors with the human Na+/glucose (hSGLT1) and Na+/Cl–/GABA (hGAT1) cotransporters. Inhibitor constants were estimated from both inhibition of substrate-dependent current and inhibitor-induced changes in cotransporter conformation. 2 The competitive, non-transported inhibitors are substrate derivatives with inhibition constants from 200 nM (phlorizin) to 17 mM (esculin) for hSGLT1, and 300 nM (SKF89976A) to 10 mM (baclofen) for hGAT1. At least for hSGLT1, values determined using either method were proportional over 5-orders of magnitude. 3 Correlation of inhibition to structure of the inhibitors resulted in a pharmacophore for glycoside binding to hSGLT1: the aglycon is coplanar with the pyranose ring, and binds to a hydrophobic/aromatic surface of at least 7×12Å. Important hydrogen bond interactions occur at five positions bordering this surface. 4 In both hSGLT1 and hGAT1 the data suggests that there is a large, hydrophobic inhibitor binding site ∼8Å from the substrate binding site. This suggests an architectural similarity between hSGLT1 and hGAT1. There is also structural similarity between non-competitive and competitive inhibitors, e.g., phloretin is the aglycon of phlorizin (hSGLT1) and nortriptyline resembles SKF89976A without nipecotic acid (hGAT1). 5 Our studies establish that measurement of the effect of inhibitors on presteady state currents is a valid non-radioactive method for the determination of inhibitor binding constants Furthermore, anal. of the presteady state currents provide novel insights into partial reactions of the transport cycle and mode of action of the inhibitors. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Synthetic Route of C22H26ClNO2).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Synthetic Route of C22H26ClNO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

N’Goka, Victor et al. published their research in European Journal of Medicinal Chemistry in 2004 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of SKF-89976A Hydrochloride

Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids was written by N’Goka, Victor;Stenbol, Tine B.;Krogsgaard-Larsen, Povl;Schlewer, Gilbert. And the article was included in European Journal of Medicinal Chemistry in 2004.Application In Synthesis of SKF-89976A Hydrochloride This article mentions the following:

Nipecotic acid derivatives, I [R1 = Ph, 4-PhC6H4, 2-MeC6H4; R2 = Ph, 2-MeC6H4, H, 2-ClC6H4, α-thienyl; R1R2 = fluorenyl, dibenzosuberyl; R3 = H, Et], bearing an aryl iminoxymethyl side chain at the position 6 were synthesized and tested for their GABA uptake inhibitory properties. Contrarily to the N-substituted derivatives, the introduction of the oxime function in the side chain of analogs of the active nipecotic derivative does neither increase, nor maintain the activity. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Application In Synthesis of SKF-89976A Hydrochloride).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of SKF-89976A Hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Hirayama, Bruce A. et al. published their research in British Journal of Pharmacology in 2001 | CAS: 85375-15-1

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Synthetic Route of C22H26ClNO2

Common mechanisms of inhibition for the Na+/glucose (hSGLT1) and Na+/Cl–/GABA (hGAT1) cotransporters was written by Hirayama, Bruce A.;Diez-Sampedro, Ana;Wright, Ernest M.. And the article was included in British Journal of Pharmacology in 2001.Synthetic Route of C22H26ClNO2 This article mentions the following:

1 Electrophysiol. methods were used to investigate the interaction of inhibitors with the human Na+/glucose (hSGLT1) and Na+/Cl–/GABA (hGAT1) cotransporters. Inhibitor constants were estimated from both inhibition of substrate-dependent current and inhibitor-induced changes in cotransporter conformation. 2 The competitive, non-transported inhibitors are substrate derivatives with inhibition constants from 200 nM (phlorizin) to 17 mM (esculin) for hSGLT1, and 300 nM (SKF89976A) to 10 mM (baclofen) for hGAT1. At least for hSGLT1, values determined using either method were proportional over 5-orders of magnitude. 3 Correlation of inhibition to structure of the inhibitors resulted in a pharmacophore for glycoside binding to hSGLT1: the aglycon is coplanar with the pyranose ring, and binds to a hydrophobic/aromatic surface of at least 7×12Å. Important hydrogen bond interactions occur at five positions bordering this surface. 4 In both hSGLT1 and hGAT1 the data suggests that there is a large, hydrophobic inhibitor binding site ∼8Å from the substrate binding site. This suggests an architectural similarity between hSGLT1 and hGAT1. There is also structural similarity between non-competitive and competitive inhibitors, e.g., phloretin is the aglycon of phlorizin (hSGLT1) and nortriptyline resembles SKF89976A without nipecotic acid (hGAT1). 5 Our studies establish that measurement of the effect of inhibitors on presteady state currents is a valid non-radioactive method for the determination of inhibitor binding constants Furthermore, anal. of the presteady state currents provide novel insights into partial reactions of the transport cycle and mode of action of the inhibitors. In the experiment, the researchers used many compounds, for example, SKF-89976A Hydrochloride (cas: 85375-15-1Synthetic Route of C22H26ClNO2).

SKF-89976A Hydrochloride (cas: 85375-15-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Synthetic Route of C22H26ClNO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem