Category: 85375-15-1

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

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