Tag: 347.8541

R- and L-type Ca²⁺ channels are insensitive to eliprodil in rat cultured cerebellar granule neurons was written by Biton, B.;Godet, D.;Granger, P.;Avenet, P.. And the article was included in European Journal of Pharmacology in 1997.Quality Control of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol This article mentions the following:

We have investigated, by using the whole-cell patch-clamp technique, the Ca²⁺ channel antagonist properties of eliprodil in cultured cerebellar granule cells which are known to express L-, N-, P- as well as Q- and R-type Ca²⁺ channels. Eliprodil maximally antagonized 50 of the voltage-dependent Ba²⁺ current with an IC₅₀ of 4 渭M. 蠅-Conotoxin-GVIA (3.2 渭M) and 蠅-agatoxin-IVA (0.5 渭M) blocked 28% and 43% of the current, resp. When eliprodil (30 渭M) was added to 蠅-conotoxin-GVIA or 蠅-agatoxin-IVA the magnitude of the maximal inhibition was identical to that obtained with eliprodil alone confirming a full blockade by eliprodil of N-, P- and Q-type Ca²⁺ channels. The L-type channel antagonist nimodipine (10 渭M) blocked 24% of the current; this blockade was fully additive to that of eliprodil, indicating that the nimodipine-sensitive component of the current is eliprodil-insensitive. In the presence of eliprodil and nimodipine a residual Cd²⁺ sensitive current (25%), identified as the R-type current, remained unblocked. We conclude that in cerebellar granule neurons R- and L-type Ca²⁺ channels are insensitive to eliprodil. The nimodipine- sensitive channels present in cerebellar granule neurons may represent a neuronal subtype of L channels distinct from that (eliprodil-sensitive/nimodipine-sensitive) present in cortical or hippocampal neurons. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3Quality Control of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol).

1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3) 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.Quality Control of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Characterization of haloperidol and trifluperidol as subtype-selective N-methyl-D-aspartate (NMDA) receptor antagonists using [³H]TCP and [³H]ifenprodil binding in rat brain membranes was written by Coughenour, Linda L.;Cordon, John J.. And the article was included in Journal of Pharmacology and Experimental Therapeutics in 1997.Quality Control of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol This article mentions the following:

[³H]TCP and [³H]ifenprodil binding to N-methyl-D-aspartate (NMDA) receptors in rat forebrain membranes was used to compare the inhibition of haloperiodol and trifluperidol with that of ifenprodil and eliprodil. In the [³H]TCP binding assay, inhibition curves of ifenprodil, eliprodil, haloperidol and trifluperidol revealed two affinity states in the presence of glutamate, glycine and spermidine. The potency of these agents to inhibit the high-affinity fraction of the binding agreed with the results of other studies investigating their potency to block glutamate-induced current at recombinant NR1a/NR2B NMDA receptors expressed in Xenopus oocytes. These agents also inhibited [³H]ifenprodil binding in a biphasic manner, whether in the absence or the presence of either the sigma site ligand GBR-12909 affinity sites labeled with [³H]ifenprodil. The only alteration in the affinity was a decrease in the IC₅₀ value of haloperidol to inhibit the high-affinity fraction of [³H]ifenprodil binding. GBR-12909 also reduced the fraction of [³H]ifenprodil sites inhibited by these compounds with high affinity, with no change in the affinity for either fraction. These data suggest that spermidine is neither a competitive antagonist at the fraction of the binding inhibited by these agents with high affinity, nor is this fraction of the binding to sigma sites. Haloperidol and trifluperidol represent a new class of agent that interacts at a site that is labeled by [³H]ifenprodil as well as [³H]TCP in rat brain membranes and that closely reflects ifenprodil’s voltage-independent site on the recombinant NR1a/NR2B subtype of the NMDA receptor. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3Quality Control of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol).

1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Quality Control of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Administration of Memantine During Withdrawal Mitigates Overactivity and Spatial Learning Impairments Associated with Neonatal Alcohol Exposure in Rats was written by Idrus, Nirelia M.;McGough, Nancy N. H.;Riley, Edward P.;Thomas, Jennifer D.. And the article was included in Alcoholism: Clinical & Experimental Research in 2014.Safety of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol This article mentions the following:

Background : Prenatal alc. exposure can disrupt central nervous system development, manifesting as behavioral deficits that include motor, emotional, and cognitive dysfunction. Both clin. and animal studies have reported binge drinking during development to be highly correlated with an increased risk of fetal alc. spectrum disorders (FASD). We hypothesized that binge drinking may be especially damaging because it is associated with episodes of alc. withdrawal. Specifically, we have been investigating the possibility that NMDA receptor-mediated excitotoxicity occurs during alc. withdrawal and contributes to developmental alc.-related neuropathol. Consistent with this hypothesis, administration of the NMDA receptor antagonists MK-801 or eliprodil during withdrawal attenuates behavioral alterations associated with early alc. exposure. In this study, we investigated the effects of memantine, a clin. used NMDA receptor antagonist, on minimizing ethanol-induced overactivity and spatial learning deficits. Methods : Sprague-Dawley pups were exposed to 6.0 g/kg ethanol via intubation on postnatal day (PD) 6, a period of brain development that models late gestation in humans. Controls were intubated with a calorically matched maltose solution During withdrawal, 24 and 36 h after ethanol exposure, subjects were injected with a total of either 0, 20, or 30 mg/kg memantine. The subjects’ locomotor levels were recorded in open field activity monitors on PDs 18 to 21 and on a serial spatial discrimination reversal learning task on PDs 40 to 43. Results : Alc. exposure induced overactivity and impaired performance in spatial learning. Memantine administration significantly attenuated the ethanol-associated behavioral alterations in a dose-dependent manner. Thus, memantine may be neuroprotective when administered during ethanol withdrawal. Conclusions : These data have important implications for the treatment of EtOH’s neurotoxic effects and provide further support that ethanol withdrawal significantly contributes to FASD. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3Safety of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol).

1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3) 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. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Safety of 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Neuroprotective effects of 7-nitroindazole in the gerbil model of global cerebral ischemia was written by O’Neill, Michael J.;Hicks, Caroline;Ward, Mark. And the article was included in European Journal of Pharmacology in 1996.SDS of cas: 119431-25-3 This article mentions the following:

To evaluate the role played by nitric oxide in global cerebral ischemia we examined the effects of 7-nitroindazole and a sodium salt of 7-nitroindazole (inhibitors of neuronal nitric oxide (NO) synthase) and N^G-nitro-L-arginine Me ester (a more general inhibitor of NO synthase) in the gerbil model of cerebral ischemia. Four experiments were carried out. In the first experiment, animals were either sham -operated, subjected to 5 min bilateral carotid occlusion (BCAO) or administered 7-nitroindazole or N^G-nitro-L-arginine Me ester immediately after occlusion followed by three further doses at 3, 6 and 24 h post-occlusion. In the second experiment, we examined the effects of a sodium salt of 7-nitroindazole, which is more soluble than 7-nitroindazole, using the same protocol. In the third experiment, the effects of the sodium salt of 7-nitroindazole administered at 10 mg/kg at 0, 3, 6, 24, 27, 30, 33, 52, 55, 72, 75 and 78 h post-occlusion or at 0.05 mg/h for 72 h via mini-pumps were evaluated. In sep. experiments, we examined the effects of three reference compounds dizocilpine (MK-801), 2,3-dihydroxy-6-nitro-7-sulfamoylbenz(F)quinoxaline (NBQX) and eliprodil using the same model. Extensive neuronal death was observed in the CA1 layer of the hippocampus in 5 min bilateral carotid occluded animals 5 days after surgery. Both 7-nitroindazole and N^G-nitro-L-arginine Me ester provided significant neuroprotection against this neuronal death. The sodium salt of 7-nitroindazole showed no protection when administered up to 12 times post-occlusion, but did provide significant neuroprotection when administered via mini-pump. The neuroprotection was similar to that provided by MK-801 and eliprodil, but not as good as that observed with NBQX. These results indicate that nitric oxide plays a role in ischemic cell death and that selective neuronal nitric oxide synthase inhibitors can protect against ischemic brain damage. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3SDS of cas: 119431-25-3).

1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.SDS of cas: 119431-25-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

High throughput measurement of Ca⁺⁺ dynamics in human stem cell-derived cardiomyocytes by kinetic image cytometry: a cardiac risk assessment characterization using a large panel of cardioactive and inactive compounds was written by Lu, Hua Rong;Whittaker, Ross;Price, Jeffrey H.;Vega, Raquel;Pfeiffer, Emily R.;Cerignoli, Fabio;Towart, Rob;Gallacher, David J.. And the article was included in Toxicological Sciences in 2015.Reference of 119431-25-3 This article mentions the following:

Human induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) are emerging as a powerful in vitro model for cardiac safety assessment which may allow for better identification of compounds with poor arrhythmogenic liability profiles early in the drug discovery process. Here, we describe our examination of the Kinetic Image Cytometer (KIC) system’s ability to predict adverse compound effects using hiPS-CMs and a library of 53 compounds, the majority of which are known to be cardioactive compounds, and several neg. controls. The KIC provides a high throughput method for analyzing intracellular calcium transients. In the cardiomyocyte, intracellular calcium transients integrate the electrochem. signals of the action potential (AP) with the mol. signaling pathways regulating contraction. Drug-induced alterations in the shape and duration of AP result in changes to the shape and duration of the intracellular calcium transient. By examining calcium transient dynamics in hiPS-CMs, KIC can be used as a phenotypic screen to assess compound effects across multiple ion channel types (MITs), detecting MITs, calcium handling and signaling effects. The results of this blinded study indicate that using hiPS-CMs, KIC is able to accurately detect drug-induced changes in Ca²⁺ transient dynamics (ie, duration and beat rate) and therefore, may be useful in predicting drug-induced arrhythmogenic liabilities in early de-risking within the drug discovery phase. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3Reference of 119431-25-3).

1-(4-Chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethan-1-ol (cas: 119431-25-3) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Reference of 119431-25-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem