Category: 1690-72-8

Spivak, Charles E.; Waters, James A.; Aronstam, Robert S. published an article in Molecular Pharmacology. The title of the article was 《Binding of semirigid nicotinic agonists to nicotinic and muscarinic receptors》.COA of Formula: C8H15NO2 The author mentioned the following in the article:

Isoarecolone methiodide (1-methyl-4-acetyl-1,2,3,6-tetrahydropyridine methiodide) was previously shown to be among the most potent agonists tested at the frog neuromuscular junction. Because nicotinic receptors from different sources vary in their selectivities, isoarecolone methiodide as well as 19 addnl. congeners, most of which were also previously tested at the frog neuromuscular junction, were studied in binding assays. Torpedo nobiliana was the tissue source for nicotinic receptors. Two types of experiments were conducted. The first evaluated the affinities of the agonists (including acetylcholine and carbamylcholine) for the recognition site by allowing the agonists to compete for that site with 125I-α-bungarotoxin. The inhibition potencies obtained correlated strongly (Spearman’s correlation coefficient, -0.91) with the potency obtained at the frog neuromuscular junction. The second type of experiment evaluated the agonists for their ability to activate the receptor. The binding of [3H]perhydrohistrionicotoxin, which was employed as an indicator of the activation of the receptor, was measured in the presence of each of the agonists. Isoarecolone methiodide was the most potent of all. A few of the agonists (partial agonists) were incapable of fully enhancing this binding. For the full agonists, the concentration that produced half of the maximum binding of [3H]perhydrohistrionicotoxin was defined as the EC50. The correlation coefficient (Spearman’s) for EC50 vs. potency at the frog neuromuscular junction was -0.73, indicating innate differences between Torpedo and frog receptors. In addition, these compounds were treated for their affinity at muscarinic receptors from rat brain. Competition experiments were carried out using [3H]N-methylscopolamine. The affinity of isoarecolone methiodide was only about 7-fold lower than that of acetylcholine and less than 2-fold lower than that of carbamylcholine. In contrast, 1-methyl-4-acetylpiperazine methiodide was much more selective for nicotinic receptors. Its activity was similar to isoarecolone methiodide at the nicotinic receptor, but it was among the weakest compounds in its affinity for the muscarinic receptor. The experimental process involved the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8COA of Formula: C8H15NO2)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.COA of Formula: C8H15NO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Avery, E. E.; Baevsky, M. F.; Braswell, S. J.; Duffus, C. W.; Evans, G. O. II; Rocha, D. K.; Wynne, R. A. published their research in Journal of Molecular Catalysis on August 1 ,1989. The article was titled 《Palladium phosphine-catalyzed hydroesterifications of unsaturated nitrogen heterocycles》.Reference of Methyl 1-methylpiperidine-3-carboxylate The article contains the following contents:

Pd(PPh3)2Cl2-catalyzed hydroesterification of HCl salts of 1,2,3,6-tetrahydropyridine derivatives gave 37-95% conversion to mixtures of isomeric Me esters. E.g., treatment of N-carbethoxynortropidine with CO-MeOH in MeCOEt containing Pd(PPh3)2Cl2 gave 95% conversion to mainly 3- and 4-(carbomethoxy)isomers I and II, resp., in 1:1.5 ratio. The experimental part of the paper was very detailed, including the reaction process of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Reference of Methyl 1-methylpiperidine-3-carboxylate)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Reference of Methyl 1-methylpiperidine-3-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Swain, C. J.; Baker, R.; Kneen, C.; Moseley, J.; Saunders, J.; Seward, E. M.; Stevenson, G.; Beer, M.; Stanton, J.; Watling, K. published an article on January 31 ,1991. The article was titled 《Novel 5-HT3 antagonists. Indole oxadiazoles》, and you may find the article in Journal of Medicinal Chemistry.Safety of Methyl 1-methylpiperidine-3-carboxylate The information in the text is summarized as follows:

The synthesis and biochem. evaluation of a series of oxadiazole and indolyloxadiazole 5-HT3 (hydroxytryptamine) antagonists are described. The key pharmacophoric elements have been defined as a basic nitrogen, a linking group capable of H-bonding interactions, and an aromatic moiety. The steric limitations of the aromatic binding site have been determined by substitution about the indole ring. Variation of the heterocyclic linking group has shown that while 2 H-bonding interactions are possible, only 1 is essential for high affinity. The environment of the basic nitrogen has been investigated and shown to be optimal when constrained within an azabicyclic system. These results have been incorporated into a proposed binding model for the 5-HT3 antagonist binding site, in which the optimum distance between the aromatic binding site and the basic amine is 8.4-8.9 Å and the steric limitations are defined by van der Waals difference mapping. The experimental process involved the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Safety of Methyl 1-methylpiperidine-3-carboxylate)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Safety of Methyl 1-methylpiperidine-3-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinson’s agents》 were Tiwari, Shashi B.; Kohli, D. V.. And the article was published in Medicinal Chemistry Research in 2008. Recommanded Product: 1690-72-8 The author mentioned the following in the article:

A series of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole derivatives, e.g., I, was prepared and their evaluation for anti-Parkinson’s activity was measured in vivo using albino rats. The result of the biol. activity studies indicated that some of the synthesized compounds have good agonistic activity on the dopamine receptors and a few of them were also found to be free from neurotoxicity. Thus these compounds might be useful ligands for studying the functional role of dopamine receptors in vivo. The high log P value of the compounds indicates that they should easily cross the blood-brain barrier (log P > 2.6). In the experimental materials used by the author, we found Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Recommanded Product: 1690-72-8)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Recommanded Product: 1690-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Diffusion of reduced arecoline and arecaidine through human vaginal and buccal mucosa》 was written by Van der Bijl, P.; Van Eyk, A. D.; Van Wyk, C. W.; Stander, I. A.. Category: piperidines And the article was included in Journal of Oral Pathology & Medicine on April 30 ,2001. The article conveys some information:

Because alkaloids from areca nut, arecoline and arecaidine, have been implicated in the development of oral submucous fibrosis, the authors determined their diffusion kinetics through human buccal and vaginal mucosa. Four clin. healthy vaginal mucosa specimens (mean patient age ± standard deviation: 47±15 yr; age range: 31-60 yr) and 4 buccal mucosa specimens from 2 male patients and 2 female patients (mean patient age ± standard deviation: 31±9 yr; age range: 17-53 yr) were obtained during surgery. In vitro flux rates of reduced arecoline and arecaidine (r-arecoline and r-arecaidine) were determined by use of a flow-through diffusion apparatus Anal. of variance, a Duncan multiple range test, and an unpaired t-test were used to determine steady state kinetics and flux differences over time intervals. Although statistically significant differences were observed between flux values for both alkaloids and tissues at certain time points, these were not considered to be of biol. (clin.) significance. However, the flux rates across both mucosa of r-arecoline were significantly higher statistically than those of r-arecaidine. The findings demonstrated the differences in the diffusion kinetics between r-arecoline and r-arecaidine across human buccal and vaginal mucosa, an observation that could be explained in terms of their ionization characteristics. Addnl., the results obtained further support the hypothesis that human vaginal mucosa can be used as a model for buccal mucosa in studies of permeability to various chem. compounds The results came from multiple reactions, including the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Category: piperidines)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Related Products of 1690-72-8On October 31, 1990 ,《Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors》 appeared in Journal of Medicinal Chemistry. The author of the article were Street, Leslie J.; Baker, Raymond; Book, Tracey; Kneen, Clare O.; MacLeod, Angus M.; Merchant, Kevin J.; Showell, Graham A.; Saunders, John; Herbert, Richard H.. The article conveys some information:

The synthesis and biochem. evaluation of novel 1,2,4-oxadiazole-based muscarinic agonists which can readily penetrate into the CNS is reported. Efficacy and binding of these compounds are markedly influenced by the structure and physicochem. properties of the cationic head group. In a series of azabicyclic ligands efficacy and affinity are influenced by the size of the surface area presented to the receptor at the active site, and the degree of conformational flexibility. The exo-1-azanorbornane I represents the optimum arrangement, and this compound is one of the most efficacious and potent muscarinic agonists known. In a series of isoquinuclidine-based muscarinic agonists efficacy and affinity are influenced by the geometry between the cationic head group and H-bond acceptor pharmacophore and steric bulk in the vicinity of the base. The anti configuration represented by II is optimal for muscarinic activity. Ligands with pKa <6.5 show poor binding to the muscarinic receptor as exemplified by the diazabicyclic derivative III. In the experiment, the researchers used Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Related Products of 1690-72-8)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. 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. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Related Products of 1690-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 1971,European Journal of Pharmacology included an article by Jung, Annemarie; Luellmann, Heinz; Ziegler, Albrecht. Electric Literature of C8H15NO2. The article was titled 《Attempt to correlate kinetic data of the drug receptor interaction with the chemical structures of cholinomimetic agents》. The information in the text is summarized as follows:

The chem. structures of cholinomimetic agents, such as acetylcholine (I) [51-84-3]; carbachol [51-83-2]; muscarine [300-54-9]; different esters of secondary, tertiary, or quaternary arecaidines or Δ3-pyrrolinecarboxylic acids; and the acetates of pyrrolidinol and pyrrolidinecarbinol, and their association and dissociation rate constants could be used to estimate their ability to bind with the receptor sites of isolated guinea pig atria. The ability to bind, as well as the kinetic constants, was dependant on the number of C-atoms at the N, the length of the ester side chain, the conformation for the heterocyclic ring system, and the position of the ester group. The influence of structural characteristics of the cholinergics on their properties was different from that on the parameters that determine their binding ability. The results came from multiple reactions, including the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Electric Literature of C8H15NO2)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. 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. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Electric Literature of C8H15NO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Influence of pH on the action of parasmypathomimetic drugs》 were Luellmann, Heinz; Peters, Thies. And the article was published in European Journal of Pharmacology in 1967. Product Details of 1690-72-8 The author mentioned the following in the article:

The influence of pH on the activity of parasympathomimetics with a tertiary N was investigated using guinea pig isolated atria and ileum segments. Carbachol and arecaidine ester methiodide, both quaternary cholinomimetics, were used as reference compounds The responses of the organs were unchanged within the pH ranges 6.2-8.4 (ileum) and 6.3-8.8 (atria). The pK values of the tertiary parasympathomimetics investigated also lay within these ranges. The tertiary parasympathomimetics had agonist activity only in the protonated form. The slope of the concentration-response curves was reduced for both tertiary and quaternary parasympathomimetics as the OH- concentration was increased. In contrast to the behavior of the quaternary compounds, the intrinsic activity of the tertiary parasympathomimetics increased when OH- concentration was raised. The intrinsic activity of the tertiary compounds may be even higher than that of the quaternary compounds The pH of the medium not only determined the degree of protonation of the tertiary agonists, but also influenced the slope of the concentration-response curves and the intrinsic activity. In the experimental materials used by the author, we found Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Product Details of 1690-72-8)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Product Details of 1690-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Diffusion of reduced arecoline and arecaidine through human vaginal and buccal mucosa》 was written by Van der Bijl, P.; Van Eyk, A. D.; Van Wyk, C. W.; Stander, I. A.. Category: piperidines And the article was included in Journal of Oral Pathology & Medicine on April 30 ,2001. The article conveys some information:

Because alkaloids from areca nut, arecoline and arecaidine, have been implicated in the development of oral submucous fibrosis, the authors determined their diffusion kinetics through human buccal and vaginal mucosa. Four clin. healthy vaginal mucosa specimens (mean patient age ± standard deviation: 47±15 yr; age range: 31-60 yr) and 4 buccal mucosa specimens from 2 male patients and 2 female patients (mean patient age ± standard deviation: 31±9 yr; age range: 17-53 yr) were obtained during surgery. In vitro flux rates of reduced arecoline and arecaidine (r-arecoline and r-arecaidine) were determined by use of a flow-through diffusion apparatus Anal. of variance, a Duncan multiple range test, and an unpaired t-test were used to determine steady state kinetics and flux differences over time intervals. Although statistically significant differences were observed between flux values for both alkaloids and tissues at certain time points, these were not considered to be of biol. (clin.) significance. However, the flux rates across both mucosa of r-arecoline were significantly higher statistically than those of r-arecaidine. The findings demonstrated the differences in the diffusion kinetics between r-arecoline and r-arecaidine across human buccal and vaginal mucosa, an observation that could be explained in terms of their ionization characteristics. Addnl., the results obtained further support the hypothesis that human vaginal mucosa can be used as a model for buccal mucosa in studies of permeability to various chem. compounds The results came from multiple reactions, including the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Category: piperidines)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Diffusion of reduced arecoline and arecaidine through human vaginal and buccal mucosa》 was written by Van der Bijl, P.; Van Eyk, A. D.; Van Wyk, C. W.; Stander, I. A.. Category: piperidines And the article was included in Journal of Oral Pathology & Medicine on April 30 ,2001. The article conveys some information:

Because alkaloids from areca nut, arecoline and arecaidine, have been implicated in the development of oral submucous fibrosis, the authors determined their diffusion kinetics through human buccal and vaginal mucosa. Four clin. healthy vaginal mucosa specimens (mean patient age ± standard deviation: 47±15 yr; age range: 31-60 yr) and 4 buccal mucosa specimens from 2 male patients and 2 female patients (mean patient age ± standard deviation: 31±9 yr; age range: 17-53 yr) were obtained during surgery. In vitro flux rates of reduced arecoline and arecaidine (r-arecoline and r-arecaidine) were determined by use of a flow-through diffusion apparatus Anal. of variance, a Duncan multiple range test, and an unpaired t-test were used to determine steady state kinetics and flux differences over time intervals. Although statistically significant differences were observed between flux values for both alkaloids and tissues at certain time points, these were not considered to be of biol. (clin.) significance. However, the flux rates across both mucosa of r-arecoline were significantly higher statistically than those of r-arecaidine. The findings demonstrated the differences in the diffusion kinetics between r-arecoline and r-arecaidine across human buccal and vaginal mucosa, an observation that could be explained in terms of their ionization characteristics. Addnl., the results obtained further support the hypothesis that human vaginal mucosa can be used as a model for buccal mucosa in studies of permeability to various chem. compounds The results came from multiple reactions, including the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Category: piperidines)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem