Call us toll-free

Synthesis of Allene Substituted Nipecotic Acids by ..

1-Boc-L-nipecotic acid is used as an organic chemical synthesis intermediate

Approximate price

Pages:

275 Words

$19,50

Amino Acid supplement, dosage, side effect, essential …

Francesco Paolo Bonina; Loredana Arenare; Francesco Palagiano; Antonella Saija; Felice Nava; Domenico Trombetta; Paolo De Caprariis. Synthesis, stability and pharmacological evaluation of nipecotic acid prodrugs. Journal of Pharmaceutical Sciences. 1999, 88, (5),561-567

Synthesis, stability and pharmacological evaluation of nipecotic acid prodrugs.

AB - BACKGROUND:: Many general anesthetics are thought to produce a loss of wakefulness, in part, by enhancing γ-aminobutyric acid (GABA) neurotransmission. However, GABAergic neurotransmission in the pontine reticular formation promotes wakefulness. This study tested the hypotheses that (1) relative to wakefulness, isoflurane decreases GABA levels in the pontine reticular formation; and (2) pontine reticular formation administration of drugs that increase or decrease GABA levels increases or decreases, respectively, isoflurane induction time. METHODS:: To test hypothesis 1, cats (n = 5) received a craniotomy and permanent electrodes for recording the electroencephalogram and electromyogram. Dialysis samples were collected from the pontine reticular formation during isoflurane anesthesia and wakefulness. GABA levels were quantified using high-performance liquid chromatography. For hypothesis 2, rats (n = 10) were implanted with a guide cannula aimed for the pontine reticular formation. Each rat received microinjections of Ringer's (vehicle control), the GABA uptake inhibitor nipecotic acid, and the GABA synthesis inhibitor 3-mercaptopropionic acid. Rats were then anesthetized with isoflurane, and induction time was quantified as loss of righting reflex. Breathing rate was also measured. RESULTS:: Relative to wakefulness, GABA levels were significantly decreased by isoflurane. Increased power in the electroencephalogram and decreased activity in the electromyogram caused by isoflurane covaried with pontine reticular formation GABA levels. Nipecotic acid and 3-mercaptopropionic acid significantly increased and decreased, respectively, isoflurane induction time. Nipecotic acid also increased breathing rate. CONCLUSION:: Decreasing pontine reticular formation GABA levels comprises one mechanism by which isoflurane causes loss of consciousness, altered cortical excitability, muscular hypotonia, and decreased respiratory rate.

Infine Chemicals Co., Limited.--Infine|Infine Chemicals

59-67-6|64-17-5 Synthesising nipecotic acid | 498-95-3 Synthesis Route, Search nipecotic acid Synthesis route and MSDS, CAS 498-95-3 Synthesis …

The relative reactivities of several secondary amines serving as hydride donors in propargylic amines undergoing a [1,5]-hydride transfer reaction to yield the respective terminal and 1,3-disubstituted allenes were studied. For this study, a two-step procedure was employed. At first, the synthesis of propargylic amines via the CuI-catalyzed aldehyde-alkyne-amine reactions (A3 coupling) was accomplished. The obtained propargylic amines were subsequently transformed to the desired allenes under CdI2 or ZnI2 catalysis. As a result, among the various secondary amines employed, differing in steric bulk, electronic nature, and conformational properties, allyl(-butyl)amine was found to be the best hydride donor for the synthesis of terminal allenes. For the synthesis of 1,3-disubstituted allenes, the propyne derivatives containing either a allyl(-butyl)amine or a 1,2,3,6-tetrahydropyridine unit in propargylic position performed best. Finally, with the developed procedure, nipecotic acid derivatives containing an -allenyl substituent were synthesized with good yields using either ZnI2 as catalyst for the preparation of 1-substituted or CdI2 for the synthesis of 1,3-disubstitued allenes.

N2 - BACKGROUND:: Many general anesthetics are thought to produce a loss of wakefulness, in part, by enhancing γ-aminobutyric acid (GABA) neurotransmission. However, GABAergic neurotransmission in the pontine reticular formation promotes wakefulness. This study tested the hypotheses that (1) relative to wakefulness, isoflurane decreases GABA levels in the pontine reticular formation; and (2) pontine reticular formation administration of drugs that increase or decrease GABA levels increases or decreases, respectively, isoflurane induction time. METHODS:: To test hypothesis 1, cats (n = 5) received a craniotomy and permanent electrodes for recording the electroencephalogram and electromyogram. Dialysis samples were collected from the pontine reticular formation during isoflurane anesthesia and wakefulness. GABA levels were quantified using high-performance liquid chromatography. For hypothesis 2, rats (n = 10) were implanted with a guide cannula aimed for the pontine reticular formation. Each rat received microinjections of Ringer's (vehicle control), the GABA uptake inhibitor nipecotic acid, and the GABA synthesis inhibitor 3-mercaptopropionic acid. Rats were then anesthetized with isoflurane, and induction time was quantified as loss of righting reflex. Breathing rate was also measured. RESULTS:: Relative to wakefulness, GABA levels were significantly decreased by isoflurane. Increased power in the electroencephalogram and decreased activity in the electromyogram caused by isoflurane covaried with pontine reticular formation GABA levels. Nipecotic acid and 3-mercaptopropionic acid significantly increased and decreased, respectively, isoflurane induction time. Nipecotic acid also increased breathing rate. CONCLUSION:: Decreasing pontine reticular formation GABA levels comprises one mechanism by which isoflurane causes loss of consciousness, altered cortical excitability, muscular hypotonia, and decreased respiratory rate.

Nipecotic acid Supplier | CAS 60252-41-7 | Tocris …

Each rat received microinjections of Ringer's (vehicle control), the GABA uptake inhibitor nipecotic acid, and the GABA synthesis inhibitor 3-mercaptopropionic acid.

Francesco Paolo Bonina; Loredana Arenare; Francesco Palagiano; Antonella Saija; Felice Nava; Domenico Trombetta; Paolo De Caprariis. Synthesis, stability and pharmacological evaluation of nipecotic acid prodrugs. Journal of Pharmaceutical Sciences. 1999, 88, (5),561-567

Overview of the procedures applied for the propargylic amine synthesis, additional data for the influence of the catalyst loading on the allene formation, amine reactivity study with nipecotic acid derived propargylic amines, 1H NMR experiment to investigate ZnI2 coordination to 29g, and copies of the 1H and 13C NMR spectra ()

Custom Synthesis, a Specialty. Home » Products » (R)-Boc-Nipecotic acid (R)-Boc-Nipecotic acid. Search Products. Product Name. CAS Number. Product Number. Back
Order now
  • 88495-54-9 - 1-Boc-L-nipecotic acid, 97% - Boc-Nip-OH …

    Applications : Intermediate in organic synthesis and building blocks for chemical synthesis and nipecotic acid drug.

  • 01/11/2003 · First asymmetric syn..

    Riluzole - Wikipedia

  • Development of Highly Potent GAT1 Inhibitors: Synthesis …

    Riluzole (marketed as Rilutek and Teglutik) is a drug used to treat amyotrophic lateral sclerosis

Order now

Hydrolysis of nipecotic acid phenyl esters - …

BACKGROUND:: Many general anesthetics are thought to produce a loss of wakefulness, in part, by enhancing γ-aminobutyric acid (GABA) neurotransmission. However, GABAergic neurotransmission in the pontine reticular formation promotes wakefulness. This study tested the hypotheses that (1) relative to wakefulness, isoflurane decreases GABA levels in the pontine reticular formation; and (2) pontine reticular formation administration of drugs that increase or decrease GABA levels increases or decreases, respectively, isoflurane induction time. METHODS:: To test hypothesis 1, cats (n = 5) received a craniotomy and permanent electrodes for recording the electroencephalogram and electromyogram. Dialysis samples were collected from the pontine reticular formation during isoflurane anesthesia and wakefulness. GABA levels were quantified using high-performance liquid chromatography. For hypothesis 2, rats (n = 10) were implanted with a guide cannula aimed for the pontine reticular formation. Each rat received microinjections of Ringer's (vehicle control), the GABA uptake inhibitor nipecotic acid, and the GABA synthesis inhibitor 3-mercaptopropionic acid. Rats were then anesthetized with isoflurane, and induction time was quantified as loss of righting reflex. Breathing rate was also measured. RESULTS:: Relative to wakefulness, GABA levels were significantly decreased by isoflurane. Increased power in the electroencephalogram and decreased activity in the electromyogram caused by isoflurane covaried with pontine reticular formation GABA levels. Nipecotic acid and 3-mercaptopropionic acid significantly increased and decreased, respectively, isoflurane induction time. Nipecotic acid also increased breathing rate. CONCLUSION:: Decreasing pontine reticular formation GABA levels comprises one mechanism by which isoflurane causes loss of consciousness, altered cortical excitability, muscular hypotonia, and decreased respiratory rate.

Order now
  • Kim

    "I have always been impressed by the quick turnaround and your thoroughness. Easily the most professional essay writing service on the web."

  • Paul

    "Your assistance and the first class service is much appreciated. My essay reads so well and without your help I'm sure I would have been marked down again on grammar and syntax."

  • Ellen

    "Thanks again for your excellent work with my assignments. No doubts you're true experts at what you do and very approachable."

  • Joyce

    "Very professional, cheap and friendly service. Thanks for writing two important essays for me, I wouldn't have written it myself because of the tight deadline."

  • Albert

    "Thanks for your cautious eye, attention to detail and overall superb service. Thanks to you, now I am confident that I can submit my term paper on time."

  • Mary

    "Thank you for the GREAT work you have done. Just wanted to tell that I'm very happy with my essay and will get back with more assignments soon."

Ready to tackle your homework?

Place an order