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Sunday, August 22, 2021

8-22-2021-0311 - Pharmaceuticals Wiki Glutamate Glycine Related RIVS

 Agonist Glutamate

Neboglamine (INN) (developmental code names CR-2249XY-2401), formerly known as nebostinel, is a positive allosteric modulator of the glycine site of the NMDA receptor which is under investigation for Rottapharm for the treatment of schizophrenia and cocaine dependence.[1][2][3][4][5][6] It shows cognition- and memory-enhancing effects in animal models.[7][8][9] As of June 2015, it is in phase IIclinical trials for both schizophrenia and cocaine abuse.[10]

https://en.wikipedia.org/wiki/Neboglamine

Spermidine is a polyamine compound (C
7
H
19
N
3
) found in ribosomes and living tissues, and having various metabolic functions within organisms. It was originally isolated from semen.[1]

https://en.wikipedia.org/wiki/Spermidine

Tetrazolylglycine (Tet-GlyLY-285,265) is a potent and selective NMDA receptoragonist, stimulating the NMDA receptor with higher potency than either glutamate or NMDA.[1] It is a potent convulsant and excitotoxin and is used in scientific research.[2][3]

https://en.wikipedia.org/wiki/Tetrazolylglycine

Proline (symbol Pro or P)[5] is an organic acid classed as a proteinogenic amino acid (used in the biosynthesis of proteins), although it does not contain the amino group -NH
2
 but is rather a secondary amine. The secondary amine nitrogen is in the protonated NH2+ form under biological conditions, while the carboxy group is in the deprotonated −COO form. The "side chain" from the α carbon connects to the nitrogen forming a pyrrolidine loop, classifying it as a aliphatic amino acid. It is non-essential in humans, meaning the body can synthesize it from the non-essential amino acid L-glutamate. It is encoded by all the codons starting with CC (CCU, CCC, CCA, and CCG).

Proline is the only proteinogenic secondary amino acid which is a secondary amine, as the nitrogen atom is attached both to the α-carbon and to a chain of three carbons that together form a five-membered ring.


https://en.wikipedia.org/wiki/Proline

Homoquinolinic acid (HQA) is a potent excitotoxin[1] which is a conformationally-restricted analogue of N-methyl-D-aspartate (NMDA) and a partial agonist of the main/glutamate site of the NMDA receptor, with some selectivity for NR2B subunit-containing receptors.[2][3][4] It is approximately equipotent to NMDA and about five times more potent than quinolinic acid as an agonist of the NMDA receptor.[5] HQA has also been found to label a novel, yet uncharacterized binding site, which can be distinguished from the NMDA receptor with the use of 2-carboxy-3-carboxymethylquinoline (CCMQ), a selective ligand of the uncharacterized site.[6]

See also[edit]

https://en.wikipedia.org/wiki/Homoquinolinic_acid

Desflurane (1,2,2,2-tetrafluoroethyl difluoromethyl ether) is a highly fluorinated methyl ethyl ether used for maintenance of general anesthesia. Like halothaneenflurane, and isoflurane, it is a racemic mixture of (R) and (S) optical isomers (enantiomers). Together with sevoflurane, it is gradually replacing isoflurane for human use, except in economically undeveloped areas, where its high cost precludes its use. It has the most rapid onset and offset of the volatile anestheticdrugs used for general anesthesia due to its low solubility in blood.

Some drawbacks of desflurane are its low potency, its pungency and its high cost (though at low flow fresh gas rates, the cost difference between desflurane and isoflurane appears to be insignificant[1]). It may cause tachycardia and airway irritability when administered at concentrations greater than 10 vol%. Due to this airway irritability, desflurane is infrequently used to induce anesthesia via inhalation techniques.

Though it vaporises very readily, it is a liquid at room temperature. Anaesthetic machines are fitted with a specialized anaesthetic vaporiser unit that heats liquid desflurane to a constant temperature. This enables the agent to be available at a constant vapor pressure, negating the effects fluctuating ambient temperatures would otherwise have on its concentration imparted into the fresh gas flow of the anesthesia machine.

Desflurane, along with enflurane and to a lesser extent isoflurane, has been shown to react with the carbon dioxide absorbent in anesthesia circuits to produce detectable levels of carbon monoxide through degradation of the anesthetic agent. The CO
2
 absorbent Baralyme, when dried, is most culpable for the production of carbon monoxide from desflurane degradation, although it is also seen with soda lime absorbent as well. Dry conditions in the carbon dioxide absorbent are conducive to this phenomenon, such as those resulting from high fresh gas flows.[2]

https://en.wikipedia.org/wiki/Desflurane


Toluene (/ˈtɒljun/), also known as toluol (/ˈtɒljuɒl/), is an aromatic hydrocarbon. It is a colorless, water-insoluble liquid with the smell associated with paint thinners. It is a mono-substituted benzene derivative, consisting of a methyl group (CH₃) attached to a phenyl group. As such, its systematic IUPAC name is methylbenzene. Toluene is predominantly used as an industrial feedstock and a solvent.

As the solvent in some types of paint thinnerpermanent markerscontact cementand certain types of glue, toluene is sometimes used as a recreational inhalant[7] and has the potential of causing severe neurological harm.[8][9]

https://en.wikipedia.org/wiki/Toluene

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