Amino receptor

PCP, like ketamine, targets a particular receptor site, located in the channel for calcium, associated with excitatory amino receptors A-methyl-D-aspartate (NMDA) located in the brain [23],... 

L-Arginine synthesis represents the primary synthesis of the amidine group other naturally occurring guanidino compounds, chiefly Phosphagens (see), are synthesized by transfer of the amidine group from l-arginine to the appropriate amino receptor. 

Fig. 18. (a) A bicycloguamdinium receptor and (b) its three-point association to the 2witterionic a-amino acid trypthophan (118). 

P-Endorphin. A peptide corresponding to the 31 C-terminal amino acids of P-LPH was first discovered in camel pituitary tissue (10). This substance is P-endorphin, which exerts a potent analgesic effect by binding to cell surface receptors in the central nervous system. The sequence of P-endorphin is well conserved across species for the first 25 N-terminal amino acids. Opiates derived from plant sources, eg, heroin, morphine, opium, etc, exert their actions by interacting with the P-endorphin receptor. On a molar basis, this peptide has approximately five times the potency of morphine. Both P-endorphin and ACTH ate cosecreted from the pituitary gland. Whereas the physiologic importance of P-endorphin release into the systemic circulation is not certain, this molecule clearly has been shown to be an important neurotransmitter within the central nervous system. Endorphin has been invaluable as a research tool, but has not been clinically useful due to the avadabihty of plant-derived opiates. 

Several human receptors for the neurohypophyseal hormones have been cloned and the sequences elucidated. The human V2 receptor for antidiuretic hormone presumably contains 371 amino acids and seven transmembrane segments and activates cycHc AMP (76). The oxytocin receptor is a classic G-protein-coupled type of receptor with a proposed membrane topography also involving seven transmembrane components (84). A schematic representation of the oxytocin receptor stmcture within the membrane is shown in Eigure 4 (85). 

Fig. 2. Schematic of the G-proteia coupled receptor (GPCR). The seven a-heUcal hydrophobic regions spanning the membrane are joined by extraceUular and iatraceUular loops. The amino terminal is located extraceUulady and the carboxy terminal iatraceUulady.

D,L-CC-amino-3-hydroxy-5-methyl-4-isoxa2ol Ionotropic glutamate receptors [77521-29-0] C7H10N2O4 (174)... 

Fig. 5. Schematic diagram of the presumed arrangement of the amino acid sequence for the 5-opioid receptor, showing seven putative transmembrane segments three intracellular loops, A three extracellular loops, B the extracellular N-terrninus and the intracellular C-terrninus, where (0) represents amino acid residues common to ] -, 5-, and K-receptors ( ), amino acid residues common to all three opioid receptors and other neuropeptide receptors and (O), other amino acids. Branches on the N-terruinal region indicate possible glycosylation sites, whereas P symbols in the C-terminal region indicate...

Use of D-amino acids in the synthesis of a hairpin loop portion from the CD4 receptor provides a stable CD4 receptor mimic, which blocks experimental allergic encephalomyelitis (144). This synthetic constmct is not simply the mirror image or enantiomer of the CD4 hairpin loop, but rather an aH-D-constmct in the reverse sequence, thus providing stereochemicaHy similar side-chain projections of the now inverted backbone (Fig. 11). This peptide mimetic, unlike its aH-L amino acid counterpart, is resistant to en2yme degradation. As one would expect, the aH-D amino acid CD4 hairpin loop, synthesi2ed in the natural direction, the enantiomer of the natural constmct, is inactive. 

Fig. 11. Use of D-amino acids in the synthesis of a hairpin loop portion from the CD4 receptor (a) all L-Ser—Lys—Ala tripeptide constmcted in the natural...

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