Opiate Receptors and Opiate Antagonists in Psychiatric and Related Research A Review

摘要: The discovery of opiate receptors in the human brain sparked search for their endogenous ligands. Independently, Terenius and Wahlstrom (1975) Hughes isolated important ligands are two pentapeptides Met- Leu-enkephalin (Hughes et al.,1975) as well β-endorphin (β-lipotropin61–91). There is overwhelming evidence that glycoprotein pro-opiocortin parent substance both adrenocorticotropic hormone (ACTH) (Mains al., 1977). Enkephalins, on other hand, may have a different precursor share common with growth (Weber 1978, 1979). Kangawa al. (1979) identified new 15-residue peptide containing pig hypothalamus, termed α-neoendorphin. Thus, it appears α-neoendorphin be Leu-enkephalin. Recently, has been reported adrenal gland contains polypeptide enkephalins (Kimura 1980). Shine colleagues (1980), by employing gene cloning techniques, manipulated bacteria to produce β-endorphins. This will provide future enough β-endorphins clinical evaluations toxicity studies inexpensively. As metabolized rapid cleavage tyrosine-glycine bond, attempts protect against this led long-acting more potent analogs. In addition, receptor binding affinity, an factor determining activity these molecules, can increased enhancing lipophilicity around C-terminal amino acid.