Recent evidence suggests that highly selective m-opioid ago-nists may provide good analgesia with less development of tolerance and dependence. H-Tyr-D-Arg-Phe-Lys-NH2 (DALDA) and H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt 1]DALDA) were found to display high binding affinity and much greater selec-tivity for the m-opioid receptor (Ki d/Ki m. 10,000) compared with H-Tyr-D-Ala-Gly-MePhe-Gly-ol (DAMGO). In addition, [Dmt1]DALDA was 3000-fold more potent than morphine when administered intrathecally. A potential problem with peptide analogs as therapeutic agents is their susceptibility to enzy-matic degradation in vivo and short elimination half-lives. In thi
Opioid receptors play the pain control function in the body. Most of the research is carried out to ...
A new series of 12 dermorphin tetrapeptides, W-Tyr-D-MetO-Phe-Xaa-Y (W = H, H2NC = (NH); Xaa = Gly, ...
Opioid receptors are important targets for the treatment of pain and potentially for other disease s...
In this study the μ opioid receptor (MOR) ligands DALDA (Tyr-d-Arg-Phe-Lys-NH2) and Dmt1-DALDA (Dmt-...
Three dimethyl-L-tyrosine (Dmt) based peptide analogues were identified in a previous study as excel...
[Dmt1]DALDA (H-Dmt-D-Arg-Phe-Lys-NH2; Dmt 2,6-di-methyltyrosine) binds with high affinity and selec...
Most naturally occurring opioid peptides, such as the endomorphins, are not highly selective for a s...
The influence of the side chain charges of the second and fourth amino acid residues in the peptidic...
The influence of the side chain charges of the second and fourth amino acid residues in the peptidic...
Most naturally occurring opioid peptides, such as the endomorphins, are not highly selective for a s...
In this study the μ opioid receptor (MOR) ligands DALDA (Tyr-d-Arg-Phe-Lys-NH<sub>2</sub>) and Dmt<s...
Acute and chronic pain present major medical problems worldwide, having negative impacts on human he...
Morphine and related drugs, which are the most effective analgesics for the relief of severe pain, a...
The single amino acid replacement of 2',6'-dimethyl-L-tyrosine in deltorphin B (H-Dmt-D-Ala-Phe-Glu-...
Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesir...
Opioid receptors play the pain control function in the body. Most of the research is carried out to ...
A new series of 12 dermorphin tetrapeptides, W-Tyr-D-MetO-Phe-Xaa-Y (W = H, H2NC = (NH); Xaa = Gly, ...
Opioid receptors are important targets for the treatment of pain and potentially for other disease s...
In this study the μ opioid receptor (MOR) ligands DALDA (Tyr-d-Arg-Phe-Lys-NH2) and Dmt1-DALDA (Dmt-...
Three dimethyl-L-tyrosine (Dmt) based peptide analogues were identified in a previous study as excel...
[Dmt1]DALDA (H-Dmt-D-Arg-Phe-Lys-NH2; Dmt 2,6-di-methyltyrosine) binds with high affinity and selec...
Most naturally occurring opioid peptides, such as the endomorphins, are not highly selective for a s...
The influence of the side chain charges of the second and fourth amino acid residues in the peptidic...
The influence of the side chain charges of the second and fourth amino acid residues in the peptidic...
Most naturally occurring opioid peptides, such as the endomorphins, are not highly selective for a s...
In this study the μ opioid receptor (MOR) ligands DALDA (Tyr-d-Arg-Phe-Lys-NH<sub>2</sub>) and Dmt<s...
Acute and chronic pain present major medical problems worldwide, having negative impacts on human he...
Morphine and related drugs, which are the most effective analgesics for the relief of severe pain, a...
The single amino acid replacement of 2',6'-dimethyl-L-tyrosine in deltorphin B (H-Dmt-D-Ala-Phe-Glu-...
Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesir...
Opioid receptors play the pain control function in the body. Most of the research is carried out to ...
A new series of 12 dermorphin tetrapeptides, W-Tyr-D-MetO-Phe-Xaa-Y (W = H, H2NC = (NH); Xaa = Gly, ...
Opioid receptors are important targets for the treatment of pain and potentially for other disease s...