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Binding of Tyr-W-MIF-1 (Tyr-Pro-Trp-Gly-NH2) and related peptides to μ1 and μ2 opiate receptors
| Content Provider | Semantic Scholar |
|---|---|
| Author | Zadina, James E. Paul, Donald G. Gergen, Kerra A. Kastin, Abba J. |
| Copyright Year | 1996 |
| Abstract | Abstract Two endogenous brain peptides (Tyr-W-MIF-1 (Tyr-Pro-Trp-Gly-NH 2 ) and Tyr-MIF-1 (Tyr-Pro-Leu-Gly-NH 2 )), a cyclized analog and two fragments of Tyr-W-MIF-1, and hemorphin (Tyr-Pro-Trp-Thr) were tested for binding to μ 1 and μ 2 opiate receptors. All these peptides bound to both μ 1 and μ 2 sites in assays optimized to discriminate these subtypes of the μ opiate receptor in membranes from bovine thalamus. The cyclized analog of Tyr-W-MIF-1, previously shown to have potency near that of Tyr- d -Ala-Gly- N -MePhe-Gly-ol (DAMGO) and morphine in producing analgesia after intracerebroventricular (i.c.v.) injection, bound to μ 1 and μ 2 sites with affinities similar to those of (DAMGO). Tyr-W-MIF-1, previously shown to induce analgesia after i.c.v. injection but with much higher potency after intrathecal (i.t.) injection, also bound to both μ 1 and μ 2 sites with an affinity between that of morphiceptin and hemorphin. Although the highest ratios of K i 's for μ 2 / μ 1 were shown by hemorphin, Tyr-MIF-1, and Tyr-W-MIF-1, none of the compounds were significantly different in selectivity. The results indicate that the relatively lower potency of Tyr-W-MIF-1 after i.c.v., compared with i.t. injection, is not due to a lack of binding to μ 1 sites. They suggest that it has relatively high efficacy at μ 2 , but low efficacy at μ 1 sites, a possibility that might explain some of the novel properties of these peptides. |
| Starting Page | 65 |
| Ending Page | 69 |
| Page Count | 5 |
| File Format | PDF HTM / HTML |
| DOI | 10.1016/S0304-3940(96)12928-1 |
| Volume Number | 215 |
| Alternate Webpage(s) | https://api.elsevier.com/content/article/pii/S0304394096129281 |
| Alternate Webpage(s) | https://www.sciencedirect.com/science/article/pii/S0304394096129281?dgcid=api_sd_search-api-endpoint |
| Alternate Webpage(s) | https://doi.org/10.1016/S0304-3940%2896%2912928-1 |
| Journal | Neuroscience Letters |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
