TIPP[ψ], a highly selective δ ligand Journal Article
| Authors: | Visconti, L. M.; Standifer, K. M.; Schiller, P. W.; Pasternak, G. W. |
| Article Title: | TIPP[ψ], a highly selective δ ligand |
| Abstract: | TIPP[ψ] is a new δ-selective opioid peptide antagonist. In the current study, we have explored its selectivity against the μ and κ receptor subtypes. Against [3H]DPDPE binding, TIPP[ψ] is quite potent, with a Ki value of < 1 nM, confirming its potent activity at δ receptors. In contrast, its Ki values against μ1, μ2, κ1, κ2 and κ3 binding sites are all >5 μM. DPDPE also is δ-selective. It labels δ sites >25-fold more potently than μ1 receptors and is even more selective against the other subtypes. However, this selectivity does not compare to the δ μ1 selectivity of TIPP[ψ] which exceeds 15,000. This far higher selectivity, coupled with its antagonist properties, gives TIPP[ψ] a number of advantages over previously reported δ-selective compounds. We have utilized these advantages to develop an improved μ1 binding assay using TIPP[ψ]. © 1994. |
| Keywords: | controlled study; unclassified drug; nonhuman; comparative study; animal; animal tissue; drug selectivity; newborn; ligands; cattle; morphine; oligopeptides; ligand binding; mu opiate receptor; receptors, opioid, mu; naloxone; corpus striatum; enkephalin[2,5 dextro penicillamine]; delta opiate receptor; receptor subtype; binding, competitive; opiate antagonist; receptors, opioid, delta; 3,4 dichloro n methyl n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate; thalamus; kappa opiate receptor; enkephalin[2 dextro alanine 4 methylphenylalanine 5 glycine]; narcotic antagonists; opiate agonist; guinea pigs; brain homogenate; priority journal; article; diprenorphine; receptors, opioid, kappa; beta endorphin; support, u.s. gov't, p.h.s.; enkephalins; enkephalin[2 dextro alanine 5 dextro leucine]; enkephalin, d-penicillamine (2,5)-; deltorphin[2 dextro alanine 4 glutamic acid]; opaite receptor; δ antagonist; μ1 receptor; leucine enkephalin[2 dextro serine 6 threonine]; tipp |
| Journal Title: | Neuroscience Letters |
| Volume: | 181 |
| Issue: | 1-2 |
| ISSN: | 0304-3940 |
| Publisher: | Elsevier Science, Inc. |
| Date Published: | 1994-11-07 |
| Start Page: | 47 |
| End Page: | 49 |
| Language: | English |
| DOI: | 10.1016/0304-3940(94)90557-6 |
| PROVIDER: | scopus |
| PUBMED: | 7898768 |
| DOI/URL: | |
| Notes: | Export Date: 14 January 2019 -- Article -- CODEN: NELED C2 -- Source: Scopus |
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