[125I][D-Ala2]deltorphin-I: A high affinity, delta-selective opioid receptor ligand

Content Provider	Semantic Scholar
Author	Dupin, Sylvie Tafani, J. A. M. Mazarguil, Honoré Zajac, Jean-Marie
Copyright Year	1991
Abstract	The selective delta opioid agonist [D-Ala2]deltorphin-I was radioiodinated and the product purified using reverse phase HPLC. The binding characteristics and distribution profile of [125I][D-Ala2]deltorphin-I were assessed in mouse brain using homogenate binding techniques and quantitative autoradiography. [125I][D-Ala2]deltorphin-I bound with high affinity to a single class of sites (KD = 0.5 nM) in brain membrane preparations and striatal sections. Competition studies indicated that [125I][D-Ala2]deltorphin-I was selectively labeling delta opioid receptors as shown by the ratio of apparent affinities for mu and delta receptors (KI mu/KI delta = 1388). The autoradiographical distribution profile of [125I][D-Ala2]deltorphin-I binding sites was also consistent with that of other delta-selective radioligands. The data indicate that [125I][D-Ala2]deltorphin-I binds to delta opioid receptors with high affinity and selectivity. Because of its very high specific activity, it can be detected rapidly with high sensitivity by autoradiographic emulsion.
Starting Page	825
Ending Page	830
Page Count	6
File Format	PDF HTM / HTML
DOI	10.1016/0196-9781(91)90141-B
PubMed reference number	1664947
Journal	Medline
Volume Number	12
Alternate Webpage(s)	https://api.elsevier.com/content/article/pii/019697819190141B
Alternate Webpage(s)	https://www.sciencedirect.com/science/article/pii/019697819190141B?dgcid=api_sd_search-api-endpoint
Alternate Webpage(s)	https://doi.org/10.1016/0196-9781%2891%2990141-B
Journal	Peptides
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article