Pharmacological characterization of the vesamicol analogue (+)-[(125)I]MIBT in primate brain

Autor:	J K, Staley, D C, Mash, S M, Parsons, A B, Khare, S M, Efange
Rok vydání:	1998
Předmět:	Brain Chemistry Male Iodobenzenes Vesicular Acetylcholine Transport Proteins Vesicular Transport Proteins Membrane Transport Proteins Ligands Macaca mulatta Acetylcholine Neostriatum Radioligand Assay Piperidines Neuromuscular Depolarizing Agents Animals Synaptic Vesicles Carrier Proteins
Zdroj:	European journal of pharmacology. 338(2)
ISSN:	0014-2999
Popis:	The vesamicol analogue, meta-[(125)I]iodobenzyltrozamicol [(+)-[(125)I]MIBT] was evaluated as a probe for the in vitro labeling of the vesicular acetylcholine transporter in primate brain. In the striatum, (+)-[(125)I]MIBT bound a single high-affinity site with a Kd value of 4.4 +/- 0.7 nM. Competition for (+)-[(125)I]MIBT binding to the striatum by a group of vesamicol analogues displayed a pharmacological profile similar to the rank order of potency previously observed for the vesicular acetylcholine transporter on Torpedo synaptic vesicles. High-affinity binding of (+)-[(125)I]MIBT in the occipital cortex was characterized by a Kd value of 4.6 +/- 1.1 nM. However, the rank order of potency for inhibition of (+)-[(125)I]MIBT binding to the occipital cortex by the same test compounds differed from that observed in the striatum. The results suggest that (+)-[(125)I]MIBT is a reliable probe of the vesicular acetylcholine transporter in primate striatum, but its binding in primate occipital cortex is more complex.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::cc6e88a378c2eba2017ffd190f9b5cb1 https://pubmed.ncbi.nlm.nih.gov/9455998 Zobrazit plný text záznamu Full Text from ScienceDirect