These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


PUBMED FOR HANDHELDS

Search MEDLINE/PubMed


  • Title: NS-49, a novel alpha 1a-adrenoceptor-selective agonist characterization using recombinant human alpha 1-adrenoceptors.
    Author: Obika K, Shibata K, Horie K, Foglar R, Kimura K, Tsujimoto G.
    Journal: Eur J Pharmacol; 1995 Nov 30; 291(3):327-34. PubMed ID: 8719417.
    Abstract:
    alpha 1-Adrenoreceptors comprise a heterogeneous family and subtype-selective ligands are valuable in studying the functional role of each receptor subtype. Using the Chinese hamster ovary (CHO) cells stably expressing the cloned human alpha 1-adrenoceptor subtypes (alpha 1a, alpha 1b, and alpha 1d)1, we have compared a newly synthesized phenethylamine class agonist (R)-(-)-3'-(2-amino-1-hydroxyethyl)-4'-fluoromethanesulfonanilide hydrochloride (NS-49) with imidazoline class agonist oxymetazoline in their binding affinities and intrinsic activities in causing transient increases of cytosolic Ca2+ concentrations ([Ca2+¿i response). Radioligand binding studies with 2-[beta-(4-hydroxyl-3-[125I]iodophenyl)ethylamino-methyl]tetralone ([125I]HEAT) showed NS-49 and oxymetazoline had higher affinities at alpha 1a-than at alpha 1b- and alpha 1d-subtypes (-log Ki values at alpha 1a-, alpha 1b-and alpha 1d-subtype: 6.18, 5.13, and 5.38 for NS-49: 8.19, 6.50, and 6.44 for oxymetazoline, respectively). In functional studies, both oxymetazoline and NS-49 worked as a selective and partial agonist at alpha 1a-subtype: however, NS-49 is more efficacious than oxymetazoline. NS-49 is the phenethylamine class of alpha 1-adrenoceptor partial agonist relatively selective and efficacious for the human alpha 1a-adrenoceptor subtype, NS-49 would be potentially useful for studying the physiological role of alpha 1-adrenoceptor subtype.
    [Abstract] [Full Text] [Related] [New Search]