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Mutations of Cys-17 and Ala-271 in the Human Histamine H₂
Receptor Determine the Species Selectivity of Guanidine-Type Agonists and Increase Constitutive Activity

Preuss, Hendrik and Ghorai, Prasanta and Kraus, Anja and Dove, Stefan and Buschauer, Armin and Seifert, Roland (2007) Mutations of Cys-17 and Ala-271 in the Human Histamine H₂
Receptor Determine the Species Selectivity of Guanidine-Type Agonists and Increase Constitutive Activity.
Journal of Pharmacology and Experimental Therapeutics 321 (3), pp. 975-982.

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Abstract

In a steady-state GTPase activity assay, N-[3-(1H-imidazol-4-yl)propyl)]guanidines and N(G)-acylated derivatives are more potent and efficacious at fusion proteins of guinea pig (gpH₂R-GsαS) than human (hH₂R-GsαS) histamine H₂ receptor, coupled to the short splice variant of Gsα, GsαS. Whereas Ala-271 (hH₂R) and Asp-271 (gpH₂R) in transmembrane domain 7 were identified to determine the potency ...

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Item Type:Article
Date:March 2007
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann formerly Prof. Seifert)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1124/jpet.107.120519DOI
Subjects:500 Science > 570 Life sciences
600 Technology > 610 Medical sciences Medicine
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Armin Buschauer
Deposited On:28 Jan 2008 15:09
Last Modified:13 Mar 2014 10:20
Item ID:2671
Owner Only: item control page

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