Preuss, Hendrik, Ghorai, Prasanta, Kraus, Anja, Dove, Stefan, 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: |
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| Dewey Decimal Classification: | 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 | ||||
| Item ID: | 2671 |
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