Sökning: "agonist selectivity"

Visar resultat 1 - 5 av 18 avhandlingar innehållade orden agonist selectivity.

1. 1. Muscarinic receptors and urinary bladder selectivity : Properties that determine the organ selectivity of compounds

   Författare :Staffan Sundquist; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical biosciences; bladder; muscarinic; receptor subtypes; smooth muscle; multivariate; Farmaceutisk biovetenskap; Biopharmacy; Biofarmaci; galenisk farmaci; Pharmaceutics;

   Sammanfattning : Urinary bladder contraction is mainly mediated by activation of muscarinic acetylcholine receptors (mAChR). Muscarinic antagonists are often effective in treatment of unstable bladder. The effectiveness of this treatment has often been limited by side effects as dry mouth. LÄS MER

3. 2. Selectivity of dopamine D1 and D2 receptor agonists – A combined computational approach

   Författare :Marcus Malo; Göteborgs universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; dopamine; agonists; GPCRs; pharmacophore modeling; protein structure modeling; agonist selectivity;

   Sammanfattning : Dopamine (DA) is an endogenous neurotransmitter acting in the central nervous system. DA plays a key role in many vital brain functions such as behavior, cognition, motor activity, learning, and reward. Dopamine receptors belong to the rhodopsin like family of G-protein coupled receptors (GPCRs). LÄS MER

4. 3. Modulation of Receptor Signaling and Functional Selectivity in Neutrophils

   Författare :Michael Gabl; Göteborgs universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; neutrophils; G-protein coupled receptors; reactive oxygen species; ligands; functional selectivity; allosteric modulation;

   Sammanfattning : Neutrophils are important effector cells of the innate immune system and in the regulation of inflammation. Many of their functions, such as chemotactic migration, secretion of granule constituents and activation of the oxygen radical-producing NADPH-oxidase, are regulated by cell surface receptors. LÄS MER

5. 4. Design, Synthesis and Biological Evaluation of Selective Nonpeptide AT2 Receptor Agonists and Antagonists

   Författare :Charlotta Wallinder; Anders Hallberg; Mathias Alterman; Anders Karlén; Elizabeth E. Sugg; Uppsala universitet; []
   Nyckelord :AT2 receptor agonist; AT2 receptor antagonist; Ang II peptidomimetics;

   Sammanfattning : The G protein-coupled receptors (GPCRs) are important targets in drug discovery. In several cases, the endogenous ligands that activate the GPCRs of pharmaceutical interest are peptides. LÄS MER

7. 5. Design and Synthesis of Novel AT2 Receptor Ligands : From Peptides to Drug-Like Molecules

   Författare :Jennie Georgsson; Anders Hallberg; Kevin Burgess; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; angiotensin II; AT1; AT2; AT2 receptor agonist; peptidomimetics; γ-turn mimetics; carbonylation; microwave; molybdenum hexacarbonyl; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi;

   Sammanfattning : Many peptide receptors are of pharmaceutical interest and there is thus a need for new ligands for such receptors. Unfortunately, peptides are not suitable as orally administrated drugs since they are associated with poor absorption, rapid metabolism and low sub-receptor selectivity. LÄS MER