Zobrazeno 1 - 10 of 10 pro vyhledávání: '"Richard G. W. Proudman"'
1
Akademický článek
The signaling and selectivity of α‐adrenoceptor agonists for the human α2A, α2B and α2C‐adrenoceptors and comparison with human α1 and β‐adrenoceptors
Autor: Richard G. W. Proudman, Juliana Akinaga, Jillian G. Baker
Publikováno v: Pharmacology Research & Perspectives, Vol 10, Iss 5, Pp n/a-n/a (2022)
Abstract α2‐adrenoceptors, (α2A, α2B and α2C‐subtypes), are Gi‐coupled receptors. Central activation of brain α2A and α2C‐adrenoceptors is the main site for α2‐agonist mediated clinical responses in hypertension, ADHD, muscle spasm a
Externí odkaz: https://doaj.org/article/62f574fc49f84753a64d6f5b7905307a
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2
Akademický článek
The selectivity of α‐adrenoceptor agonists for the human α1A, α1B, and α1D‐adrenoceptors
Autor: Richard G. W. Proudman, Jillian G. Baker
Publikováno v: Pharmacology Research & Perspectives, Vol 9, Iss 4, Pp n/a-n/a (2021)
Abstract Highly selective drugs offer a way to minimize side‐effects. For agonist ligands, this could be through highly selective affinity or highly selective efficacy, but this requires careful measurements of intrinsic efficacy. The α1‐adrenoc
Externí odkaz: https://doaj.org/article/7a84ce3fee584887aa48f7f483492269
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3
Akademický článek
The affinity and selectivity of α‐adrenoceptor antagonists, antidepressants, and antipsychotics for the human α1A, α1B, and α1D‐adrenoceptors
Autor: Richard G. W. Proudman, Andre S. Pupo, Jillian G. Baker
Publikováno v: Pharmacology Research & Perspectives, Vol 8, Iss 4, Pp n/a-n/a (2020)
Abstract α1‐adrenoceptor antagonists are widely used for hypertension (eg, doxazosin) and benign prostatic hypertrophy (BPH, eg, tamsulosin). Some antidepressants and antipsychotics have been reported to have α1 affinity. This study examined 101
Externí odkaz: https://doaj.org/article/510f385e83cc4e3dba11141b3a79376c
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5
Akademický článek
Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor.
Autor: Jillian G Baker, Richard G W Proudman, Stephen J Hill
Publikováno v: PLoS ONE, Vol 8, Iss 11, p e77582 (2013)
β-blockers are widely used to improve symptoms and prolong life in heart disease primarily by inhibiting the actions of endogenous catecholamines at the β1-adrenoceptor. There are two common naturally occurring polymorphisms within the human β1-ad
Externí odkaz: https://doaj.org/article/f6380be59a3f44898054a21246513f9f
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6
The pharmacological effects of the thermostabilising (m23) mutations and intra and extracellular (β36) deletions essential for crystallisation of the turkey β-adrenoceptor
Autor: Richard G. W. Proudman, Jillian G. Baker, Christopher G. Tate
Publikováno v: Naunyn-Schmiedeberg's Archives of Pharmacology
The X-ray crystal structure of the turkey β-adrenoceptor has recently been determined. However, mutations were introduced into the native receptor that was essential for structure determination. These may cause alterations to the receptor pharmacolo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::765a88cacab310058a4b2ecc796e116a
http://europepmc.org/articles/PMC3116118
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7
Role of Key Transmembrane Residues in Agonist and Antagonist Actions at the Two Conformations of the Human β1-Adrenoceptor
Autor: Richard G. W. Proudman, Stephen J. Hill, Jillian G. Baker, Peter Fischer, Nicola C. Hawley
Publikováno v: Molecular Pharmacology. 74:1246-1260
Studies with 4-[3-[(1,1-dimethylethyl)amino]2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one hydrochloride (CGP 12177) at the human beta1-adrenoceptor have provided evidence for two binding modes or conformations that have markedly different pharm
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc2778ab2f39ae74442be8a945613c45
https://doi.org/10.1124/mol.108.048371
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8
Salmeterol's extreme β2 selectivity is due to residues in both extracellular loops and transmembrane domains
Autor: Stephen J. Hill, Jillian G. Baker, Richard G. W. Proudman
Publikováno v: Molecular pharmacology. 87(1)
Salmeterol is a long-acting β2-agonist, widely used as an inhaled treatment of asthma and chronic obstructive pulmonary disease. It has very high β2-affinity (log KD -8.95) and is very selective for the β2-adrenoceptor (1000-fold selectivity over
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::408be54b9bb1ccd8e9b5a1617abc9747
https://pubmed.ncbi.nlm.nih.gov/25324048
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9
Identification of Key Residues in Transmembrane 4 Responsible for the Secondary, Low-Affinity Conformation of the Human β1-Adrenoceptor
Autor: Richard G. W. Proudman, Stephen J. Hill, Jillian G. Baker
The β1-adrenoceptor exists in two agonist conformations/states: 1) a high-affinity state where responses to catecholamines and other agonists (e.g., cimaterol) are potently inhibited by β1-adrenoceptor antagonists, and 2) a low-affinity secondary c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b68cab50431222d73bf813b2dbb965fd
https://europepmc.org/articles/PMC4132118/
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10
Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor
Autor: Richard G. W. Proudman, Stephen J. Hill, Jillian G. Baker
Publikováno v: PLoS ONE
PLoS ONE, Vol 8, Iss 11, p e77582 (2013)
β-blockers are widely used to improve symptoms and prolong life in heart disease primarily by inhibiting the actions of endogenous catecholamines at the β1-adrenoceptor. There are two common naturally occurring polymorphisms within the human β1-ad
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74ca7c85252abe6663f81a20d3814b3a
http://eprints.nottingham.ac.uk/2360/
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