Qualitative and quantitative assessment of relative agonist efficacy
A Christopoulos, EE El-Fakahany - Biochemical pharmacology, 1999 - Elsevier
Historically, the ability of a ligand to bind to its receptor and the ability to subsequently
activate that receptor have been described as the properties of affinity and intrinsic efficacy …
activate that receptor have been described as the properties of affinity and intrinsic efficacy …
The fall and rise of pharmacology–(Re-) defining the discipline?
RJ Winquist, K Mullane, M Williams - Biochemical Pharmacology, 2014 - Elsevier
Pharmacology is an integrative discipline that originated from activities, now nearly 7000
years old, to identify therapeutics from natural product sources. Research in the 19th …
years old, to identify therapeutics from natural product sources. Research in the 19th …
Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors
T Disingrini, M Muth, C Dallanoce… - Journal of medicinal …, 2006 - ACS Publications
A novel series of muscarinic receptor ligands of the hexamethonio-type was prepared which
contained, on one side, the phthalimidopropane or 1, 8-naphthalimido-2, 2-dimethylpropane …
contained, on one side, the phthalimidopropane or 1, 8-naphthalimido-2, 2-dimethylpropane …
The classification of receptors for adenosine and adenine nucleotides
G Burnstock, NJ Buckley - Methods used in adenosine research, 1985 - Springer
Adenosine and adenine nucleotides exert potent extracellular actions on a wide range of
physiological systems, including the nervous, cardiovascular, gastrointestinal, urogenital …
physiological systems, including the nervous, cardiovascular, gastrointestinal, urogenital …
Interactions of agonists with M2 and M4 muscarinic receptor subtypes mediating cyclic AMP inhibition.
M McKinney, JH Miller, VA Gibson, L Nickelson… - Molecular …, 1991 - ASPET
In this study the similarities and differences between the M2 and M4 subtypes in their
recognition of agonists were explored. A CHO-K1 cell line transfected with the human m2 …
recognition of agonists were explored. A CHO-K1 cell line transfected with the human m2 …
The quantification of relative efficacy of agonists
TP Kenakin - Journal of pharmacological methods, 1985 - Elsevier
While much pharmacological effort has been expended in the measurement, quantification,
and comparison of agonist affinity for the classification of drugs and drug receptors …
and comparison of agonist affinity for the classification of drugs and drug receptors …
β-Adrenoceptor blocking agents as partial agonists in isolated heart muscle: Dissociation of stimulation and blockade
AJ Kaumann, JR Blinks - Naunyn-Schmiedeberg's archives of …, 1980 - Springer
The cardiac stimulant actions of nine β-adrenoceptor blocking agents were examined in
kitten papillary muscles and in isolated atria of kittens and guinea pigs to determine to what …
kitten papillary muscles and in isolated atria of kittens and guinea pigs to determine to what …
An analysis of functional antagonism and synergism.
D Mackay - British journal of pharmacology, 1981 - ncbi.nlm.nih.gov
Abstract 1 A method is described for deriving null equations for functional antagonism and
synergism. These null equations relate together the concentrations of agonist required to …
synergism. These null equations relate together the concentrations of agonist required to …
New analogues of oxotremorine and oxotremorine-M: estimation of their in vitro affinity and efficacy at muscarinic receptor subtypes
E Barocelli, V Ballabeni, S Bertoni, C Dallanoce… - Life Sciences, 2000 - Elsevier
Two subsets of tertiary amines (1a-6a) and methiodides (1b-6b) with a structural
resemblance to oxotremorine and oxotremorine-M were tested at rabbit vas deferens (M1) …
resemblance to oxotremorine and oxotremorine-M were tested at rabbit vas deferens (M1) …
The mathematics of drug-receptor interactions
D Mackay - Journal of Pharmacy and Pharmacology, 1966 - academic.oup.com
MOST pharmacological observations support the hypothesis that drugs produce their effects
by interacting in a specific way with some component of the living cell. This component …
by interacting in a specific way with some component of the living cell. This component …