Literature DB >> 18023486

Why the Schild method is better than Schild realised.

David Colquhoun1.   

Abstract

It is almost 60 years since Heinz Schild devised a method that allowed measurement of a genuine physical quantity, the equilibrium constant for binding of a competitive antagonist. The clever bit was that the measurements could be made using responses from tissues despite the fact that little or nothing was known about how the agonist worked. Since then, attempts have been made to generalise the Schild equation, but they are all based on false premises. It turns out that generalisation is usually not needed. His original simple result is still valid in cases where several agonist molecules must be bound to produce a response, even if the agonist binding sites interact or are not identical.

Mesh:

Substances:

Year:  2007        PMID: 18023486     DOI: 10.1016/j.tips.2007.09.011

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN: 0165-6147            Impact factor:   14.819


  23 in total

1.  Using the self-administration of apomorphine and cocaine to measure the pharmacodynamic potencies and pharmacokinetics of competitive dopamine receptor antagonists.

Authors:  Andrew B Norman; Michael R Tabet; Mantana K Norman; Vladimir L Tsibulsky
Journal:  J Neurosci Methods       Date:  2010-10-23       Impact factor: 2.390

Review 2.  On the fitting of binding data when receptor dimerization is suspected.

Authors:  J Giraldo
Journal:  Br J Pharmacol       Date:  2008-06-09       Impact factor: 8.739

3.  The affinity of D2-like dopamine receptor antagonists determines the time to maximal effect on cocaine self-administration.

Authors:  Andrew B Norman; Michael R Tabet; Mantana K Norman; Brittney K Fey; Vladimir L Tsibulsky; Ronald W Millard
Journal:  J Pharmacol Exp Ther       Date:  2011-05-23       Impact factor: 4.030

4.  A triad of residues is functionally transferrable between 5-HT3 serotonin receptors and nicotinic acetylcholine receptors.

Authors:  Richard Mosesso; Dennis A Dougherty
Journal:  J Biol Chem       Date:  2018-01-03       Impact factor: 5.157

5.  Competitive dopamine receptor antagonists increase the equiactive cocaine concentration during self-administration.

Authors:  Andrew B Norman; Mantana K Norman; Michael R Tabet; Vladimir L Tsibulsky; Amadeo J Pesce
Journal:  Synapse       Date:  2010-10-08       Impact factor: 2.562

Review 6.  100 years of modelling ligand-receptor binding and response: A focus on GPCRs.

Authors:  David B Finlay; Stephen B Duffull; Michelle Glass
Journal:  Br J Pharmacol       Date:  2020-02-28       Impact factor: 8.739

7.  Mechanisms of μ-opioid receptor inhibition of NMDA receptor-induced substance P release in the rat spinal cord.

Authors:  Wenling Chen; Helena S Ennes; James A McRoberts; Juan Carlos Marvizón
Journal:  Neuropharmacology       Date:  2017-10-16       Impact factor: 5.250

8.  Probing the CB1 Cannabinoid Receptor Binding Pocket with AM6538, a High-Affinity Irreversible Antagonist.

Authors:  Robert B Laprairie; Kiran Vemuri; Edward L Stahl; Anisha Korde; Jo-Hao Ho; Travis W Grim; Tian Hua; Yiran Wu; Raymond C Stevens; Zhi-Jie Liu; Alexandros Makriyannis; Laura M Bohn
Journal:  Mol Pharmacol       Date:  2019-09-12       Impact factor: 4.436

Review 9.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

Authors:  R L Jones; M A Giembycz; D F Woodward
Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

10.  Detailed mechanistic analysis of gevokizumab, an allosteric anti-IL-1β antibody with differential receptor-modulating properties.

Authors:  Hassan Issafras; John A Corbin; Ira D Goldfine; Marina K Roell
Journal:  J Pharmacol Exp Ther       Date:  2013-11-05       Impact factor: 4.030

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.