Literature DB >> 8516953

Further concerns over Cheng-Prusoff analysis.

P Leff1, I G Dougall.   

Abstract

In his article in last month's issue of TiPS (14, 89-91), Douglas Craig discussed the application of the Cheng-Prusoff relationship to the analysis of antagonists in functional experiments. Craig described how the translation of this method from biochemistry to pharmacology can be accompanied by errors due to theoretical misunderstanding. He also emphasized the lower level of rigour associated with this means of estimating antagonist affinity constants compared with Schild analysis. In this article, Paul Leff and Iain Dougall extend Craig's arguments by describing some additional ways in which the application of the Cheng-Prusoff method to pharmacological experiments are likely to result in misinterpretation and erroneous estimates of antagonist affinity.

Mesh:

Year:  1993        PMID: 8516953     DOI: 10.1016/0165-6147(93)90080-4

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


  38 in total

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Review 4.  Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays.

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7.  VUF10166, a novel compound with differing activities at 5-HT₃A and 5-HT₃AB receptors.

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8.  Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand.

Authors:  David G Witte; Betty Bei Yao; Thomas R Miller; Tracy L Carr; Steven Cassar; Rahul Sharma; Ramin Faghih; Bruce W Surber; Timothy A Esbenshade; Arthur A Hancock; Kathleen M Krueger
Journal:  Br J Pharmacol       Date:  2006-05-22       Impact factor: 8.739

9.  A novel P2-purinoceptor expressed by a subpopulation of astrocytes from the dorsal spinal cord of the rat.

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Journal:  Br J Pharmacol       Date:  1995-12       Impact factor: 8.739

10.  Recruitment of beta-arrestin2 to the dopamine D2 receptor: insights into anti-psychotic and anti-parkinsonian drug receptor signaling.

Authors:  Ib V Klewe; Søren M Nielsen; Louise Tarpø; Eneko Urizar; Concetta Dipace; Jonathan A Javitch; Ulrik Gether; Jan Egebjerg; Kenneth V Christensen
Journal:  Neuropharmacology       Date:  2008-04-08       Impact factor: 5.250

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