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Richard B. Mailman talks with
ScienceWatch.com and answers a few questions about
this month's New Hot Paper in the field of Pharmacology
& Toxicology. The author has also sent along
images of their work.
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Article Title: Functional selectivity and classical
concepts of quantitative pharmacology
Authors: Urban, JD, et al.,
Journal: J PHARMACOL EXP THER
Volume: 320
Issue: 1
Page: 1-13
Year: JAN 2007
* Univ N Carolina, Neurosci Hosp, Sch Med, CB 7160,7011 NC,
Chapel Hill, NC 27599 USA.
* Univ N Carolina, Curriculum Toxicol, Chapel Hill, NC
27599 USA.
* Univ N Carolina, Dept Pharmacol, Chapel Hill, NC 27599
USA.
* Univ N Carolina, Sch Med, Dept Neurol, Chapel Hill, NC
27599 USA.
(addresses have been truncated)
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Figures and descriptions:
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Figure
1:
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Figure 1: Early example of functional
selectivity. Dopamine D2 agonists have been
shown to affect both cAMP synthesis (cAMP)
and G protein-regulated potassium channels
(GIRK). Here, studies in pituitary
lactotrophs with the drug dihydrexidine
show it to be a full agonist at cAMP (right
panel) and an antagonist at GIRK (left
panel). For additional details, see Kilts
et al., J Pharmacol. Exp
Ther. 301: 1179-1189 2002, (PMID:
12023553).
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Figure
2:
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Figure 2: Drug discovery consequences of
functional selectivity. This cartoon
indicates how a compound with D2 properties
like dihydrexidine (Figure 1) might have a
better pharmacological profile if the two
signaling pathways were related to
different physiological effects. Modified
from Mailman, Trends Pharmacol.
Sci. 28(8): 390-396, (PMID:
17629962).
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2008 : March 2008 - New Hot Papers : Richard B. Mailman - Figures & Descriptions
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