Pain And Acetylcholine
ironjustice
Complete Freund Adjuvant–Induced Mechanical Hyperalgesia
in the Rat Via a Central Site of Action
The Journal of Pain, Volume 9, Issue 7, July 2008, Pages 580-587
Stephen J. Medhurst, Jon P. Hatcher, Christopher J. Hille,
Sharon Bingham, Nick M. Clayton, Andy Billinton, Iain P. Chessell
Abstract
The role of specific nicotinic receptor (nAChR) subtypes in
antinociception has not been fully elucidated because of the
lack, until recently, of selective tool compounds.
(R)-N-(1-azabicyclo[2.2.2]oct-3-yl)(5-(2-pyridyl)thiopene-2-
carboxamide)
(compound B) is reported to be an agonist selective for the α7nAChR
and in the present study was found to be efficacious in inflammatory
pain models in 2 species.
Compound B reversed complete Freund adjuvant–induced reductions
in paw withdrawal thresholds in rat and mouse in a dose-related
manner, producing maximum reversals of 65% ± 4% at 10 mg/kg and
87% ± 15% at 20 mg/kg.
When rats and mice were predosed with the centrally penetrant,
broad-spectrum nicotinic receptor antagonist mecamylamine, the
efficacy of the agonist was significantly inhibited, producing
reversals
of only 11% ± 5% at 10 mg/kg and 5% ± 13% at 20 mg/kg, confirming
activity via nicotinic receptors.
Rats were also predosed systemically with the selective low-brain
penetrant α7-antagonist methyllycaconitine, which had no effect on
agonist activity (90% ± 18% at 10 mg/kg), suggesting a central
involvement.
This hypothesis was further established with methyllycaconitine
completely inhibited the agonist effect when dosed intrathecally
(1% ± 7%).
Perspective
These studies provide good rationale for the utility of selective,
central nervous system penetrant agonists at the α7-nicotinic
receptor for the treatment of inflammatory pain.
PMID: 18923838
Who loves ya.
Tom
Jesus Was A Vegetarian!
http://tinyurl.com/634q5a
Man Is A Herbivore!
http://tinyurl.com/4rq595
DEAD PEOPLE WALKING
http://tinyurl.com/zk9fk
Happy Oyster
wrote:
>Man Is A Herbivore!
Cattle are wonderful plants. They even can walk!
--
Sehr reich ist auch der Vatikan * Sie lieben Prunk, sie lieben Pracht,
und stets dem Gelde zugetan. * vor allem aber ihre Macht.
Hinter den Kulissen der P�pstissen: http://www.reimbibel.de
Ken
ironjustice
Im sorry predators cannot be heard over the sound of how
awesome I am.
Ken
ironjustice
Ken
schizophrenia,
megalomania and masochism, coupled with low self-esteem and a hignly
confused sexuality.
No wonder he's unable to function in society and lives on the public
dole
Obsessions are repeated, persistent and unwanted ideas, thoughts,
images or impulses that you have involuntarily and that seem to make
no sense. These obsessions typically intrude when you're trying to
think of or do other things.
Compulsions are repetitive behaviors that you feel driven to perform.
These repetitive behaviors are meant to prevent or reduce anxiety or
distress related to your obsessions. You may also make up rules or
rituals to follow that help control the anxiety you feel when having
obsessive thoughts.