Why Imitrex may not work sometimes

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Posted by Miguel ( on July 26, 2000 at 00:16:06:

Well, it seems that Imitrex is nothing but a 5-HT1A specific
agonist. This means - a simple vasoconstrictor. I guess
the pharmacologists at Glaxo-Welcome had to settle for
the band-aid approach to pluging a gushing aorta. Simply...
they missed the receptor? It appears that CH is 5-HT2 receptor
dependent. Some drugs act as partial agonists for these receptors,
i.e.: LSD. So...I guess because LSD and other LSD analogs are perhaps
not patentable, or perhaps not ethical to prescribe under
current social structures only one of the symptoms was
addressed by the scientists...vasodilation...via imitrex and zomig. Do they
provide relief to migraine or CH? Sometimes. However, such relief
is only temporary (means - you have to keep buying the drug to get relief)
and sometimes dangerous because of its effects likely being detrimental
to those that suffer from cardiovascular disease. I guess they could
not make a 5-HT2 receptor antagonist, at least one that wouldn't result in the
subject going for a trip without luggage, or that could cross the
blood-brain barrier. So, they settled for the next best thing
something that hits a specific receptor that appears to
control casodilatory responses in some areas of the cerebral
cortex, while hoping that your CH takes place there and only there.

A question remains. Does LSD cross the blood-brain barrier?

If LSD is a partial agonist (a partial antagonist from another perspective) of
5-HT2 receptors, what would a bonafide irreversible, full antagoist accomplish besides
ending CH immediately?

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