histamine
agonists
there no therapeutic products acting selective agonists h3 receptors, although there several compounds used research tools reasonably selective agonists. examples are:
(r)-α-methylhistamine
cipralisant (initially assessed h3 antagonist, later found agonist, shows functional selectivity, activating g-protein coupled pathways not others)
imbutamine (also h4 agonist)
immepip
imetit
immethridine
methimepip
proxyfan (complex functional selectivity; partial agonist effects on camp inhibition , mapk activity, antagonist on histamine release, , inverse agonist on arachidonic acid release)
antagonists
these include:
a-349,821
abt-239
betahistine (also weak h1 agonist)
burimamide (also weak h2 antagonist)
ciproxifan
clobenpropit (also h4 antagonist)
conessine
failproxifan (no tolerance formation, ciproxifan)
impentamine
iodophenpropit
irdabisant
pitolisant
thioperamide (also h4 antagonist)
vuf-5681 (4-[3-(1h-imidazol-4-yl)propyl]piperidine)
^ krueger km, witte dg, ireland-denny l, et al. (july 2005). g protein-dependent pharmacology of histamine h3 receptor ligands: evidence heterogeneous active state receptor conformations . j. pharmacol. exp. ther. 314 (1): 271–81. doi:10.1124/jpet.104.078865. pmid 15821027.
^ tedford ce, phillips jg, gregory r, pawlowski gp, fadnis l, khan ma, ali sm, handley mk, yates sl (may 1999). development of trans-2-[1h-imidazol-4-yl] cyclopropane derivatives new high-affinity histamine h3 receptor ligands (abstract). journal of pharmacology , experimental therapeutics. 289 (2): 1160–8. pmid 10215700.
^ esbenshade ta, fox gb, krueger km, et al. (september 2004). pharmacological , behavioral properties of a-349821, selective , potent human histamine h3 receptor antagonist . biochem. pharmacol. 68 (5): 933–45. doi:10.1016/j.bcp.2004.05.048. pmid 15294456.
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