Distribution and selectivity of drugs for 5-HT receptor subtypes

Distribution and selectivity of drugs for 5-HT receptor subtypes
5-HT1A receptors
Hippocampus, septum, amygdala, cortical limbic area
Agonists: buspirone, gepirone, ipsapirone, flesinoxan
Antagonists: WAY100135, BMY7378, NAN-190
Possible clinical use of agonists: anxiolytics, antidepressants
5-HT1B receptors
Substantia nigra, globus pallidus, dorsal subiculum, superior colliculi
Non-selective: pinodol, propanolol
? selective partial agonists: CP-93, 129
Possible clinical use of antagonists: antidepressants
5-HT1D receptors
Caudate nucleus but widely distributed in human dry and GP brain, similar to
5-HT1B of rat brain
Non-selective: rauwolscine, yohimbine
? selective: L-694, 247
Possible clinical use of antagonists: antidepressants
5-HT1E receptor
In mammalian brain
Possible clinical use: ?
5-HT2A
Neocortex but widely distributed in the mammalian brain
Agonists: DOI, DOB
Non-selective antagonists: ketanserin, ritanserin
Possible clinical use of antagonists: antidepressants, anxiolytics, ? neuroleptics
5-HT2B
In mammalian brain
Possible clinical use: ?
5-HT2C
Choroid plexus
Non-selective antagonists: spiperone, amperozide, pimozide
Possible clinical use of antagonists: neuroleptics
5-HT3
Area postrema, entorhinal and frontal cortex, hippocampus
Agonists: ondansetron, granisetron, zacopride
Possible clinical use of antagonists: antiemetics, anxiolytics, ? antidementia
5-HT4
Collicular and hippocampal neurons
Antagonists SC-205-557, SC-53606
Agonist: SC-49518
Possible clinical use: ?
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8-OHDPAT= Dipropylamino-8-hydroxy-1,2,3,4-tetrahydronaphthylene
RU-24969 = 5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl) 1H indol
mCPP = 1-(3 chlorophenyl) piperazine
TFMPP = 1-(m-trifluoromethylphenyl) piperazine
DOI = 1-(2,5-dimethoxy-1-iodophenyl) 2-aminopropane
MDL73005 = 8,2 (2,3-dihydro-1,4-benzodioxin-2yl) methylamino-ethyl-8-azaspirol (4,5) decan-7,9-dione
NAN190 = 1-(2-methoxyphenyl) 4-(4(2-phthalimido)entyl-piperazine)
5-CT = 5-carboxamidotryptamine
ICI 169369 = (2-(2-dimethylamino-ethylthio-3-phenylquinoline))
ICS 205-930 = (3-tropanyl)-IH-indole-2-carboxylic acid ester
DOM = 2,5-dimethoxy-4-dimethylbenzene ethamine