TABLE 1. Properties of three histamine receptor subtypes
 

H1

H2

H3

Coding sequence

491 a.a. (bovine)

488 a.a. (guinea pig)

486 a.a. (rat)

358 a.a. (rat)

359 a.a. (dog, human, guinea pig)

?

Chromosome localization

Chromosome 3

Chromosome 5

?

Highest brain densities

Thalamus

Cerebellum

Hippocampus

Striatum

Cerebral cortex

Amygdala

Striatum

Frontal cortex

Substantia nigra

Autoreceptor

No

No

Yes

Affinity for histamine

Micromolar

Micromolar

Nanomolar

Characteristic agonists

2(3-trifluoronethyl)histamine

Impromidine

Sopromidine

(R)a-methylhistamine

Imetit

Characteristic antagonists

Mepyramine (pyrilamine)

Cimetidine

Thioperamide

Radioligands

[3H]Mepyramine

[125I]Iodobolpyramine

[3H]Tiotidine

[125I]Iodoaminopotentidine

[3H](R)a-methylhistamine

[125I]Iodoproxyfan

Second messengers

Inositol phosphates (+)

Arachidonic acid (+)

cAMP (potentiation)

cAMP (+)

Arachidonic acid (-)

Ca2+ (+)

Inositol phosphates (-)

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published 2000