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Histaminergic transmission in the mammalian brain.
Article de synthese sur le metabolisme de l'histamine, sur la localisation des voies neuronales and des recepteurs histaminergiques, dans le controle neuroendocrine dans la regulation cardiovasculaire. Expand
Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Northern blot and in situ hybridization analyses showed the 5-HT7 transcripts to be expressed in discrete areas of the limbic brain (e.g., pyramidal hippocampus cells, tenia tecta, amygdaloid, or mammillary nuclei), suggesting that the receptor mediates serotoninergic controls in functions like mood, learning, or neuroendocrine and vegetative behaviors. Expand
Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor
It is shown here that histamine inhibits its own release from depolarized slices of rat cerebral cortex, an action apparently mediated by a class of receptor (H3) pharmacologically distinct from those previously characterized, that is, the H1 and H2 receptors. Expand
A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation.
Cloned a rat cDNA encoding a functional serotonin receptor (5-HT6), its coding sequence corresponds to a glycoprotein of 436 amino acids displaying significant homology with other cloned monoaminergic receptors, e.g., various serotonin receptors. Expand
High constitutive activity of native H3 receptors regulates histamine neurons in brain
It is shown that constitutive activity of native H3 receptors is present in rodent brain and that it controls histaminergic neuron activity in vivo, and inverse agonists may find therapeutic applications, even in the case of diseases involving non-mutated receptors expressed at normal levels. Expand
Highly potent and selective ligands for histamine H3-receptors
New drugs selective for histamine H3-receptors can be used to establish that these receptors are involved in the feedback control ofhistamine synthesis and release, and to demonstrate theirExpand
A detailed mapping of the histamine H3 receptor and its gene transcripts in rat brain
The detailed distribution of histamine H(3) receptor mRNAs in rat brain was analyzed by in situ hybridization using a 33P-labelled riboprobe and was combined for the first time with the detailedExpand
BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, Hydrochloride], a Nonimidazole Inverse Agonist/Antagonist at the Human Histamine H3 Receptor: Preclinical Pharmacology
Preclinical data suggest that BF2.649 is a valuable drug candidate to be developed in wakefulness or memory deficits and other cognitive disorders. Expand
Protean agonism at histamine H3 receptors in vitro and in vivo
Protean agonism demonstrates the existence of ligand-directed active states LR* different from, and competing with, constitutively active states R* of GPCRs, and defines a pharmacological entity with important therapeutic implications. Expand
Autoinhibition of histamine synthesis mediated by presynaptic H3-receptors
It is concluded that H3-receptors control not only release but also synthesis of histamine at the level of nerve endings and also, presumably, of perikarya. Expand