H1‐antihistamines: inverse agonism, anti‐inflammatory actions and cardiac effects

R Leurs, MK Church… - Clinical & Experimental …, 2002 - Wiley Online Library
This review addresses novel concepts of histamine H1‐receptor function and attempts to
relate them to the anti‐inflammatory effects of H1‐antihistamines. Furthermore, the …

Fine tuning of sympathetic transmitter release via ionotropic and metabotropic presynaptic receptors

S Boehm, H Kubista - Pharmacological reviews, 2002 - ASPET
The release of transmitters at sympathoeffector junctions is not constant, but subject to
modulation by a plethora of different mechanisms. In this respect, presynaptic receptors …

Convergent excitation of dorsal raphe serotonin neurons by multiple arousal systems (orexin/hypocretin, histamine and noradrenaline)

RE Brown, OA Sergeeva, KS Eriksson… - Journal of …, 2002 - Soc Neuroscience
Dorsal raphe serotonin neurons fire tonically at a low rate during waking. In vitro, however,
they are not spontaneously active, indicating that afferent inputs are necessary for tonic …

A detailed mapping of the histamine H3 receptor and its gene transcripts in rat brain

C Pillot, A Heron, V Cochois, J Tardivel-Lacombe… - Neuroscience, 2002 - Elsevier
The detailed distribution of histamine H3 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 …

Binding characteristics of cetirizine and levocetirizine to human H1 histamine receptors: Contribution of Lys191and Thr194

M Gillard, C Van Der Perren, N Moguilevsky… - Molecular …, 2002 - ASPET
Competition experiments with [3H] mepyramine showed that cetirizine and its enantiomers,
levocetirizine and (S)-cetirizine, bound with high affinity and stereoselectivity to human H1 …

Behavioral characterization of mice lacking histamine H3 receptors

H Toyota, C Dugovic, M Koehl, AD Laposky, K Ngo… - Molecular …, 2002 - ASPET
Brain histamine H3 receptors are predominantly presynaptic and serve an important
autoregulatory function for the release of histamine and other neurotransmitters. They have …

Biochemical characterization of desloratadine, a potent antagonist of the human histamine H1 receptor

JC Anthes, H Gilchrest, C Richard, S Eckel… - European journal of …, 2002 - Elsevier
We have characterized desloratadine (5H-benzo [5, 6] cyclohepta [1, 2-b] pyridine, 8-chloro-
6, 11-dihydro-11-(4-piperidinylidene), CAS 100643-71-8) as a potent antagonist of the …

Histamine H3‐receptor‐mediated [35S]GTPγ[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors

A Rouleau, X Ligneau… - British journal of …, 2002 - Wiley Online Library
Constitutive activity of the recombinant and native rat and human H3 receptors (H3Rs) was
studied using H3R‐mediated [35S] GTPγ [S] binding and [3H]‐arachidonic acid release …

Expression and function of histamine receptors in human monocyte-derived dendritic cells

M Idzko, A la Sala, D Ferrari, E Panther… - Journal of allergy and …, 2002 - Elsevier
Background: Histamine is a well-known mediator eliciting different responses in immune
and nonimmune cells, but its role in modulating dendritic cell (DC) functions has been …

Histamine Receptors: Specific Ligands, Receptor Biochemistry, and Signal Transduction

RA Bakker, H Timmerman, R Leurs - Histamine and H1 …, 2002 - taylorfrancis.com
The monoamine histamine is an important chemical messenger that regulates a wide variety
of physiological responses in the brain and peripheral organs. In the central nervous system …