Canonica GW, Blaiss M (February 2011). «Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidence». The World Allergy Organization Journal4 (2): 47-53. PMC3500039. PMID23268457. doi:10.1097/WOX.0b013e3182093e19. «The H1-receptor is a transmembrane protein belonging to the G-protein coupled receptor family. Signal transduction from the extracellular to the intracellular environment occurs as the GPCR becomes activated after binding of a specific ligand or agonist. A subunit of the G-protein subsequently dissociates and affects intracellular messaging including downstream signaling accomplished through various intermediaries such as cyclic AMP, cyclic GMP, calcium, and nuclear factor kappa B (NF-κB), a ubiquitous transcription factor thought to play an important role in immune-cell chemotaxis, proinflammatory cytokine production, expression of cell adhesion molecules, and other allergic and inflammatory conditions.1,8,12,30–32 ... For example, the H1-receptor promotes NF-κB in both a constitutive and agonist-dependent manner and all clinically available H1-antihistamines inhibit constitutive H1-receptor-mediated NF-κB production ... Importantly, because antihistamines can theoretically behave as inverse agonists or neutral antagonists, they are more properly described as H1-antihistamines rather than H1-receptor antagonists.15».
Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (December 2004). «The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders». Trends in Pharmacological Sciences25 (12): 618-625. PMID15530639. doi:10.1016/j.tips.2004.10.003.
Canonica GW, Blaiss M (February 2011). «Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidence». The World Allergy Organization Journal4 (2): 47-53. PMC3500039. PMID23268457. doi:10.1097/WOX.0b013e3182093e19. «The H1-receptor is a transmembrane protein belonging to the G-protein coupled receptor family. Signal transduction from the extracellular to the intracellular environment occurs as the GPCR becomes activated after binding of a specific ligand or agonist. A subunit of the G-protein subsequently dissociates and affects intracellular messaging including downstream signaling accomplished through various intermediaries such as cyclic AMP, cyclic GMP, calcium, and nuclear factor kappa B (NF-κB), a ubiquitous transcription factor thought to play an important role in immune-cell chemotaxis, proinflammatory cytokine production, expression of cell adhesion molecules, and other allergic and inflammatory conditions.1,8,12,30–32 ... For example, the H1-receptor promotes NF-κB in both a constitutive and agonist-dependent manner and all clinically available H1-antihistamines inhibit constitutive H1-receptor-mediated NF-κB production ... Importantly, because antihistamines can theoretically behave as inverse agonists or neutral antagonists, they are more properly described as H1-antihistamines rather than H1-receptor antagonists.15».
Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (December 2004). «The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders». Trends in Pharmacological Sciences25 (12): 618-625. PMID15530639. doi:10.1016/j.tips.2004.10.003.
