Malenka R. C., Nestler E. J., Hyman S. E.Chapter 6: Widely Projecting Systems: Monoamines, Acetylcholine, and Orexin // Molecular Neuropharmacology: A Foundation for Clinical Neuroscience (англ.) / Sydor A., Brown R. Y.. — 2nd. — New York: McGraw-Hill Medical, 2009. — P. 175—176. — ISBN 9780071481274.. — «Within the brain, histamine is synthesized exclusively by neurons with their cell bodies in the tuberomammillary nucleus (TMN) that lies within the posterior hypothalamus. There are approximately 64000 histaminergic neurons per side in humans. These cells project throughout the brain and spinal cord. Areas that receive especially dense projections include the cerebral cortex, hippocampus, neostriatum, nucleus accumbens, amygdala, and hypothalamus. ... While the best characterized function of the histamine system in the brain is regulation of sleep and arousal, histamine is also involved in learning and memory ... It also appears that histamine is involved in the regulation of feeding and energy balance.».
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Shimamura T., Shiroishi M., Weyand S., Tsujimoto H., Winter G., Katritch V., Abagyan R., Cherezov V., Liu W., Han G.W., Kobayashi T., Stevens R.C., Iwata S. Structure of the human histamine H1 receptor complex with doxepin (англ.) // Nature : journal. — 2011. — July (vol. 475, no. 7354). — P. 65—70. — doi:10.1038/nature10236. — PMID21697825. — PMC3131495.
de Graaf C., Kooistra A.J., Vischer H.F., Katritch V., Kuijer M., Shiroishi M., Iwata S., Shimamura T., Stevens R.C., de Esch I.J., Leurs R. Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor (англ.) // Journal of Medicinal Chemistry[англ.] : journal. — 2011. — December (vol. 54, no. 23). — P. 8195—8206. — doi:10.1021/jm2011589. — PMID22007643. — PMC3228891.
Canonica G.W., Blaiss M. Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidence (англ.) // The World Allergy Organization Journal : journal. — 2011. — February (vol. 4, no. 2). — P. 47—53. — doi:10.1097/WOX.0b013e3182093e19. — PMID23268457. — PMC3500039.. — «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 GCPR 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».
Shimamura T., Shiroishi M., Weyand S., Tsujimoto H., Winter G., Katritch V., Abagyan R., Cherezov V., Liu W., Han G.W., Kobayashi T., Stevens R.C., Iwata S. Structure of the human histamine H1 receptor complex with doxepin (англ.) // Nature : journal. — 2011. — July (vol. 475, no. 7354). — P. 65—70. — doi:10.1038/nature10236. — PMID21697825. — PMC3131495.
de Graaf C., Kooistra A.J., Vischer H.F., Katritch V., Kuijer M., Shiroishi M., Iwata S., Shimamura T., Stevens R.C., de Esch I.J., Leurs R. Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor (англ.) // Journal of Medicinal Chemistry[англ.] : journal. — 2011. — December (vol. 54, no. 23). — P. 8195—8206. — doi:10.1021/jm2011589. — PMID22007643. — PMC3228891.
Canonica G.W., Blaiss M. Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidence (англ.) // The World Allergy Organization Journal : journal. — 2011. — February (vol. 4, no. 2). — P. 47—53. — doi:10.1097/WOX.0b013e3182093e19. — PMID23268457. — PMC3500039.. — «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 GCPR 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».
de Graaf C., Kooistra A.J., Vischer H.F., Katritch V., Kuijer M., Shiroishi M., Iwata S., Shimamura T., Stevens R.C., de Esch I.J., Leurs R. Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor (англ.) // Journal of Medicinal Chemistry[англ.] : journal. — 2011. — December (vol. 54, no. 23). — P. 8195—8206. — doi:10.1021/jm2011589. — PMID22007643. — PMC3228891.
