Receptorium histamini H1

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Receptorium histamini H₁

Chromosoma: 3p25.3 (HRH-1)
Obsessum a drogis his:
ABT-239, Amitriptylinum, Aripiprazolum, Astemizolum, Cetirizinum, Chlorphenaminum, Chlorpromazinum, Ciproxifanum, Clemastinum, Clobenpropitum, Clozapinum, Conessinum, Cyclizinum, Cyproheptadinum, Desloratadinum, Doxepinum, Diphenhydraminum, Epinastinum, Fexofenadinum, Fluphenazinum, Haloperidolum, Histaminum, Hydroxyzinum, Impromidinum, Ketotifenum, Laevocetirizinum, Loratadinum, Loxapinum, Mirtazapinum, MK-0249, Molindonum, Olanzapinum, Perphenazinum, Pimozidum, Pipamperonum, Pitolisantum, Promethazinum, Pyridylethylaminum, Pyrilaminum, Quetiapinum, Risperidonum, Sertindolum, Terfenadinum, Thioridazinum, Thiothixenum, Trifluoperazinum, Trimipraminum, Tripelennaminum, Triprolidinum, Vilazodonum, Ziprasidonum, Zotepinum.

Receptorium histamini H₁ (abbreviatura H1R) est simul receptorium histamini typi rhodopsini et familiae receptoriorum proteino G copulatorum (classis G_q) per histaminum ligandum endogenum incitatur^[1]. Inveniuntur H1R in musculis levibus intestini nonstriatis, endotheliis vasorum, corde, systemate nervoso centrali, systemate nervoso autonomico.

Hoc receptorium per inflammationem effectus conciliat, pro eo antagonistis receptorii H₁ virtutes antiinflammatorii sunt. Receptorii histamini H₁ competitores (antagonistae) noti sunt qui receptorium obsidere ergo functiones eorum competere ad postremum antiallergicae efficere possunt. Fatigatio quoque propter receptorii H₁ stimulationem inducitur.

Natura receptorii H₁

Genetica

Genum nomine HRH1 chromosomate 3 (3p25.3, OMIM: 600167) locatum est^[2].

Structura

Structura H1R crystallina investigata per Doxepinum antagonistam inversam est. Effectuum physiologicorum situs anionum pernecesse est^[3]. Istac greges chemici ut grex acidi carboxylici R–COOH ad H1R deactivandum interagunt.

Distributio in corpore

Receptoria H₁ in musculis levibus intestini nonstriatis, endotheliis vasorum, corde, systemate nervoso centrali, systemate nervoso autonomico^[4] locata sunt.

In systemate nervoso centrali et autonomico

In hypothalamo receptoria H₁ inventa sunt, quibus effectus pondus augmendi substantiis antipsychoticis explicantur^[5].

Natura physiologica

Receptorium histamini H₁ receptorium proteino G copulatum

Receptorium histamini H₁ proteino G copulatum (classis G_q) est, familia A18 (familia A - Rhodopsin-like, subfamilia A18 - receptoria histamini et aliorum). In cerebro haec receptoria stimulantur neuronis histaminergicis^[6] origo quorum est hypothalami nucleus tuberomamillaris. Neuroni nuclei tuberomamillaris enim rhythmum circadianum regulant, et illius activiate status vigilans fit.^[7]

Cum receptoria H₁ obsessa effectus fatigationis evocantur. Ideo plures substantiae antihistaminicae effectus adversus defatigant.

Inflammatio

Stimulatio receptoriorum H₁ significans iter NF-κB promovet,^[8]^[9] itaque responsum systematis immunitatis cum inflammatione graviori, quod est pars reactionis allergicae, sequitur.

Effectus

Antagonistae receptoriorum H₁ (H1R) ut Olanzapinum et Quetiapinum lassitudinem atque famis incrementum efficiunt^[10]
Fumatio chronica per H1R incrementum inflammationis cum periculo atherosclerosis producere potest^[11].
Kim et al. effectus numeri circadiani in ratto descripseruntt^[12].

Antagonistae

Medicamenta

Antagonistae receptoriorum H₁ sunt per exemplum:

Diphenhydraminum
Loratadinum
Cetirizinum
Fexofenadinum
Clemastinum — medicamentum "anti"-histaminum cum effectibus antiallergicis et pauci effectus adversii
Quetiapinum

Nexus interni

Synapsis chemica

Notae

↑ Classificatio internationalis receptorum Histamini: Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997). Pharmacol. Rev. 49 (3): 253–78
↑ De Backer M. D., Loonen I., Verhasselt P., Neefs J. M., Luyten W. H. (1998). "Structure of the human histamine H1 receptor gene". Biochem J 335 (Pt 3): 663-70
↑ Shiroishi M, Kobayashi T (2017). "Structural Analysis of the Histamine H1 Receptor". Handb Exp Pharmacol 241: 21-30
↑ Murakami M., Yoshikawa T., Nakamura T., Ohba T., Matsuzaki Y., Sawamura D., Kuwasako K., Yanagisawa T., Ono K., Nakaji S., Yanai K. (2015). "Involvement of the histamine H1 receptor in the regulation of sympathetic nerve activity". Biochemical and biophysical research communications 458 (3): 584-9
↑ Kim S. F., Huang A. S., Snowman A. M., Teuscher C., Snyder S. H. (2007). "From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase". PNAS 104 (9): 3456-9
↑ hic: histaminum per synapses secernens
↑ "The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders". Trends in Pharmacological Sciences 25 (12): 618–25. Dec 2004
↑ Bakker RA, Schoonus SBJ, Smit MJ, Timmerman H, Leurs R (nov 2001). "Histamine H1-Receptor Activation of Nuclear Factor-κB: Roles for Gβγ- and Gαq/11-Subunits in Constitutive and Agonist-Mediated Signaling". Mol Pharmcacol 60 (11): 1133-42
↑ Canonica GW, Blaiss M (feb 2011). "Antihistaminic, Anti-Inflammatory, and Antiallergic Properties of the Nonsedating Second-Generation Antihistamine Desloratadine: A Review of the Evidence". World Allergy Organ J 4 (2): 47-53
↑ Sato H, Ito C, Hiraoka K, Tashiro M, Shibuya K, Funaki Y, Yoshikawa T, Iwata R, Matsuoka H, Yanai K (2015). "Histamine H1 receptor occupancy by the new-generation antipsychotics olanzapine and quetiapine: a positron emission tomography study in healthy volunteers". Psychopharmacology (Berl) 232 (19): 3497-505
↑ Barua RS, Sharma M, Dileepan KN (2015). "Cigarette Smoke Amplifies Inflammatory Response and Atherosclerosis Progression Through Activation of the H1R-TLR2/4-COX2 Axis". Front Immunol 6: 572
↑ Kim YS, Kim YB, Kim WB, Lee SW, Oh SB, Han HC, Lee CJ, Colwell CS, Kim YI (2016). "Histamine 1 receptor-Gβγ-cAMP/PKA-CFTR pathway mediates the histamine-induced resetting of the suprachiasmatic circadian clock". Mol Brain 9 (1): 49

Receptoria histamini


Receptorium histamini • Receptorium histamini H1 • Receptorium histamini H2 • Receptorium histamini H3 • Receptorium histamini H4

[1] Classificatio internationalis receptorum Histamini: Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997). Pharmacol. Rev. 49 (3): 253–78

[2] De Backer M. D., Loonen I., Verhasselt P., Neefs J. M., Luyten W. H. (1998). "Structure of the human histamine H1 receptor gene". Biochem J 335 (Pt 3): 663-70

[3] Shiroishi M, Kobayashi T (2017). "Structural Analysis of the Histamine H1 Receptor". Handb Exp Pharmacol 241: 21-30

[4] Murakami M., Yoshikawa T., Nakamura T., Ohba T., Matsuzaki Y., Sawamura D., Kuwasako K., Yanagisawa T., Ono K., Nakaji S., Yanai K. (2015). "Involvement of the histamine H1 receptor in the regulation of sympathetic nerve activity". Biochemical and biophysical research communications 458 (3): 584-9

[5] Kim S. F., Huang A. S., Snowman A. M., Teuscher C., Snyder S. H. (2007). "From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase". PNAS 104 (9): 3456-9

[6] : histaminum per synapses secernens

[pmid15530639-7] "The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders". Trends in Pharmacological Sciences 25 (12): 618–25. Dec 2004

[8] Bakker RA, Schoonus SBJ, Smit MJ, Timmerman H, Leurs R (nov 2001). "Histamine H1-Receptor Activation of Nuclear Factor-κB: Roles for Gβγ- and Gαq/11-Subunits in Constitutive and Agonist-Mediated Signaling". Mol Pharmcacol 60 (11): 1133-42

[9] Canonica GW, Blaiss M (feb 2011). "Antihistaminic, Anti-Inflammatory, and Antiallergic Properties of the Nonsedating Second-Generation Antihistamine Desloratadine: A Review of the Evidence". World Allergy Organ J 4 (2): 47-53

[10] Sato H, Ito C, Hiraoka K, Tashiro M, Shibuya K, Funaki Y, Yoshikawa T, Iwata R, Matsuoka H, Yanai K (2015). "Histamine H1 receptor occupancy by the new-generation antipsychotics olanzapine and quetiapine: a positron emission tomography study in healthy volunteers". Psychopharmacology (Berl) 232 (19): 3497-505

[11] Barua RS, Sharma M, Dileepan KN (2015). "Cigarette Smoke Amplifies Inflammatory Response and Atherosclerosis Progression Through Activation of the H1R-TLR2/4-COX2 Axis". Front Immunol 6: 572

[12] Kim YS, Kim YB, Kim WB, Lee SW, Oh SB, Han HC, Lee CJ, Colwell CS, Kim YI (2016). "Histamine 1 receptor-Gβγ-cAMP/PKA-CFTR pathway mediates the histamine-induced resetting of the suprachiasmatic circadian clock". Mol Brain 9 (1): 49

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