Histamine Receptor
Histamine is synthesized in the tuberomamillary nucleus (TMN) neurons from histidine by the specific enzyme histidine decarboxylase (HDC). Four histamine receptors, which are GPCRs, have been cloned (H1eH4R). H1R, H2R and H3R are expressed in distinctive patterns in the brain and all three receptor types are highly expressed in the hypothalamus. The H1Rs mediate excitatory actions on central neurons usually by recruiting Gq/11 and PLC, which leads to the formation of the two second messengers, diacylglycerol (DAG) and inositol-1,4,5-triphosphate (Ins(1,4,5)P3) and Ca2þ release from internal stores. The H2Rs couple to Gs, adenylyl cyclase (AC) and PKA, which phosphorylates proteins and activates the transcription factor cyclic-AMP-response element (CRE)-binding protein (CREB). The H3Rs couple to Gs, adenylyl cyclase (AC) and PKA, which phosphorylates proteins and activates the transcription factor cyclic-AMP-response element (CRE)-binding protein (CREB).
References
1.Tabarean IV. Neuropharmacology. 2016;106:13–19.
References
1.Tabarean IV. Neuropharmacology. 2016;106:13–19.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(471)
Bombesin Receptor(11)
Bradykinin Receptor(18)
Calcium Channel(137)
cAMP(9)
Cannabinoid Receptor(69)
CaSR(17)
CGRP Receptor(14)
Chemokine Receptor(104)
Cholecystokinin Receptor(17)
CRF Receptor(13)
Dopamine Receptor(145)
Endothelin Receptor(20)
FFAR(5)
Galanin Receptor(1)
GHSR(16)
Glucagon Receptor(36)
GPCR19(7)
GPR119(3)
Hedgehog (Hh)(27)
Histamine Receptor(110)
Imidazoline Receptor(1)
Leukotriene Receptor(9)
LHR(1)
LPA Receptor(12)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(6)
Melanocortin Receptor(22)
Melatonin Receptor(5)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(34)
Neuropeptide Y Receptor(36)
Neurotensin Receptor(8)
Orexin Receptor(14)
Other Targets(3)
OXTR(2)
P2Y Receptor(8)
PAR(24)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(60)
PTH Receptor(1)
S1P Receptor(22)
SGLT(22)
Somatostatin Receptor(11)
Urotensin Receptor(4)
Vasopressin Receptor(16)
Histamine Receptor
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Bavisant
catalog no : M29598
cas no: 929622-08-2
Bavisant is a selective and orally active Human H3 receptor antagonist. Bavisant can be used in research on mechanisms of action, involving wakefulness and cognition and the treatment for ADHD. -
Thioperamide maleate
catalog no : M28347
cas no: 148440-81-7
Thioperamide maleate is an effective and selective antagonist of H3 receptor (Ki = 4.3 nM) for inhibition of [3H]histamine synthesis (Ki = 31 nM). -
GSK-239512
catalog no : M27879
cas no: 720691-69-0
GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders. -
Tecastemizole
catalog no : M27833
cas no: 75970-99-9
Tecastemizole is a selective antagonist of H1 receptor and a major metabolite of astemizole with anti-inflammatory effects. -
HTMT dimaleate
catalog no : M27635
cas no: 195867-54-0
HTMT dimaleate is an H1 and H2 receptor agonist.