Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Miyoshi, Katsuhiro; Kawakami, Nozomi; Wakayama, Yousuke; Izumi, Norimasa; Horio, Shuhei; Fukui, Hirokazu

doi:10.1254/jphs.fpj04012x

Cited by 13 publications

(11 citation statements)

References 18 publications

(14 reference statements)

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“…Immunoreactive bands were visualized by chemiluminescence using the ECL Western Blotting Detection System (Amersham, Little Chalfont, Buckinghamshire, UK). We confirmed that the band shown in each figure corresponded to the c-myc tagged H1R and that was consistent with the previous report (15).…”

Section: +supporting

confidence: 93%

“…Despite of the importance of phosphorylation, there is no evidence of H1R phosphorylation in intact cells. The muscarinic M 3 receptor also belongs to the family of Gq-protein coupled receptors, and activation of M 3 muscarinic receptor caused heterologous down-regulation of H1R (15). H1R and M 3 muscarinic receptor exist in many same tissues, such as smooth muscle and the central nervous system, and share the regulation of biological responses.…”

Section: Introductionmentioning

confidence: 99%

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Homologous and Heterologous Phosphorylations of Human Histamine H1 Receptor in Intact Cells

et al. 2004

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Abstract. Homologous and heterologous phosphorylations of histamine H 1 receptor (H1R) in intact cells were investigated using Chinese hamster ovary cells stably co-expressing c-myctagged human histamine H 1 and muscarinic M 3 receptors. Increase in histamine-induced homologous phosphorylation of H1R was induced in a dose-and time-dependent manner. Maximum phosphorylation of H1R by 8-fold over the basal level was induced 1 min after the stimulation, and the increased phosphorylation level was maintained over 40 min. M 3 receptormediated heterologous phosphorylation of H1R reached maximum by 2-fold over the basal level at 5 min after the stimulation and then rapidly returned to the basal level by 40 min after the stimulation. Histamine-induced phosphorylation of H1R was partially inhibited by three protein kinase inhibitors including Ro-31-8220 for protein kinase C (PKC), KN-93 for calcium / calmodulin-dependent kinase II (CaMKII), and KT5823 for protein kinase G (PKG), while, M 3 -receptor-mediated phosphorylation of H1R was completely inhibited by Ro 31-8220. Protein kinase activators including phorbol 12-myristate 13-acetate (PMA), 8-bromo-cyclic GMP (8-BrcGMP), and 8-bromo-cyclic AMP (8-Br-cAMP) induced increases in H1R phosphorylation. Increased phosphorylation of H1R, by 5-fold over the basal level, induced with a combination of PMA, 8-Br-cGMP, and 8-Br-cAMP was still lower than that with histamine. It was suggested that H1R-mediated H1R phosphorylation involves the activation of PKC, CaMKII, PKG, and other unidentified kinases including G-protein coupled receptor kinases (GRKs) and that PKC is solely involved in M 3 receptor-mediated H1R phosphorylation.

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Section: +supporting

confidence: 93%

Section: Introductionmentioning

confidence: 99%

Homologous and Heterologous Phosphorylations of Human Histamine H1 Receptor in Intact Cells

et al. 2004

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“…Our previous study showed that simvastatin (1 mg/kg/day) significantly increased muscarinic M1/4 receptor binding in the rat brain ); while Miyoshi (2004) showed that in Chinese hamster ovary (CHO) cells, stimulation of muscarinic M1/4 could lead to down-regulation of H1 receptors (Miyoshi 2004). …”

Section: Discussionmentioning

confidence: 99%

“…Belonging to GPCRs, H1 receptor and muscarinic M1/4 receptors are co-expressed in various tissues (Miyoshi 2004). Therefore, it was reasonable to propose that the effect of simvastatin on H1 receptors could be specific and due to, for instance, interference with cell membrane integrity through interaction with muscarinic receptors.…”

Section: Discussionmentioning

confidence: 99%

Effects of simvastatin and 6-hydroxydopamine on histaminergic H1 receptor binding density in rat brains

Deng

Mackovski

et al. 2010

Progress in Neuro-Psychopharmacology and Biological Psychiatry

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Statins have been widely used for the treatment of a variety of medical conditions including psychoneurological disorders beyond their original use in lowering cholesterol. Histamine receptors play an important role in the regulation of neural activity, however, it is unknown whether statins act on histamine receptors, particularly for their neural regulatory effects. This study examined the effects of simvastatin and 6-hydroxydopamine (6-OHDA) lesions on histamine H1 receptors using [3H] pyrilamine binding autoradiography. Compared to the saline group, simvastatin (1 mg/kg/day) significantly decreased H1 receptor bindings in the primary motor cortex (M1), ventromedial hypothalamic nucleus (VMH), caudate putamen (CPu), accumbens core (AcbC) and prefrontal cortex (PfC) (all pb0.05); however 10 mg/kg/day simvastatin increased H1 receptor density only in the medial amygdaloid nucleus (Mep) (pb0.05), but had no significant effect in other regions examined. The 6-OHDA lesion did not alter H1 receptor binding density in most brain areas, except a trend decrease in the hippocampus (p=0.07) and a trend increase in the cingulate cortex (p=0.06). These results suggested that simvastatin has different effects on the H1 receptors in different rat brain regions depending on the doses. Therefore, simvastatin can modulate histaminergic neurotransmission in the brain, and support the role of H1 receptors in psychoneurological disorders.

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“…They studied the above phenomena by the specific tritiated antagonist N-methyl-4-piperidylbenzilate ([ 3 H]-4NMPB), direct and competition binding studies of antagonists with high affinity to the presynaptic receptor, and saturability occurring at very low ligand concentration, in a stereospecific manner as well as simple mass action law [10] , and some study also derived five subtypes of muscarinic acetylcholine receptors (M 1 to M 5 ) which control physiological processes, such as the function of heart and smooth muscles, glandular secretion, release of neurotransmitters, gene expression and cognitive functions as learning and memory helps us to understand the subtypes of the muscarinic acetylcholine receptors, the role in physiological processes and role in different processes. AFRC Laboratory of Molecular Signalling, Department of Zoology, University of Cambridge studied the role of muscarinic acetylcholine receptors (mAChRs) on the cell body of the fast coxal depressor motor neurone (D f ) in the metathoracic ganglion of the cockroach Periplaneta, investigated using electrophysiological methods [11] .…”

Section: Muscarinic Receptorsmentioning

confidence: 99%

Basic and modern concepts on cholinergic receptor: A review

Tiwari¹,

Dwivedi²,

Singh³

et al. 2013

Asian Pacific Journal of Tropical Disease

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Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Cited by 13 publications

References 18 publications

Homologous and Heterologous Phosphorylations of Human Histamine H1 Receptor in Intact Cells

Homologous and Heterologous Phosphorylations of Human Histamine H1 Receptor in Intact Cells

Effects of simvastatin and 6-hydroxydopamine on histaminergic H1 receptor binding density in rat brains

Basic and modern concepts on cholinergic receptor: A review

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