Histamine as an endogenous antagonist of nicotinic ACh-receptor

Ohta, Y.; Ariyoshi, Mamoru; Koketsu, K.

doi:10.1016/0006-8993(84)90389-5

Cited by 13 publications

(6 citation statements)

References 14 publications

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“…In the present study, H 2 R expression remained constant throughout all the phases of myogenesis, and thus, may be involved in the maintenance of relaxation following burst release of histamine (since H 2 R stimulation requires high histamine concentrations), with a curare-like effect (which is a competitive antagonist of the nicotinic acetylcholine receptor) ( 15 ). By contrast, H 2 R antagonists have been demonstrated to possess an anti-cholinesterase activity ( 16 ).…”

Section: Discussionmentioning

confidence: 55%

Identification of histamine receptor subtypes in skeletal myogenesis

Chen

Stegaev

Kouri

et al. 2014

Molecular Medicine Reports

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To date, conventional and/or novel histamine receptors (HRs) have not been investigated in mouse skeletal myogenesis. Therefore, the present study aimed to investigate the HR-subtypes in skeletal myogenesis. The myogenesis of C2C12 skeletal myoblasts was evaluated using desmin, myogenin and myosin heavy chain (Myh) as early, intermediate and late differentiation markers, respectively. Reverse transcription-quantitative polymerase chain reaction and immunostaining were performed and the messenger RNA (mRNA) expression levels of the HR-subtypes and markers were determined. H1R mRNA was found to be highly expressed in myoblasts at day 0; however, the expression levels were reduced as differentiation progressed. By contrast, H2R mRNA expression remained constant, while H3R mRNA expression increased by 28-, 103- and 198-fold at days 2, 4 and 6 compared with the baseline level (day 0), respectively. In addition, Myh expression increased by 7,718-, 94,487- and 286,288-fold on days 2, 4 and 6 compared with the baseline expression level (day 0). Weak positive staining of the cells for H3R protein was observed on day 2, whereas highly positive staining was observed on days 4 and 6. HR expression during myogenesis was, in part, regulated by the stage of differentiation. These results along with previous findings indicated possible involvement of H1R in the regulation of progenitor cell mitogenesis and of H2R in the relaxation of acetylcholine-stimulated contraction of muscle cells, following the activation of professional histamine-producing cells, including mast cells. By contrast, H3R may participate in the regulation of specialized myocyte functions, potentially by maintaining the relaxed state under the influence of constitutive H3R activity and low histamine concentrations, locally produced/released by non-professional histamine-producing cells.

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Section: Discussionmentioning

confidence: 55%

Identification of histamine receptor subtypes in skeletal myogenesis

Chen

Stegaev

Kouri

et al. 2014

Molecular Medicine Reports

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Section: A) Experimental Evidencementioning

confidence: 99%

“…Histamine shifted the dose-response relationship between ACh concentration and ACh-current in parallel manner to the right, suggesting that histamine depresses the ACh-current in competitive manner [17,55]. The blocking action of ETX-b on neuromuscular transmission was prevented by a previous application of histamine [55]. AKASU et al, [8] reported that luteinizing hormone-releasing hormone (LH-RH), an endogenous polypeptide, depressed the sensitivity of nicotinic ACh-receptors at low concentrations in bullfrog sympathetic ganglion cells and at frog skeletal muscle end-plates in a non-competitive manner, similar to catecholamines.…”

Section: A) Experimental Evidencementioning

confidence: 99%

Modulation of receptor sensitivity and action potentials by transmitters in vertebrate neurones.

Koketsu

1984

Jpn.J.Physiol

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According to the classical concept of synaptic transmission, it occurs at a synapse where a presynaptic nerve terminal (synaptic knob) comes in close contact with the subsynaptic membrane of a postsynaptic neurone. A very narrow gap,, called the synaptic cleft, separates the pre-and subsynaptic membranes. Transmitters released from presynaptic nerve terminals diffuse across the synaptic cleft andd interact with receptors which are located at the subsynaptic membrane. The action of the transmitter is very rapid and powerful. The interaction of the transmitter with receptors results in the generation of a postsynaptic potential. The size of the postsynaptic potential is indicative of the efficiency of synaptic transmission. The postsynaptic potential (PSP) can be either an excitatory postsynaptic potential (EPSP) or an inhibitory postsynaptic potential (IPSP). When the EPSP depolarizes the postsynaptic membrane to a critical membrane potential, an action potential is produced which propagates along the membrane of the postsynaptic neurone.Such a typical transmission does not always occur. In many cases, a neurone which releases a transmitter does not make close contact with its target neurones. In general, endogenous substances, such as transmitters or hormones, reach the membranes of their target neurones via many different routes after they are released. Thus the actions of endogenous substances reaching remote target neurones should be relatively weak and slow, but sustained. This is different from the typical synaptic transmission. Furthermore, the mode of action of these substances may be more complex. The combination of these substances with their target receptors changes the physiological state of target neurones in a variety of ways. These actions of endogenous substances are considered to be modulatory on the target neurones.There appear to be at least four different types of modulatory actions by transmitters. In type 1 modulation, a transmitter acts on the membrane of a target neurone and changes the amount of transmitter or hormone released from the target neurone. Much research has been devoted to this type of modulatory action of transmitters, especially in connection with presynaptic inhibition. In type 2 modulation, the transmitter changes the sensitivity of a receptor located on

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“…Hence, the modulation of cholinergic transmission at the frog neuromuscular junction by histamine is obviously inhibitory since histamine (100 JIM, used in the present experiments) decreased not only the release of ACh from motor nerve terminals but also the sensitivity of the endplate receptor to ACh (see also results by Scuka, 1973;Ohta et al, 1984). However, further experiments need to be performed to investigate the physiological significance of this effect of histamine.…”

Section: Discussionmentioning

confidence: 71%

“…The results obtained demonstrated that histamine may act as an antagonist of ACh at the binding site of the nicotinic receptor-ionic channel complex. A preliminary account of this work has been published previously (Ohta et al, 1984).…”

Section: Introductionmentioning

confidence: 99%

Histamine is an antagonist of the acetylcholine receptor at the frog endplate

Ariyoshi

Hasuo

Koketsu

et al. 1985

British J Pharmacology

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The effects of histamine on the acetylcholine (ACh) receptor‐channel complex were examined by means of voltage‐clamp at the frog endplate. ACh was ionophoretically applied to the endplate. Histamine was added to the perfusate. Histamine (100 nM − 1 mM) reversibly depressed the peak amplitude of the ACh‐induced inward current in a dose‐dependent manner. The double reciprocal plot of the dose‐response relationship between the peak ACh current and the amount of ACh applied suggested that histamine (100 μM) depressed the ACh‐induced current in a competitive manner. Histamine prevented the specific ACh binding site within the receptor‐channel complex from binding erabutoxin, a sea‐snake venom, which binds irreversibly to the specific ACh binding site. Histamine had no detectable effects on the equilibrium potential of the endplate current but shortened the half‐decay time of the endplate current in a voltage‐dependent manner. It was therefore concluded that histamine blocks not only the specific ACh binding site but also interacts with the ACh‐channel site. The present experiments strongly suggest that histamine can act as an antagonist to modulate nicotinic cholinergic transmission.

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Histamine as an endogenous antagonist of nicotinic ACh-receptor

Cited by 13 publications

References 14 publications

Identification of histamine receptor subtypes in skeletal myogenesis

Identification of histamine receptor subtypes in skeletal myogenesis

Modulation of receptor sensitivity and action potentials by transmitters in vertebrate neurones.

Histamine is an antagonist of the acetylcholine receptor at the frog endplate

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