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Pre-Synaptic Control by Histamine H3 Receptors of Neurotransmitter Release

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Biomedical Aspects of Histamine

Abstract

Histamine regulates pre- and post-synaptically several brain functions, through the interaction with G protein-coupled receptors. Four such receptors (H1–H4) have been cloned, and three of them (H1, H2, and H3) are widely distributed in the mammalian nervous system. The histamine H3 receptor (H3R) was first identified in 1983 by Arrang and colleagues as an auto-receptor controlling histamine synthesis and release. Although H3Rs can be found in the periphery, mainly on axons of sympathetic and parasympathetic neurons, the central nervous system contains the great majority of such receptors, and the comparison with mRNA levels indicates that in most areas H3Rs are expressed on nerve terminals. Several lines of evidence have shown that in addition to its function as auto-receptor, the H3R regulates as a hetero-receptor the release of a number of neuroactive substances, namely acetylcholine, 5-hydroxytryptamine (5-HT, serotonin), noradrenaline, dopamine, glutamate, γ-aminobutyric acid (GABA) and substance P. In this work we review the reported actions of H3R activation on neurotransmitter release.

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Abbreviations

Acn:

acetylcholine

CNS:

central nervous system

EC50 :

half maximal effective concentration

EPSCs:

excitatory post-synaptic currents

EPSPs:

excitatory post-synaptic potentials

IPSCs:

inhibitory post-synaptic currents

IPSPs:

inhibitory post-synaptic potentials

GABA:

γ-aminobutyric acid

GPCRs:

G protein-coupled receptors

5-HT:

5-hydroxytryptamine (serotonin)

H3R:

histamine H3 receptor

hH3R:

human histamine H3 receptor

rH3R:

rat histamine H3 receptor

HPLC:

high-performance liquid chromatography

IC50 :

half maximal inhibitory concentration

K d :

dissociation constant

K i :

inhibition constant

K B :

antagonist dissociation constant

MAPKs:

mitogen-activated protein kinases

NAMH:

N α-methylhistamine

NEM:

N-ethylmaleimide

pA2 :

–log10 K B (estimated from a Schild plot)

pD2 :

–log10 EC50 or IC50

pK i :

–log10 of the inhibition constant

PTX:

pertussis toxin

RAMH:

(R)-α-methylhistamine

SNr:

substantia nigra pars reticulata

TTX:

tetrotoxin

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Authors and Affiliations

  1. Departamento de Fisiología, Biofísica y Neurociencias, Cinvestav-IPN, México, D.F. 07000, México

    Angélica Osorio-Espinoza & José-Antonio Arias-Montaño

  2. Colegio de Ciencia y Tecnología, Universidad de la Ciudad de México, Av. La Corona No. 320, Col. Loma La Palma, México, D.F. 07160, México

    Judith Ramos-Jiménez

Authors
  1. Angélica Osorio-Espinoza
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  2. Judith Ramos-Jiménez
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  3. José-Antonio Arias-Montaño
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Correspondence to José-Antonio Arias-Montaño .

Editor information

Editors and Affiliations

  1. School of Medicine, Dept. Internal Medicine, Southern Illinois University, N. Rutledge 751, Springfield, 62702, Illinois, USA

    Nancy Khardori

  2. J. N. Medical College, Dept. Pharmacology, Aligarh Muslim University, Aligarh, 202002, India

    Rahat Ali Khan

  3. Jawaharlal Nehru Medical College &, Hospital, Aligarh Muslim University, Aligarh, 202002, India

    Trivendra Tripathi

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Osorio-Espinoza, A., Ramos-Jiménez, J., Arias-Montaño, JA. (2010). Pre-Synaptic Control by Histamine H3 Receptors of Neurotransmitter Release. In: Khardori, N., Khan, R., Tripathi, T. (eds) Biomedical Aspects of Histamine. Springer, Dordrecht. https://doi.org/10.1007/978-90-481-9349-3_15

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