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Biological and Pharmacological Aspects of Histamine Receptors and Their Ligands

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Biomedical Aspects of Histamine

Abstract

Histamine is considered a principle mediator of several physiological and pathological processes. It induces biological activities through differential expression of four types of histamine receptors (H1R, H2R, H3R and H4R). All the histamine receptors are the G protein-coupled receptor (GPCR) family, are expressed on several histamine responsive target tissues and cells, and suggest a potential role of histamine in cell proliferation, differentiation, hematopoiesis, embryonic development, regeneration, wound healing, aminergic neuron-transmission and several brain functions, secretion of pituitary hormones, regulation of gastrointestinal and circulatory functions, cardiovascular system, inflammatory reactions, immunomodulation, functioning of endocrine system and homeostasis. Since H4R has been discovered very recently and there is paucity of comprehensive literature covering new histamine receptors, their agonists/antagonists and role in various diseases. This has prompted a re-evaluation of the actions of histamine, suggesting a new potential for H4R-agonists/antagonists and a possible synergy between histamine receptors-agonists/antagonists in targeting various patho-physiological conditions. This chapter will highlight the biological and pharmacological characterization of histamine, histamine receptors, and their agonists/antagonists in various biomedical aspects.

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Abbreviations

H1R:

histamine H1 receptor

H2R:

histamine H2 receptor

H3R:

histamine H3 receptor

H4R:

histamine H4 receptor

GPCR:

G protein-coupled receptor

mRNA:

messenger RNA

cAMP:

cyclic adenosine monophosphate

Bphs:

Bordetella pertussis-induced histamine sensitization

VAASH:

vasoactive amine sensitization elicited by histamine

Hrh1:

histamine H1 receptor gene

SDS-PAGE:

sodium dodecyl sulfate polyacrylamide gel electrophoresis

CNS:

central nervous system

DAC:

1, 2-diacylglycerol

NO:

nitric oxide

cGMP:

cyclic guanosine monophosphate

NFκB:

nuclear factor kappa B

CHO:

chinese hamster ovary

cDNA:

complementary deoxyribonucleic acid

PKC:

protein kinase C

TM:

transmembrane

cAMP:

cyclic adenosine monophosphate

MAPK:

mitogen-activated protein kinase

IFN:

Interferon

TNF:

tumour necrosis factor

IL:

interleukin

T-cells:

T lymphocytes

MAPK:

mitogen-activated protein kinase

CRE:

cAMP responsive elements

CYP450:

cytochrome P450

DPPE:

N, N diethyl-2-(4-(phenylmethyl)phenoxy) ethanamine

HDC:

histidine decarboxylase

VMATs:

vesicular monoamine transporters

TGF:

transforming growth factor

OCT:

organic cation transporter

EMT:

extraneuronal monoamine transporter

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Acknowledgments

Trivendra Tripathi acknowledges University Grants Commission, New Delhi, India for providing UGC Fellowship [UGC letter DON F. 19-33/2006 (CU)] and M. Shahid is grateful to Department of Science & Technology, Ministry of Science and Technology, Government of India for awarding “Young Scientist Project Award” (FT/SR-L-111/2006).

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  1. Department of Microbiology, Jawaharlal Nehru Medical College and Hospital, Aligarh Muslim University, Aligarh, UP, 202002, India

    Mohammed Shahid & Trivendra Tripathi

  2. Section of Microbiology, Department of Biomedical Sciences, College of Medicine, Al Hassa, Kingdom of Saudi Arabia

    Mohammed Shahid

  3. Department of Pharmacology, Jawaharlal Nehru Medical College and Hospital, Aligarh Muslim University, Aligarh, UP, 202002, India

    Rahat Ali Khan

  4. Division of Infectious Diseases, Department of Internal Medicine, School of Medicine, Southern Illinois University, Springfield, IL, USA

    Nancy Khardori

  5. Section of Endocrinology, Department of Internal Medicine, College of Medicine, King Faisal University, Al Hassa, 31982, Kingdom of Saudi Arabia

    Ali Ibrahim Al-Sultan

  6. Section of Microbiology, Department of Biomedical Sciences, College of Medicine, King Faisal University, Al Hassa, 31982, Kingdom of Saudi Arabia

    Hamdan Ibrahim AL-Mohammed & Abdulrahman A. Alsultan

  7. Maryland Pathogen Research Institute, Bioscience Research Building, University of Maryland, Maryland, MD, 20742, USA

    Anwar Huq

  8. Department of Anatomy, Jawaharlal Nehru Medical College and Hospital, Aligarh Muslim University, Aligarh, 202002, UP, India

    Aijaz Ahmed Khan

  9. Department of Biochemistry, Jawaharlal Nehru Medical College and Hospital, Aligarh Muslim University, Aligarh, 202002, UP, India

    Mashiatullah Siddiqui

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  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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Shahid, M. et al. (2010). Biological and Pharmacological Aspects of Histamine Receptors and Their Ligands. In: Khardori, N., Khan, R., Tripathi, T. (eds) Biomedical Aspects of Histamine. Springer, Dordrecht. https://doi.org/10.1007/978-90-481-9349-3_4

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