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Biological and Pharmacological Aspects of Histamine Receptors and Their Ligands

  • Mohammed ShahidEmail author
  • Trivendra Tripathi
  • Rahat Ali Khan
  • Nancy Khardori
  • Ali Ibrahim Al-Sultan
  • Hamdan Ibrahim AL-Mohammed
  • Abdulrahman A. Alsultan
  • Anwar Huq
  • Aijaz Ahmed Khan
  • Mashiatullah Siddiqui
Chapter

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.

Keywords

Histamine Histamine receptors H3-receptor H4-receptor Antagonists Agonists 

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

Notes

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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Copyright information

© Springer Science+Business Media B.V. 2010

Authors and Affiliations

  • Mohammed Shahid
    • 1
    • 2
    Email author
  • Trivendra Tripathi
    • 1
  • Rahat Ali Khan
    • 3
  • Nancy Khardori
    • 4
  • Ali Ibrahim Al-Sultan
    • 5
  • Hamdan Ibrahim AL-Mohammed
    • 6
  • Abdulrahman A. Alsultan
    • 6
  • Anwar Huq
    • 7
  • Aijaz Ahmed Khan
    • 8
  • Mashiatullah Siddiqui
    • 9
  1. 1.Department of MicrobiologyJawaharlal Nehru Medical College and Hospital, Aligarh Muslim UniversityAligarhIndia
  2. 2.Section of Microbiology, Department of Biomedical SciencesCollege of MedicineAl HassaKingdom of Saudi Arabia
  3. 3.Department of PharmacologyJawaharlal Nehru Medical College and Hospital, Aligarh Muslim UniversityAligarhIndia
  4. 4.Division of Infectious Diseases, Department of Internal Medicine, School of MedicineSouthern Illinois UniversitySpringfieldUSA
  5. 5.Section of Endocrinology, Department of Internal Medicine, College of MedicineKing Faisal UniversityAl HassaKingdom of Saudi Arabia
  6. 6.Section of Microbiology, Department of Biomedical SciencesCollege of Medicine, King Faisal UniversityAl HassaKingdom of Saudi Arabia
  7. 7.Maryland Pathogen Research Institute, Bioscience Research Building, University of MarylandMarylandUSA
  8. 8.Department of AnatomyJawaharlal Nehru Medical College and Hospital, Aligarh Muslim UniversityAligarhIndia
  9. 9.Department of BiochemistryJawaharlal Nehru Medical College and Hospital, Aligarh Muslim UniversityAligarhIndia

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