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


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.


Histamine Histamine receptors H3-receptor H4-receptor Antagonists Agonists 



histamine H1 receptor


histamine H2 receptor


histamine H3 receptor


histamine H4 receptor


G protein-coupled receptor


messenger RNA


cyclic adenosine monophosphate


Bordetella pertussis-induced histamine sensitization


vasoactive amine sensitization elicited by histamine


histamine H1 receptor gene


sodium dodecyl sulfate polyacrylamide gel electrophoresis


central nervous system


1, 2-diacylglycerol


nitric oxide


cyclic guanosine monophosphate


nuclear factor kappa B


chinese hamster ovary


complementary deoxyribonucleic acid


protein kinase C




cyclic adenosine monophosphate


mitogen-activated protein kinase




tumour necrosis factor




T lymphocytes


mitogen-activated protein kinase


cAMP responsive elements


cytochrome P450


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


histidine decarboxylase


vesicular monoamine transporters


transforming growth factor


organic cation transporter


extraneuronal monoamine transporter



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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