Bengal School of Technology Sugandha, Delhi Road, Hooghly

BENGAL SCHOOL OF TECHNOLOGY
SUGANDHA, DELHI ROAD, HOOGHLY.
TITLE : ………………………………………..
Histamine and its repectors (description & distribution)
Rajarshee Putatunda
Name : …………………………………………………….
19301920054
Roll no. : ………………………………………………..
3rd year
Year : ………………….,semester : 5th semester
………………
Bachelor of Pharmacy
Course : ….………………………………………………
Medicinal Chemistry - II
Subject : …………………………………………………
PT-513 B
Subject code : ……………………….
 Chemical messenger - wide range of cellular
responses- allergic & inflammatory reactions,
gastric acid secretion, and neurotransmission
in parts of the brain.
 Plays an important role in gastric acid
secretion.
 Occurs in practically all tissues.
 lung, skin, and the GIT.
 mast cells or basophils.
 Occurs as venoms and in secretions
from insect stings.
A. Immunologic Release
 Mast cell sensitized by IgE antibodies attached to their
surface membranes, degranulate explosively when
exposed to the appropriate antigen.
 This type of release requires energy.
 Degranulation leads to the simultaneous release of
histamine, adenosine triphosphate (ATP), and other
mediators that are stored together in the granules .
 Histamine released by this mechanism is a mediator in
immediate (type I) allergic reactions, such as hay fever
and acute urticaria.
 Chemical and mechanical mast cell injury
causes degranulation and histamine release.
 Drugs such as morphine and tubocurarine,
can displace histamine from its bound form
within cells.
 This type of release does not require energy
and is not associated with mast cell injury or
degranulation.
 Loss of granules from the mast cell also
releases histamine.
 Histamine receptors (H1R–H4R) are characterized by
their function, structure, distribution, and their affinity
to histamine .
 Histamine has diverse effects, both pro-inflammatory
and anti-inflammatory, which are determined by both
the histamine receptor subtype and the cells stimulated
types .
 The H1-receptor drives cellular migration, nociception,
vasodilatation, and bronchoconstriction .
 The H2-receptor modifies gastric acid secretion, airway
mucus production, and vascular permeability .
 The H3-receptor plays an important role in neuro-
inflammatory diseases .
 The H4-receptor has also been shown to be involved in
allergy and inflammation .
 involved in allergy and inflammation.
 Found in many tissues and cells, including nerves,
respiratory epithelium, endothelial cells, hepatic cells,
vascular smooth muscle cells, dendritic cells, and
lymphocytes.
 Histamine activates H1R through Gαq/11, which then
activates phospholipase C and increases intracellular
Ca++ levels.
 Thus contracting smooth muscle of the respiratory tract,
increases vascular permeability, and induces the
production of prostacyclin and platelet activating factor by
activating H1R .
 Thus, almost all immediate hypersensitivity reactions,
including symptoms observed in the skin, such as
erythema, pruritus, and edema, may be elicited by the
 The Gαs-coupled H2R is highly expressed in various cells and
tissues, such as B cells, T cells, dendritic cells, gastricparietal
cells, smooth muscle cells, and the brain and cardiac tissues .
 Activation of the receptor can induce airway mucus
production, vascular permeability, and secretion of gastric
acid.
 The role of the H2R is well studied in histidine decarboxylase
knockout mice models which suggest that the lack of
histamine can enhance downregulation of H2R expression in
a tissue-specific manner .
 It is accountable for the relaxation of the airways, uterus, and
smooth muscle cells in the blood vessels.
 involved in the activation of the immune system, such as Th1
cytokine production, reduction of basophil degranulation, T-
cell proliferation, and antibody synthesis .
 The H3R is coupled to Gαi/o .
 It is important for homeostatic regulation of energy
levels, sleep-wake cycle, cognition, and
inflammation.
 The H3R has also been associated with rhinitis.
 Because it is expressed on presynaptic nerves in
the peripheral sympathetic adrenergic system and
also on nasal sub-mucosal glands. Stimulation of
H3R suppressed norepinephrine release at
presynaptic nerve endings and stimulated nasal
sub-mucosal gland secretion .
 Currently, several H3R ligands are available, but
not in clinical use.
 The histamine H4R is coupled to Gα/io proteins .
 is expressed on a variety of immune cells as well as on other
cells such as spleen, intestinal epithelia, lung, synovial tissue,
central nervous system, sensory neurons, and cancer cells .
 H4R mediates the pro-inflammatory responses of histamine
in both autocrine and paracrine manners.
 Histamine enhances adhesion molecule expression, cell shape
change, and cytoskeletal rearrangement via H4R, leading to
the increased migration of eosinophils .
 Sometimes basophils also express H4R on their surface and
release histamine following antigen stimulation .
 Histamine, acting via H4R, induces chemotaxis of bone
marrow-derived basophils.
 H4R may play significant roles in basophil regulation in
allergic dermatitis .
 Hu WW, Chen Z. Role of histamine and its
receptors in cerebral ischemia. ACS chemical
neuroscience. 2012 Apr 18;3(4):238-47.
 Martinez-Mir MI, Pollard H, Moreau J, Arrang
JM, Ruat M, Traiffort E, Schwartz JC, Palacios
JM. Three histamine receptors (H1, H2 and
H3) visualized in the brain of human and
non-human primates. Brain research. 1990
Sep 3;526(2):322-7.

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BENGAL SCHOOL OF TECHNOLOGY

SUGANDHA, DELHI ROAD, HOOGHLY.

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