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It consist of a nitrogenous
base,a pentose & a
phosphate .The nitrogenous
bases found in nucleotide
are aromatic heterocyclic
compound. The bases are
of two types :
PURINE
PYRIMIDINE
PURINES
purine
· . The first purine product of this pathway, IMP (inosinic acid or inosine
monophosphate), serves as a precursor to AMP and GMP.
The –NH2 group either from AMP or adenosine can be removed to produce
IMP or inosine respectively
URIC ACID
1 mg/dl (women)
HYPERURICEMIA
It refers to an elevation in the serum uric acid
GOUT
PSUEDO GOUT
Location
Only very low levels of A1 mRNA are present in lung, kidney, and small
intestine
Signal transduction
Agonist
Antagonist
1,3-dipropyl-8-phenyl(2-amino-4-chlo) xanthine.
Biological function
It is now well established that adenosine is released from
biological tissues during hypoxia and ischemic conditions.
A2A receptor
Location
immune tissues
platelets
CNS
endothelium.
Signal transduction
Antagonist
8-(3-chlorostyryl)caffeine (CSC)
(3,7-dimethyl-1-propargylxanthine)
A2B receptor
LOCATION
lower levels in the brain, spinal cord, lung, vas deferens, and pituitary in
the eye, lung, uterus, and bladder; aorta, stomach, testis, and skeletal
muscle; and the lowest levels in the jejunum, kidney, heart, skin, spleen,
and liver
Signal transduction
Agonist
N6-(3-iodobenzyl)-5′-(N-methylcarbamoyl)adenosine (IB-MECA)
R-PIA
Biological function
It inhibits cyclic neucleotide PDEs. PDEs catalyse the breakdown of cAMP & cGMP
to 5’-AMP & 5’-GMP respectively.Inhibition of PDEs will lead to accumilation of
cAMP & cGMP, thereby increasing the signal transduction througe this pathway.
Adenosine does not directly contract human isolated bronchial smooth muscle
but when inhaled act as a potent bronchoconstrictor in asthmetic subjects.
Signal transduction
Location
testis, lung, kidneys, placenta, heart, brain, spleen, liver, uterus, bladder,
jejunum, proximal colon, and eye of rat, sheep, and humans
Agonist
Antagonist
Biological function
P2X Receptor
LOCATION
vas deferens,
urinary bladder,
Signal transduction
1. P2X1 receptor.
The P2X1receptor has been cloned from rat vas deferens and human and
mouse urinary bladder
2.P2X2 receptor
3. P2X3 receptor.
4. P2X4 receptor.
The P2X4 receptor protein has been cloned from rat hippocampus, DRG
cells rat and human brain as well as rat endocrine tissue
5. P2X5 receptor.
This P2X receptor was first cloned from rat coeliac ganglia).
Rapid inward currents are activated by ATP > 2MeSATP > ADP,
whereas α,β-meATP is ineffective as an agonist.
6. P2X6 receptor.
This clone was isolated from a rat superior cervical ganglion cDNA library
1. CNS.
P2X receptors are widely distributed in the CNS; excitation and activation
of cation channels by ATP and/or α,β-meATP have been described
throughout the brain and spinal cord
2. Sensory nerves.
Rapid inward currents are mediated by ATP in the dorsal horn of the spinal
cord and there is evidence for P2X receptor-mediated fast synaptic
transmission via ATP in a small subset of dorsal horn neurons
3. PNS
receptors in pheochromocytoma cells that mediate NA and dopamine
release
4. Smooth muscle.
P2Y RECEPTOR
1.P2Y1 RECEPTOR
LOCATION
heart, vascular, connective, immune, and neural tissues. The transcript for
chick brain P2Y1 mRNA is distributed in brain,
Signal transduction
Biological function
vasodilation
2.P2Y2 RECEPTOR
LoCATION
Signal transduction
Cloned P2Y2 and endogenous P2Y2-like receptors couple via both Gi/o and
Gq/11 proteins to mediate phospholipid breakdown and phosphoinositides
as well as Ca2+ mobilization via PLCβ
Biological function
they stimulate the synthesis and release of prostacyclin and NO, leading
to vasodilatation
PEPTIDE
molecules of fewer than 50 amino acid residues are called peptides, larger
molecules being proteins.
Neural and endocrine mediators range in size from 3 to over 200 residues.
Cytokines, chemokines and growth factors are generally larger than 100
residues.
Most known peptide mediators come from the nervous system and
endocrine organs. However, some are formed in the plasma, and many
occur at other sites (e.g. vascular endothelium, heart, cells of the immune
system, etc.). The same peptide may occur in several places and serve
different functions
The soluble peptide mediators in the body, which are secreted by cells and act
on surface receptors of other cells, can be very broadly divided into four groups:
growth factors: produced by many different cells and tissues and control
cell growth and differentiation
mediators of the immune system: (cytokines and chemokines )
The mechanisms for the storage and release and the receptor
mechanisms through which their effects are produced are
essentially the same for peptide and non-peptide transmitters,
the main difference being that the vesicles are loaded with
peptide precursors in the cell body, the active peptides being
generated within the vesicles as they move to the nerve
terminals.
recapture of the released mediators does not occur as it does with amine
and amino acid mediators
The coding regions of the gene (exons) are transcribed and spliced to give
rise to mRNA, segments of which (blue) are translated to produce
preprohormones.
PEPTIDE NEUROTRANSMITTERS
1.Vasopressin
2.Oxytocin
3.Neurotensin
4Tachykinins
Substance P
NK-A &NK-B
5.VIP
6.Opiod peptide
B-endorphin
Dynorphin
Endomorphin
Nociceptin
7.Cholecystokinin
8.AG-2
10.Neuropeptide
VASOPRESSIN
Vasopressin (arginine vasopressin, AVP; antidiuretic hormone, ADH) is
a nonapeptide hormone formed in the hypothalamus and released from
the posterior pituitary. Its primary function in the body is to regulate
extracellular fluid volume by affecting renal handling of water; however, it
also is a potent vasoconstrictor
Atrial receptor firing normally inhibits the release of AVP by the posterior
pituitary. With hypovolemia or decreased central venous pressure, the
decreased firing of atrial stretch receptors leads to an increase in AVP
release.
ADH receptors
Kidney
Blood vessel
Specific drug
1 Arginine vasopressin
Therapeutic effect
for treating excessive water loss caused by diabetes insipidus and for
treating bleeding caused by esophageal varices. AVP infusion is being
investigated for use in treating septic shock, a condition that can be
caused by a bacterial infection in the blood and the release of bacterial
endotoxins such as lipopolysaccharide
2.Terlipressin
3.Felypresin
4.Lypressin
OXYTOCIN
Pharmacological action
Breast
Uterus
Misc.
NEUROTENSIN
PURINE ANALOGUES
Till today the research is going on for newer analogues of it. although the
founded once such as,
Adenosine
ATP
Azathioprine
Fludarabin
Vidarabine
6-Mercapto purine(6-MP)
2) CVS disorder:
Adenosine
3) Immunosuppressive agent:
As anticancer agent
6-Mercaptopurine (6-MP):-
Vidarabine:
Fludarabine:
Pentostatin:
As Immunosupressive agent
Azathioprine:
It metabolised to mercaptopurine.