A.

RECEPTOR
Receptors are macromolecules involved in chemical signaling between and
within cells; they may be located on the cell surface membrane or within the
cytoplasm .Activated receptors directly or indirectly regulate cellular biochemical
processes (eg, ion conductance, protein phosphorylation, DNA transcription,
enzymatic activity). Molecules (eg, drugs, hormones, neurotransmitters) that
bind to a receptor are called ligands. A ligand may activate or inactivate a
receptor; activation may increase or decrease a particular cell function. Each
ligand may interact with multiple receptor subtypes. Few if any drugs are
absolutely specific for one receptor or subtype, but most have relative selectivity.
Selectivity is the degree to which a drug acts on a given site relative to other
sites; selectivity relates largely to physicochemical binding of the drug to cellular
receptors.
A drugs ability to affect a given receptor is related to the drugs affinity
(probability of the drug occupying a receptor at any given instant) and intrinsic
efficacy (intrinsic activitydegree to which a ligand activates receptors and
leads to cellular response). A drugs affinity and activity are determined by its
chemical structure.The drug works by getting involved in the interaction between
endogenous chemical compounds with these receptors, either stimulating
(agonist) or prevent the interaction (antagonist)
Type of receptors
1. ligand-gated ion channels
This receptor is located in the cell membrane, called receptors ionotropik.
Response occurred in a matter of milliseconds. have the receptor and
transducing functions as part of the same protein molecule. Interaction of
the chemical signal with the binding site of the receptor causes the
opening or closing of an ion channel pore in another part of the same
molecule. The resulting ion flux changes the membrane potential of the
target cell and, in some cases, can also lead to entry of Ca 2+ ions that
serve as a second messenger signal within the cell. Good examples of
such receptors are the neurotransmitter receptors
Example: nicotinic receptors, GABAA receptors, glutamate receptors and
receptor 5- ionotropik HT3.
2. Receptors linked enzyme
Enzyme linked receptor is a transmembrane protein with a large section
containing the extracellular ligand binding site for (eg growth factors,
cytokines)
and the intracellular portion having enzyme activity (usually a tyrosine
kinase activity).
Initiate activation of intracellular pathways involving cytosolic and nuclear
transducer,
even gene transcription. Cytokine receptor activates Jak kinase, which in
turn
Stat activate transcription factors, which then activates gene transcription

3.

G-protein-linked receptors
GPCR, called receptors metabotropik, located in the cell membrane and
response
occur in a matter of seconds. GPCR has a single polypeptide chain with
seven helical
transmembrane. Signal transduction occurs by activation of G-protein part
later
modulate / regulate enzyme activity or function of the canal

4. Gene transcription linked receptors

Receptors linked gene transcription is also called nuclear receptors
(although some
in the cytosol, the cytosolic receptors which then migrate to the nucleus
after
bind to the ligand, such as the glucocorticoid receptor). Example:
corticosteroid receptors,
estrogen and progestogen receptors
Drug receptor interactions
Ligands such as hormones or neurotransmitters like a key that binds
the
specific receptor (which acts as a keyhole). This interaction opens the
cell's response.
Drug-like ligand, when interacting with the same receptor responds with
ligand, an agonist that can be unlocked. Other drugs that work against
called antagonists.