Assignment of Pharmacology Submitted by Laiba Shah To DR Maryum

Assignment of pharmacology submitted by laiba shah to
Dr maryum
Cell membranes Receptors :

Receptors are typically glycoproteins located in cell membranes that specifically
recognize and bind to ligands. These are smaller molecules (including drugs) that
are capable of 'ligating' themselves to the receptor protein.
Signal transduction :
This binding initiates a conformational change in the receptor protein leading to a
series of biochemical reactions inside the cell (‘signal transduction’), often
involving the generation of ‘secondary messengers’ that is eventually translated
into a biological response (e.g. muscle contraction, hormone secretion).
Formation of the drug-receptor :
Formation of the drug-receptor complex is usually reversible and the proportion
of receptors occupied (and thus the response) is directly related to the
concentration of the drug. Reversibility enables biological responses to be
modulated and means that similar ligands may compete for access to the
receptor.
Types of drug receptors :

Channel-linked receptors
Coupled directly to an ion channel. Activation opens the channel, making a cell
membrane permeable to specific ions. These channels are known as ‘ligand-
gated’ because it is receptor binding that operates them (in contrast to ‘voltage-
gated’ channels that respond to changes in membrane potential)
Example :
Nicotinic acetylcholine receptors; gamma-Aminobutyric acid (GABA) receptors.
G-Protein coupled receptors :

Coupled to intracellular effector mechanisms via a family of closely related 'G‐
proteins' that participate in signal transduction by coupling receptor binding to
intracellular enzyme activation or the opening of an ion channel.
Example :
Muscarinic acetylcholine receptors; beta-Adrenoceptors; Dopamine receptors; 5-
hydroxytryptamine (Serotonin) receptors; Opioid receptors
Kinase-linked receptors :
Linked directly to an intracellular protein kinase that triggers a cascade of
phosphorylation reactions.
Example :
Insulin receptors
Nuclear hormone receptors

Intracellular and also known as 'nuclear receptors’. Binding of a ligand promotes
or inhibits synthesis of new proteins, which may take hours or days to promote a
biological effect.
Example :
Steroid hormone receptors; Thyroid hormone receptors; Vitamin D receptors
Voltage-sensitive ion channels :

Found in excitable tissues and a potential target for drugs that can block the
channel or interfere with conductance in other ways.
Example :
Na+ channels that are blocked by local anesthetics such as lidocaine
Transporter proteins :
Specialized proteins that carry ions or molecules across cell membranes.
Movement may be in either direction, and may involve exchange of one
substance for another, co-transport of two or more substances in the same
direction, or ‘pumping’ of a single substance into or out of a cell or organelle.
Drugs may act on transporters to inhibit their activity or may also act as ‘false
substrates’, preventing the transport of the normal biological .
Example :
Inhibitors of serotonin reuptake transporter such as fluoxetine.
Cell adhesion proteins :

Type-1 membrane glycoproteins that mediate cell-cell and cell-matrix adhesion by
acting as transmembrane linkers to connect ligands on the outside of the cell
(other cell membrane molecules, ECM components) to the actin cytoskeleton.
Includes the adherins and integrins.
Example :
β2 integrins on leukocytes which are essential for effective immune responses.
Adhesion class GPCRs. Cadherins such as E-cadherin required for endothelial cell-
cell contact, and tissue morphogenesis during embryonic development.
Enzymes :
Catalyze biochemical reactions, some of which involve the production of key
mediators of physiological processes in body systems. Drugs interfere with the
active site of the enzyme or affect co‐factors required by the enzyme for activity.
In most cases inhibition of the active site is competitive although in some cases it
may be long-lasting and effectively irreversible (e.g. aspirin) .
Example :
Inhibitors of cyclooxygenase such as aspirin; Inhibitors of angiotensin converting
enzyme such as enalapril; Inhibitors of xanthine oxidase such as allopurinol .

Assignment of Pharmacology Submitted by Laiba Shah To DR Maryum

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Assignment of Pharmacology Submitted by Laiba Shah To DR Maryum

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Assignment of pharmacology submitted by laiba shah to

Cell membranes Receptors :

Types of drug receptors :

G-Protein coupled receptors :

Nuclear hormone receptors

Voltage-sensitive ion channels :

Cell adhesion proteins :

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