Ligand Gated Receptors

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Ligand Gated: Byrant et.al [1] notes that a rapid response is initiated by a ligand/drug binding to a receptor on the ligand gated channel on the cell surface. This binding of the ligand results in the ligand gated channel to open or close, triggering the entry or exit of ions into or out of the cell, along a concentration gradient, causing a cellular response the cell. [2]. Cocaine is an example of a drug which blocks sodium channels. This causes blocked neural transmission and localized loss of sensation [3]. G-Protein Coupled: These receptors are also called metabotropic receptors, which Bryant [1] states act within seconds to bring about a response, slower than the responses seen with ligand-gated receptors. These receptors become activated when a ligand binds to a receptor, located externally on the cell membrane. The G-protein becomes activated from the inactive GDP to the active form, GTP. This causes a change in the effector protein, such as an ion channel, resulting in a response in the cell [1]. Milligan [4] states that LY-404,039, an amino acid analogue drug, acts on the 5-HT2A receptor, to treat schizophrenia. Kinase Linked: …show more content…

This is due to the fact that the binding of a ligand to this receptor triggers processes which change the synthesis of proteins, such as enzymes, through gene transcription in order to bring about a response at a cellular level [5]. An example of a drug that acts on this receptor is Pazopanib, which Stenberg [6] states acts on vascular endothelial growth factor and platelet derived growth factor receptors as well as c-Kit to block tumour growth and inhibit

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