WEEK 2 6630 RESPONSES

Julian Fils Julian Fils: (Week Two)Neurotransmitters and Receptor TheoryCOLLAPSE

Discussion: Neurotransmitters and Receptor Theory

Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents, including how partial and inverse agonist functionality may impact psychopharmacologic treatments’ efficacy.

In simple terms, an agonist creates a specific action, and the antagonist opposes a particular activity. Neurotransmitters that occur naturally stimulate receptors and are thus agonists. Some medications also stimulate receptors and are therefore agonists as well. The mechanism of partial agonists or stabilizers the drugs stimulate the receptors lesser than natural neurotransmitter. It is a common misconception that antagonists are the opposite of agonists because they block agonists’ actions. However, although antagonists prevent agonists’ efforts, they have no activity of their own in the agonist’s absence (Stern et al., 2016).

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For this reason, antagonists are sometimes called “silent.” Inverse agonists, on the other hand, do have opposite actions compared to agonists. That is, they not only block agonists but can also reduce activity below the baseline level when no agonist is present. Thus, the agonist spectrum reaches from full agonists to partial agonists through “silent” antagonists and finally inverse agonists (Stahl, 2013).

Compare and contrast the actions of g couple proteins and ion gated channels

Neurotransmitters trigger G-protein-linked and ion-channel-linked cascades.  There are four elements linked to the G-protein-linked system. The first element is the neurotransmitter, also referred to as the first messenger. The second is the G-protein coupled receptors which have seven transmembrane regions. The third element a G protein, which is a connecting protein. The fourth element is an enzyme that can synthesize a second messenger when activated (Stahl, 2013).  The first steps involve the neurotransmitter binding to the receptor. It also changes the form of the receptor, which allows it to fit with the G protein. Then, the G protein binding is conformed to the receptor of the neurotransmitter. The two receptors (neurotransmitter and the G protein) work with each other, which then bind to enzyme E and synthesizes the second messenger (Stahl, 2013).

Ion channel receptors are a vital component of nervous system signaling, allowing rapid and direct conversion of a chemical neurotransmitter message to an electrical current. Efficient neurotransmission requires the precise interplay of various neurotransmitter receptors at pre-and post-synaptic compartments. Ligand-gated ion channels play a central role in intercellular communication in the nervous system. Ion channels are the cellular machinery for ion flux across the membrane and, therefore, the basis of the electrical excitation of neurons. Ligand-gated ion channels are oligomeric protein assemblies that convert a chemical signal into an ion flux through the post-synaptic membrane and are involved in essential brain functions such as attention, learning, and memory (Li et al., 2015).

Explain how the role of epigenetics may contribute to pharmacologic a