Explain the agonist-to-antagonist spectrum of action of
psychopharmacologic agents, including how partial and inverse agonist
functionality may impact the efficacy of psychopharmacologic
treatments.
The traditional
...
Explain the agonist-to-antagonist spectrum of action of
psychopharmacologic agents, including how partial and inverse agonist
functionality may impact the efficacy of psychopharmacologic
treatments.
The traditional drug-receptor theory is a concept of how drugs abide, drugreceptor interaction, and agonists' actions and antagonists with affinity and intrinsic
efficacy (Berg, & Clarke, 2018). Berg and Clark's study of the theory found that drugs
can act as antagonists or agonists. In contrast, agonists drugs have intrinsic efficacy and
affinity, and antagonists have only relationship and no inherent effectiveness. The authors
noted that the antagonists decrease the probability of agonist drug occupancy by
occupying the receptor cells. Still, the increased agonist concentration leads to the agonist
increasing receptor occupancy, thus blocking antagonists' effects. A full agonist generates
the maximal response a system is capable whereas a partial agonist produces a
submaximal reaction; However, a partial agonist's intrinsic efficacy is less than that of a
full agonist; full agonists can also differ in inherent efficacy. Lastly, the spare receptors or
receptor reserve is the ability of an agonist can produce a maximum response without
occupancy of the entire receptor population due to saturation of post-receptor signaling
mechanisms,
Compare and contrast the actions of g couple proteins and ion gated channels.
Ion gated receptors have a key role in the nervous system for signaling, allowing
rapid and conversion of chemical neurotransmitter messages to electrical current with ionotropic
receptors regulated by protein-protein interactions with other ion channels, G-protein coupled
receptors and intracellular proteins (Li et al., 2014). Li et al. found that the G Protein interactions
with ion channel receptors can increase the capacity of neuronal signaling cascades and represent
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a unique target for therapeutic intervention in neuropsychiatric disorder. The authors proposed
that neurotransmission and Ligand-gated ion channels play a central role in intercellular
communication in the nervous system and 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
basic brain functions such as attention, learning, and memory. Furthermore, Ion gated channels include
GABA, acetylcholine, glutamate, Adenosine triphosphate (ATP), AMPA, NMDA, nicotine, and glycine, and
many proteins are known to bind to the different subunits of ligand-gated ion channel receptors at
specific subcellular localization, and these interacting proteins can both modulate ion channel function
and influence the localization of the channel in the cell and in the membrane. Li et al. observed that
ion channel function is modulated by interactions with G couple proteins and influence on the dynamics
of receptor trafficking and targeting to designated subcellular areas, as well as the assembly, stability,
and turnover of the receptor on the membrane and in intracellular signaling pathways with interactions
permitting functioning to both external stimuli and intracellular states which allows for complex signal
processing by neurons and new targets for pharmacological manipulation of neuron function.
Explain how the role of epigenetics may contribute to pharmacologic action.
Epigenetics focuses on alterations and modification of genes, including
methylation, acetylation, phosphorylation, and ubiquitylation of DNA and histone
proteins (nucleosomes), and chromatin remodeling
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