Respond to two colleagues in one of the following ways: If your colleagues’ posts influenced your understanding of these concepts, be sure to share how and why.  Include additional insights you gained.If you think your colleagues might have misunderstood these concepts, offer your alternative perspective and be sure to provide an explanation for them.  Include resources to support your perspective. Main Post Agonist-to-Antagonist Spectrum of Action Molecules that bind to receptors are referred to as ligands ("Pharmacology Corner: Agonists and Antagonists", 2015).  Ligands are capable of binding to receptor sites and producing a biological response. These ligands are called agonists ("Pharmacology Corner", 2015).  The opposite effect can also take place. Ligands that block the responses of agonists are referred to as antagonists. An agonist binds to a receptor site, activates it, and causes a signal to be transmitted. This reaction is called a biological response ("Pharmacology Corner," 2015).  Conversely, an antagonist also binds to a receptor site, but blocks binding from any other agonists, thus preventing any biological response ("Pharmacology Corner", 2015).  Several types of agonists exist on a spectrum. Their place on this spectrum is measured by comparing their binding ability versus endogenous agonists already present in the body ("Pharmacology Corner", 2015).  Endogenous agonists are present in the body. Super agonists produce a greater biological response than endogenous agonists. Next on the spectrum are full agonists, which mimic the efficacy of the endogenous agonists. Next in line are the partial agonists, which only exert a partial biological response as their name suggests ("Pharmacology Corner", 2015).  The next group of agonists are the inverse agonists which act in two ways. They inhibit the normal receptor site activity, and exert the opposite pharmacological activity at the same time. Last on the spectrum are the irreversible agonists which permanently bind and activate the receptor site. Since this action is permanent, it only occurs once and results in the destruction of the receptor ("Pharmacology Corner", 2015).  G-Couple Proteins and Ion-Gated Channels Receptors called G-protein-coupled receptors (GPCRs) facilitate most physiological responses to neurotransmitters, hormones, and stimulants in the environment. As such, they have great potential to be targeted for the treatment of many diseases (Rosenbaum, Rasmussen, & Kobilka, 2009). GPCRs comprise the largest group of membrane proteins and are responsible for most cellular responses to neurotransmitters and hormones. They also contribute significantly to the human senses of vision, smell, and taste (Rosenbaum et al., 2009).  GPCRs are made up of seven alpha-helical segments separated by intracellular and extracellular looped areas (Rosenbaum et al., 2009).                                                             The fastest and least complex of signa.

1. Respond
to two colleagues in one of the following ways:
If your colleagues’ posts influenced your understanding of these
concepts, be sure to share how and why.
Include additional insights you gained.If you think your
colleagues might have misunderstood these concepts, offer your
alternative perspective and be sure to provide an explanation for
them.
Include resources to support your perspective.
Main Post
Agonist-to-Antagonist Spectrum of Action
Molecules that bind to receptors are referred to as ligands
("Pharmacology Corner: Agonists and Antagonists", 2015).
Ligands are capable of binding to receptor sites and producing a
biological response. These ligands are called
agonists ("Pharmacology Corner", 2015). The opposite effect
can also take place. Ligands that block the responses of
agonists are referred to as antagonists. An agonist binds to a
receptor site, activates it, and causes a signal to be transmitted.
This reaction is called a biological response ("Pharmacology
Corner," 2015). Conversely, an antagonist also binds to a
receptor site, but blocks binding from any other agonists, thus
preventing any biological response ("Pharmacology Corner",
2015). Several types of agonists exist on a spectrum. Their
place on this spectrum is measured by comparing their binding
ability versus endogenous agonists already present in the body

2. ("Pharmacology Corner", 2015). Endogenous agonists are
present in the body. Super agonists produce a greater biological
response than endogenous agonists. Next on the spectrum are
full agonists, which mimic the efficacy of the endogenous
agonists. Next in line are the partial agonists, which only exert
a partial biological response as their name suggests
("Pharmacology Corner", 2015). The next group of agonists are
the inverse agonists which act in two ways. They inhibit the
normal receptor site activity, and exert the opposite
pharmacological activity at the same time. Last on the spectrum
are the irreversible agonists which permanently bind and
activate the receptor site. Since this action is permanent, it only
occurs once and results in the destruction of the receptor
("Pharmacology Corner", 2015).
G-Couple Proteins and Ion-Gated Channels
Receptors called G-protein-coupled receptors (GPCRs) facilitate
most physiological responses to neurotransmitters, hormones,
and stimulants in the environment. As such, they have great
potential to be targeted for the treatment of many diseases
(Rosenbaum, Rasmussen, & Kobilka, 2009). GPCRs comprise
the largest group of membrane proteins and are responsible for
most cellular responses to neurotransmitters and hormones.
They also contribute significantly to the human senses of
vision, smell, and taste (Rosenbaum et al., 2009). GPCRs are
made up of seven alpha-helical segments separated by
intracellular and extracellular looped areas (Rosenbaum et al.,
2009).
The fastest and least complex of signal pathways occur with
signals whose receptors are gated ion channels (Ahern &
Rajagopal, 2019). Gated ion channels consist of many
transmembrane proteins that create a hole, or a channel in the
cell membrane. Each ion channel will allow the passage of a

3. certain ionic species depending on its type. They are called
gated because the passage is controlled by a gate which must be
opened to allow the ions to pass (Ahern & Rajagopal, 2019).
The opening of the gates is controlled by the binding of a signal
to the receptor. This causes the immediate passage of millions
of ions across the membrane (Ahern & Rajagopal, 2019).
Epigenetics in Pharmacologic Action
Epigenetics refers to genetic information that exists beyond the
information contained solely in the individual's genetic code
(Stefanska & MacEwan, 2015). Human diseases can be caused
by a single base genetic mutation. Scientists have made great
strides in unraveling the genetic code, recording the first
complete sequence of the human genome in 2001 (Stafanska &
MacEwan, 2015). These advances have prompted scientists to
think beyond treating illness through drugs activating receptors,
but in a more global fashion. Epigenetic mechanisms are
systems that are able to alter or cancel genetic activation, and
are present in all genes (Stefanska & MacEwan, 2015). These
mechanisms may affect more than one gene or group of
proteins, and can even regulate large groups of genes. Cancer is
one disease in which the understanding of epigenetics can be
key to more effective treatment (Stefanska & MacEwan, 2015).
Specific Client Example
One example of a common client issue is the opioid epidemic.
Naloxone (Narcan) is an opioid antagonist that binds to the
opioid receptors in the patient's brain, reversing or blocking the
effects of the opioid ("Opioid overdose reversal with
naloxone (Narcan, Evzio)", 2018). This is essential to save the
patient's life who has accidentally or intentionally overdosed on
opiate drugs. Naloxone can quickly restore a normal breathing

4. pattern in a person whose respirations have slowed or stopped
as a result of the opiate ("Opioid overdose reversal", 2018).
Naloxone (Narcan) can be administered using a pre-filled
delivery device that is sprayed into the nostril while the patient
lies supine. This device is simple to use and requires no
assembly ("Opioid overdose reversal", 2018).
References
Ahern, K., & Rajagopal, I. (2019). Ligand-gated Ion Channel
Receptors. Retrieved from
https://bio.libretexts.org/Bookshelves/Biochemistry/Book:_Bioc
hemistry_Free_and_Easy_(Ahern_and_Rajagopal)/08:_Signaling
/8.2:_Ligand- gated_Ion_Channel_Receptors.Opioid
overdose reversal with naloxone (Narcan, Evzio). (2018).
Retrieved from drugabuse.gov.Pharmacology Corner: Agonists
and Antagonists. (2015). Retrieved from
aegislabs.com/agonistsRosenbaum, D.M., Rasmussen, S.G.F., &
Kobilka, B.K. (2009). The structure and function of G-protein-
coupled receptors. Retrieved from
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3967846/#_ffn_
sectitle.Stefanska, B., & MacEwan, D.J. (2015). Epigenetics and
pharmacology. Retrieved from
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4439868/#_ffn_
sectitle.
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