Deltorphin I: Difference between revisions

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'''Deltorphin I''' is a [[heptapeptide]], a chain of seven [[amino acids]], that is naturally produced in the skin of certain species of [[frogs]]. It is one of the most potent [[opioid]] peptides known, with a high affinity for [[delta opioid receptors]] in the [[central nervous system]].
== Deltorphin I ==


==Structure and Synthesis==
[[File:Deltorphin_I.svg|thumb|right|Chemical structure of Deltorphin I]]
Deltorphin I has the [[amino acid sequence]] Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2. The D-Ala in the second position is a D-amino acid, which is less common in nature than L-amino acids. The synthesis of Deltorphin I involves the stepwise addition of these amino acids in a process known as [[peptide synthesis]].


==Biological Activity==
'''Deltorphin I''' is a naturally occurring opioid peptide that is known for its high affinity and selectivity for the [[delta-opioid receptor]]. It is one of the most potent delta-opioid receptor agonists discovered in nature. Deltorphin I was originally isolated from the skin of frogs belonging to the genus ''[[Phyllomedusa]]'', specifically ''Phyllomedusa bicolor''.
Deltorphin I is a potent [[agonist]] at the delta opioid receptor, meaning it binds to this receptor and activates it. This receptor is one of three main types of opioid receptors in the brain, the others being the [[mu opioid receptor]] and the [[kappa opioid receptor]]. Activation of the delta receptor by Deltorphin I can lead to [[analgesia]], or pain relief, as well as other effects such as changes in mood and behavior.


==Pharmacology==
== Structure ==
The [[pharmacokinetics]] of Deltorphin I, including its absorption, distribution, metabolism, and excretion, are not well understood. However, it is known that the peptide can cross the [[blood-brain barrier]], allowing it to exert its effects in the central nervous system. The delta opioid receptor is a [[G protein-coupled receptor]], and activation by Deltorphin I leads to inhibition of [[adenylate cyclase]], reducing levels of the second messenger [[cyclic AMP]].


==Clinical Significance==
Deltorphin I is a heptapeptide with the amino acid sequence Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2. The presence of D-amino acids in its structure is crucial for its high affinity and selectivity towards the delta-opioid receptor. The peptide's structure allows it to interact effectively with the receptor, leading to its potent analgesic effects.
While Deltorphin I itself is not used clinically, it has been the subject of research due to its potent opioid activity. It may serve as a lead compound for the development of new [[analgesics]] and other drugs acting on the delta opioid receptor.
 
== Mechanism of Action ==
 
Deltorphin I exerts its effects by binding to the delta-opioid receptor, a type of [[G protein-coupled receptor]] (GPCR) found in the [[central nervous system]]. Upon binding, it activates the receptor, leading to a cascade of intracellular events that result in analgesia. The activation of delta-opioid receptors by Deltorphin I can modulate neurotransmitter release and influence pain perception.
 
== Pharmacological Effects ==
 
The primary effect of Deltorphin I is analgesia, making it a subject of interest for pain management research. Unlike [[mu-opioid receptor]] agonists, delta-opioid receptor agonists like Deltorphin I may produce analgesia with a lower risk of addiction and respiratory depression. However, the clinical application of Deltorphin I is limited due to its peptide nature, which affects its stability and bioavailability.
 
== Sources and Isolation ==
 
Deltorphin I was first isolated from the skin secretions of ''Phyllomedusa bicolor'', a frog native to South America. The isolation of Deltorphin I and related peptides has provided insights into the diversity of bioactive compounds in amphibian skin and their potential therapeutic applications.
 
== Research and Applications ==
 
Research on Deltorphin I focuses on its potential use in pain management and its role in understanding the delta-opioid receptor system. Studies aim to develop analogs with improved stability and bioavailability for potential therapeutic use. Additionally, Deltorphin I serves as a tool in pharmacological research to study the delta-opioid receptor and its physiological roles.
 
== Related Pages ==


==See Also==
* [[Deltorphin II]]
* [[Dermorphin]]
* [[Opioid peptide]]
* [[Opioid peptide]]
* [[Delta opioid receptor]]
* [[Delta-opioid receptor]]
* [[Phyllomedusa]]
* [[Analgesic]]


[[Category:Peptides]]
[[Category:Opioid peptides]]
[[Category:Opioids]]
[[Category:Pharmacology]]
[[Category:Neurotransmitters]]
{{Peptide-stub}}
{{Opioid-stub}}

Latest revision as of 03:34, 13 February 2025

Deltorphin I[edit]

Chemical structure of Deltorphin I

Deltorphin I is a naturally occurring opioid peptide that is known for its high affinity and selectivity for the delta-opioid receptor. It is one of the most potent delta-opioid receptor agonists discovered in nature. Deltorphin I was originally isolated from the skin of frogs belonging to the genus Phyllomedusa, specifically Phyllomedusa bicolor.

Structure[edit]

Deltorphin I is a heptapeptide with the amino acid sequence Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2. The presence of D-amino acids in its structure is crucial for its high affinity and selectivity towards the delta-opioid receptor. The peptide's structure allows it to interact effectively with the receptor, leading to its potent analgesic effects.

Mechanism of Action[edit]

Deltorphin I exerts its effects by binding to the delta-opioid receptor, a type of G protein-coupled receptor (GPCR) found in the central nervous system. Upon binding, it activates the receptor, leading to a cascade of intracellular events that result in analgesia. The activation of delta-opioid receptors by Deltorphin I can modulate neurotransmitter release and influence pain perception.

Pharmacological Effects[edit]

The primary effect of Deltorphin I is analgesia, making it a subject of interest for pain management research. Unlike mu-opioid receptor agonists, delta-opioid receptor agonists like Deltorphin I may produce analgesia with a lower risk of addiction and respiratory depression. However, the clinical application of Deltorphin I is limited due to its peptide nature, which affects its stability and bioavailability.

Sources and Isolation[edit]

Deltorphin I was first isolated from the skin secretions of Phyllomedusa bicolor, a frog native to South America. The isolation of Deltorphin I and related peptides has provided insights into the diversity of bioactive compounds in amphibian skin and their potential therapeutic applications.

Research and Applications[edit]

Research on Deltorphin I focuses on its potential use in pain management and its role in understanding the delta-opioid receptor system. Studies aim to develop analogs with improved stability and bioavailability for potential therapeutic use. Additionally, Deltorphin I serves as a tool in pharmacological research to study the delta-opioid receptor and its physiological roles.

Related Pages[edit]