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Deltorphin
Deltorphin, also known as deltorphin A and dermenkephalin, is a natural product, naturally occurring, exogenous opioid peptide, opioid heptapeptide and thus, exorphin, with the amino acid sequence Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2. Along with the other deltorphins (such as deltorphin I and deltorphin II) and the dermorphins, deltorphin is endogenous to frogs of the genus ''Phyllomedusa'' such as ''Phyllomedusa, P. bicolor'' and ''Phyllomedusa, P. sauvagei'' where it is produced in their skin, and is not known to occur naturally in any other species. Deltorphin is one of the highest affinity (pharmacology), affinity and most binding selectivity, selective naturally occurring opioid peptides known, acting as a very potency (pharmacology), potent and highly specific agonist of the δ-opioid receptor. Deltorphins have an unusually high blood–brain barrier penetration rate. The nonselective opiate antagonist naloxone inhibits deltorphin uptake by brain microvessels, but neither the se ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Deltorphin II
Deltorphin, also known as deltorphin A and dermenkephalin, is a naturally occurring, exogenous opioid heptapeptide and thus, exorphin, with the amino acid sequence Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2. Along with the other deltorphins (such as deltorphin I and deltorphin II) and the dermorphins, deltorphin is endogenous to frogs of the genus ''Phyllomedusa'' such as '' P. bicolor'' and '' P. sauvagei'' where it is produced in their skin, and is not known to occur naturally in any other species. Deltorphin is one of the highest affinity and most selective naturally occurring opioid peptides known, acting as a very potent and highly specific agonist of the δ-opioid receptor. Deltorphins have an unusually high blood–brain barrier penetration rate. The nonselective opiate antagonist naloxone Naloxone, sold under the brand names Narcan (4 mg) and Kloxxado (8 mg) among others, is a medication used to reverse or reduce the effects of opioids. It is commonly used to counter d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Deltorphin I
Deltorphin I, also known as D-Ala2.html" ;"title="small>D-Ala2">small>D-Ala2eltorphin I or deltorphin C, is a naturally occurring, exogenous opioid heptapeptide and hence, exorphin, with the amino acid sequence Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2. While not known to be endogenous to humans or other mammals, deltorphin I, along with the other deltorphins and the dermorphins, is produced naturally in the skin of species of ''Phyllomedusa'', a genus of frogs native to South and Central America. Deltorphin possesses very high affinity and selectivity as an agonist for the δ-opioid receptor, and on account of its unusually high blood-brain-barrier penetration rate, produces centrally-mediated analgesic effects in animals even when administered peripherally. See also * Deltorphin * Dermorphin Dermorphin is a hepta-peptide first isolated from the skin of South American frogs belonging to the genus ''Phyllomedusa''. The peptide is a natural opioid that binds as an agonist with hig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Deltorphin I
Deltorphin I, also known as D-Ala2.html" ;"title="small>D-Ala2">small>D-Ala2eltorphin I or deltorphin C, is a naturally occurring, exogenous opioid heptapeptide and hence, exorphin, with the amino acid sequence Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2. While not known to be endogenous to humans or other mammals, deltorphin I, along with the other deltorphins and the dermorphins, is produced naturally in the skin of species of ''Phyllomedusa'', a genus of frogs native to South and Central America. Deltorphin possesses very high affinity and selectivity as an agonist for the δ-opioid receptor, and on account of its unusually high blood-brain-barrier penetration rate, produces centrally-mediated analgesic effects in animals even when administered peripherally. See also * Deltorphin * Dermorphin Dermorphin is a hepta-peptide first isolated from the skin of South American frogs belonging to the genus ''Phyllomedusa''. The peptide is a natural opioid that binds as an agonist with hig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
δ-opioid Receptor
The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous ligands. The regions of the brain where the δ-opioid receptor is largely expressed vary from species model to species model. In humans, the δ-opioid receptor is most heavily expressed in the basal ganglia and neocortical regions of the brain. Function The endogenous system of opioid receptors is well known for its analgesic potential; however, the exact role of δ-opioid receptor activation in pain modulation is largely up for debate. This also depends on the model at hand since receptor activity is known to change from species to species. Activation of delta receptors produces analgesia, perhaps as significant potentiators of μ-opioid receptor agonists. However, it seems like delta agonism provides heavy potentiation to any mu agonism ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Natural Product
A natural product is a natural compound or substance produced by a living organism—that is, found in nature. In the broadest sense, natural products include any substance produced by life. Natural products can also be prepared by chemical synthesis (both semisynthesis and total synthesis) and have played a central role in the development of the field of organic chemistry by providing challenging synthetic targets. The term natural product has also been extended for commercial purposes to refer to cosmetics, dietary supplements, and foods produced from natural sources without added artificial ingredients. Within the field of organic chemistry, the definition of natural products is usually restricted to organic compounds isolated from natural sources that are produced by the pathways of primary or secondary metabolism. Within the field of medicinal chemistry, the definition is often further restricted to secondary metabolites. Secondary metabolites (or specialized metaboli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
Binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants ''K''AB and ''K''AC.The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. : + B AB; \mathi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dermorphin
Dermorphin is a hepta-peptide first isolated from the skin of South American frogs belonging to the genus ''Phyllomedusa''. The peptide is a natural opioid that binds as an agonist with high potency and selectivity to mu Opioid receptors. Dermorphin is about 30–40 times more potent than morphine but theoretically may be less likely to produce drug tolerance and addiction (due to its high potency). The amino acid sequence of dermorphin is H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2. Dermorphin is not found in humans or other mammals and similar D-amino acid peptides have only been found in bacteria, amphibians and molluscs. Dermorphin appears to be made in these through an unusual posttranslational modification carried out by an amino acid isomerase. This unusual process is needed because the D-alanine in this peptide is not among the 20 amino acids coded for in the genetic code and thus the peptide cannot be synthesized in the usual way from the encodings in the genome of an organism. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naltrindole
Naltrindole is a highly potent, highly selective delta opioid receptor antagonist used in biomedical research. In May 2012 a paper was published in ''Nature'' with the structure of naltrindole in complex with the mouse δ-opioid G-protein coupled receptor, solved by X-ray crystallography. Drug design Since peptide compounds are unable to cross the blood–brain barrier, researchers developed naltrindole to be a non-peptide antagonist analog of the delta-preferring endogenous opiate enkephalin. Enkephalin contains an aromatic phenyl group on its Phe4 residue, which was hypothesized to be the "address" sequence responsible for the opiate's delta opioid receptor affinity. Thus, attachment of a phenyl-containing indole molecule to the C-ring of naltrexone's morphinan Morphinan is the prototype chemical structure of a large chemical class of psychoactive drugs, consisting of opiate analgesics, cough suppressants, and dissociative hallucinogens, among others. Structure Morphinan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naloxone
Naloxone, sold under the brand names Narcan (4 mg) and Kloxxado (8 mg) among others, is a medication used to reverse or reduce the effects of opioids. It is commonly used to counter decreased breathing in opioid overdose. Effects begin within two minutes when given intravenously, and within five minutes when injected into a muscle. The medicine can also be administered by spraying it into a person's nose. Naloxone commonly blocks the effects of opioids for 30 to 90 minutes. Multiple doses may be required, as the duration of action of some opioids is greater than that of naloxone. Administration to opioid-dependent individuals may cause symptoms of opioid withdrawal, including restlessness, agitation, nausea, vomiting, a fast heart rate, and sweating. To prevent this, small doses every few minutes can be given until the desired effect is reached. In those with previous heart disease or taking medications that negatively affect the heart, further heart problems have occur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potency (pharmacology)
In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity. A highly potent drug (e.g., fentanyl, alprazolam, risperidone, bumetanide, bisoprolol) evokes a given response at low concentrations, while a drug of lower potency ( meperidine, diazepam, ziprasidone, furosemide, metoprolol) evokes the same response only at higher concentrations. Higher potency does not necessarily mean greater effectiveness or more side effects. The IUPHAR The International Union of Basic and Clinical Pharmacology (IUPHAR) is a voluntary, non-profit association representing the interests of scientists in pharmacology-related fields to facilitate ''Better Medicines through Global Education and Resear ... has stated that 'potency' is ''"an imprecise term that should always be further defined"'', for instance as EC_, IC_, ED_, LD_ and so on. See also * Reaction inhibitor § Potency References Further ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phyllomedusa
''Phyllomedusa'' is a genus of tree frogs in the subfamily Phyllomedusinae found in tropical and subtropical South America (south to northern Argentina) and Panama. It has 16 recognised species. Taxonomy The following species are recognised in the genus ''Phyllomedusa'': * '' Phyllomedusa bahiana'' * ''Phyllomedusa bicolor'' - giant leaf frog * '' Phyllomedusa boliviana'' * '' Phyllomedusa burmeisteri'' - Burmeister's leaf frog * '' Phyllomedusa camba'' * '' Phyllomedusa chaparroi'' * '' Phyllomedusa coelestis'' * '' Phyllomedusa distincta'' * '' Phyllomedusa iheringii'' * '' Phyllomedusa neildi'' * ''Phyllomedusa sauvagii'' - waxy monkey leaf frog * ''Phyllomedusa tarsius''- tarsier leaf frog * '' Phyllomedusa tetraploidea'' * '' Phyllomedusa trinitatis'' * '' Phyllomedusa vaillantii'' - white-lined leaf frog * ''Phyllomedusa venusta'' Several other species formerly included in this genus are now placed in two other phyllomedusid genera: '' Callimedusa'' and '' Pithecopu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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