User:Microice503/Endomorphin-1
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By combining N-terminal guadino modifications, a new class of endonmorphin-1 was synthesized, the range of their bioactivities were measured by radioligand binding assay in order to conclude its potency as an opioid.[1] Endomorphin-1 has a Hight affinity and specificity for opioid receptors for behavioral, physiological and pharmacological assays, it is also a potent analgesic agent which brings effects on cardiovascular, respiratory and gastrointestinal functions as well as in immune system responses..[2]This endogenous opioid peptide can help with neuropathic pain without having the common side effects many neuropathic drugs caused which produces constipation. To make this drug side effect-free, a modification at the N-terminus by 2-aminodecainoic acid is made which in term showed an improve in the drug's metabolic stability along with improving its membrane permeability, while holding its high receptor binding affinity, helping the drug act as a potent agonist[3]
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[edit]References: Original endomorphin-1 analogues exhibit good analgesic effects - ScienceDirect (cuny.edu)
[edit]- ^ "BrowZine". browzine.com. Retrieved 2021-11-02.
- ^ "Endomorphin 1 - an overview | ScienceDirect Topics". www.sciencedirect.com. Retrieved 2021-11-13.
- ^ Varamini, Pegah; Mansfeld, Friederike M.; Blanchfield, Joanne T.; Wyse, Bruce D.; Smith, Maree T.; Toth, Istvan (2012-08-17). "Lipo-Endomorphin-1 Derivatives with Systemic Activity against Neuropathic Pain without Producing Constipation". PLoS ONE. 7 (8): e41909. doi:10.1371/journal.pone.0041909. ISSN 1932-6203. PMC 3422351. PMID 22912681.
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