DALDA (H-Tyr-D-Arg-Phe-Lys-NH2) is a synthetic peptide derivative which acts as a potent and highly selective agonist of the mu opioid receptor. It was originally derived as a more metabolically stable analogue of dermorphin, a naturally occurring opioid peptide secreted by some species of South American frogs.[1][2][3] DALDA is unable to cross the blood-brain barrier, making it highly peripherally selective, but it has been researched for the treatment of colitis and neuropathic pain, where peripheral opioid agonism is able to produce analgesic effects in the absence of central opioid receptor activation.[4][5][6][7][8][9][10][11][12] Some derivatives of DALDA such as [Dmt1]DALDA (where the tyrosine residue has been substituted with 2,6-dimethyl groups) or more complexly modified derivatives such as KGOP01, do however cross the blood-brain barrier and produce typical opioid effects.[13][14][15][16][17][18][19][20]
↑"Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity". Journal of Medicinal Chemistry32 (3): 698–703. March 1989. doi:10.1021/jm00123a035. PMID2537427.
↑"In vivo pharmacokinetics of selective mu-opioid peptide agonists". The Journal of Pharmacology and Experimental Therapeutics298 (1): 57–61. July 2001. doi:10.1016/S0022-3565(24)29351-4. PMID11408525.
↑"Conformation-activity relationships of cyclo-constrained micro/delta opioid agonists derived from the N-terminal tetrapeptide segment of dermorphin/deltorphin". Journal of Peptide Science14 (8): 898–902. August 2008. doi:10.1002/psc.1022. PMID18338322.
↑"OCP002, a Mixed Agonist of Opioid and Cannabinoid Receptors, Produces Potent Antinociception With Minimized Side Effects". Anesthesia and Analgesia136 (2): 373–386. February 2023. doi:10.1213/ANE.0000000000006266. PMID36638515.
↑"Synthesis and in vitro opioid activity profiles of DALDA analogues". European Journal of Medicinal Chemistry35 (10): 895–901. October 2000. doi:10.1016/s0223-5234(00)01171-5. PMID11121615.
↑"Antinociceptive and respiratory effects of intrathecal H-Tyr-D-Arg-Phe-Lys-NH2 (DALDA) and [Dmt1] DALDA". The Journal of Pharmacology and Experimental Therapeutics297 (1): 364–371. April 2001. doi:10.1016/S0022-3565(24)29547-1. PMID11259564.
↑"Pharmacological characterization of the dermorphin analog [Dmt(1)]DALDA, a highly potent and selective mu-opioid peptide". European Journal of Pharmacology419 (1): 15–23. May 2001. doi:10.1016/s0014-2999(01)00946-3. PMID11348625.
↑"Identification of the dermorphin tetrapeptide [Dmt1 ]-DALDA in a seized unlabelled vial and its first detection in horse urine: A case report". Drug Testing and Analysis16 (3): 268–276. March 2024. doi:10.1002/dta.3536. PMID37408356.
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