Biomaterial Database

Antinociceptive activity of deltorphin analogs in the formalin test. 1996

T Chiba, and H Murase, and A Ambo, and Y Sasaki

Department of Biochemistry, Tohoku College of Pharmacy, Sendai, Japan.

Two deltorphin (DLT: Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2) analogs, [N alpha-n-butyl-Gly6]DLT ([nBuG6]DLT) and [N alpha-iso-butyl-Gly6]DLT ([isoBuG6]DLT), were examined for their antinociceptive activities by a formalin test in mice after subcutaneous (s.c.) injection. [nBuG6]DLT exhibited potent dose-dependent antinociceptive activities at doses of more than 0.02 mumol/kg at the first and second phases, while morphine similarly inhibited of the pain responses at doses more than 0.01 mumol/kg in the formalin test. [isoBuG6]DLT showed potent antinociceptive activity at the second phase, but did not inhibit the pain response at the first phase. This phenomenon may be caused by a mu-antagonist/delta-agonist property of this compound. The antinociceptive effects of these analogs were antagonized by delta-antagonist naltrindole, but not by the mu-antagonist naloxone. These findings suggest that the antinociceptive effects were mediated via delta-receptors. These compounds may be useful as delta-agonists for clarifying the mechanism of analgesia mediated by delta-opioid receptors.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009842	Oligopeptides	Peptides composed of between two and twelve amino acids.	Oligopeptide
D005557	Formaldehyde	A highly reactive aldehyde gas formed by oxidation or incomplete combustion of hydrocarbons. In solution, it has a wide range of uses: in the manufacture of resins and textiles, as a disinfectant, and as a laboratory fixative or preservative. Formaldehyde solution (formalin) is considered a hazardous compound, and its vapor toxic. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p717)	Formalin,Formol,Methanal,Oxomethane
D000701	Analgesics, Opioid	Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.	Opioid,Opioid Analgesic,Opioid Analgesics,Opioids,Full Opioid Agonists,Opioid Full Agonists,Opioid Mixed Agonist-Antagonists,Opioid Partial Agonists,Partial Opioid Agonists,Agonist-Antagonists, Opioid Mixed,Agonists, Full Opioid,Agonists, Opioid Full,Agonists, Opioid Partial,Agonists, Partial Opioid,Analgesic, Opioid,Full Agonists, Opioid,Mixed Agonist-Antagonists, Opioid,Opioid Agonists, Full,Opioid Agonists, Partial,Opioid Mixed Agonist Antagonists,Partial Agonists, Opioid
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D017465	Receptors, Opioid, delta	A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.	Opioid Receptors, delta,Receptors, delta,Receptors, delta Opioid,delta Receptors,delta Opioid Receptor,delta Receptor,Opioid Receptor, delta,Receptor, delta,Receptor, delta Opioid,delta Opioid Receptors
D051379	Mice	The common name for the genus Mus.	Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus