BIOMAT Database Logo BIOMAT Database Logo

Comparison of opioid activity between a N-terminal tetrapeptide analogue of dermorphin, H-Tyr-D-Arg-Phe-beta-Ala-OH and morphine. 1998

T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Department of Pharmaceutics, Tohoku College of Pharmacy, Sendai, Japan.

The antinociceptive properties of dermorphin tetrapeptide analog, H-Tyr-D-Arg-Phe-beta-Ala-OH (TDAPA) were compared with morphine in mice. In the tail-pressure test, subcutaneously (s.c.) injected TDAPA and morphine produced significant antinociceptive activity. Pretreatment with naloxonazine (35 mg/kg, s.c., 24 h before testing) significantly antagonized the activity induced by TDAPA, but not morphine. The ED50 values of TDAPA changed from 0.39 mg/kg to 1.7 mg/kg by naloxonazine pretreatment In the formalin test, both TDAPA and morphine exhibited dose-related antinociceptive activity with ED50 values of 0.49 mg/kg and 2.5 mg/kg, respectively. Both drug activities were significantly antagonized by naloxonazine. These results indicate different mechanisms of action for TDAPA and morphine, suggesting TDAPA is highly selective for the mu 1-opioid receptor and may be clinically useful.

UI MeSH Term Description Entries
D008297 Male Males
D009020 Morphine The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle. Morphine Sulfate,Duramorph,MS Contin,Morphia,Morphine Chloride,Morphine Sulfate (2:1), Anhydrous,Morphine Sulfate (2:1), Pentahydrate,Oramorph SR,SDZ 202-250,SDZ202-250,Chloride, Morphine,Contin, MS,SDZ 202 250,SDZ 202250,SDZ202 250,SDZ202250,Sulfate, Morphine
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D010147 Pain Measurement Scales, questionnaires, tests, and other methods used to assess pain severity and duration in patients or experimental animals to aid in diagnosis, therapy, and physiological studies. Analgesia Tests,Analogue Pain Scale,Formalin Test,McGill Pain Questionnaire,Nociception Tests,Pain Assessment,Pain Intensity,Pain Severity,Tourniquet Pain Test,Visual Analogue Pain Scale,Analog Pain Scale,Assessment, Pain,McGill Pain Scale,Visual Analog Pain Scale,Analgesia Test,Analog Pain Scales,Analogue Pain Scales,Formalin Tests,Intensity, Pain,Measurement, Pain,Nociception Test,Pain Assessments,Pain Intensities,Pain Measurements,Pain Questionnaire, McGill,Pain Scale, Analog,Pain Scale, Analogue,Pain Scale, McGill,Pain Severities,Pain Test, Tourniquet,Questionnaire, McGill Pain,Scale, Analog Pain,Scale, Analogue Pain,Scale, McGill Pain,Severity, Pain,Test, Analgesia,Test, Formalin,Test, Nociception,Test, Tourniquet Pain,Tests, Nociception,Tourniquet Pain Tests
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
D017450 Receptors, Opioid, mu A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine. Morphine Receptors,Opioid Receptors, mu,Receptors, Morphine,Receptors, mu,Receptors, mu Opioid,mu Receptors,Morphine Receptor,mu Opioid Receptor,mu Receptor,Opioid Receptor, mu,Receptor, Morphine,Receptor, mu,Receptor, mu Opioid,mu 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
D018847 Opioid Peptides The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way. Opiates, Endogenous,Endogenous Opiates,Opiate Peptides,Opioid Peptide,Peptide, Opioid,Peptides, Opiate,Peptides, Opioid

Related Publications

T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Blood-brain barrier transport of a novel micro 1-specific opioid peptide, H-Tyr-D-Arg-Phe-beta-Ala-OH (TAPA).
March 2003, Journal of neurochemistry,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Selective antagonism by naloxonazine of antinociception by Tyr-D-Arg-Phe-beta-Ala, a novel dermorphin analogue with high affinity at mu-opioid receptors.
April 2000, European journal of pharmacology,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Tyr-D-Arg-Phe-beta-Ala-NH2, a novel dermorphin analog, impairs memory consolidation in mice.
August 1993, European journal of pharmacology,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Attenuation of memory with Tyr-D-Arg-Phe-beta-Ala-NH2, a novel dermorphin analog with high affinity for mu-opioid receptors.
December 1995, European journal of pharmacology,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Potent analgesic activity of the enkephalin-like tetrapeptide H-Tyr-D-Ala-Gly-Phe-NH2.
October 1978, Life sciences,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Synthesis and binding characteristics of a novel enkephalin analogue, [3H]Tyr-D-Ala-Gly-Phe-D-Nle-Arg-Phe.
September 2003, Peptides,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Structure-activity relationships (SAR) of [D-Arg(2)]dermorphin(1-4) analogues, N(alpha)-amidino-Tyr-D-Arg-Phe-X.
June 2002, Chemical & pharmaceutical bulletin,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Production and immunohistochemical application of antiserum against Tyr-D-Ala-Phe, a N-terminal tripeptide common to dermorphin/deltorphin family.
November 2000, Peptides,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Magic angle spinning NMR study of interaction of N-terminal sequence of dermorphin (Tyr-d-Ala-Phe-Gly) with phospholipids.
November 2012, Biochimica et biophysica acta,
T Sato, and N Takahashi, and K Tan-No, and K Kisara, and T Sakurada, and S Sakurada
Spinal antinociception: comparison of a dermorphin tetrapeptide analogue, [D-arginine2, sarcosine4]-dermorphin (1-4) and morphine in rats.
April 1990, Neuropharmacology,
Copied contents to your clipboard!