Opiate-like peptides. Part VIII. Methylamides and dimethylamides of [D-Leu5]-enkephalin and [D-Ala2, D-Leu5]-enkephalin. Synthesis and analgesic activity. 1986

K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski

Syntheses of [D-Ala2, D-Leu5]-enkephalin, methyl ester of [D-Ala2, D-Leu3]-enkephalin, methylamides and dimethylamides of [D-Leu5]-enkephalin and [D-Ala2, D-Leu5]-enkephalin are described together with their analgesic activity determined on the basis of four analgesic tests: the hot-plate method, the reaction to electric stimulus, the tail immersion test and the frequency of writhing syndrome test. The neurotoxicity was estimated by the rota-rod test. The most pronounced analgesic effect was induced by compound: [D-Ala2, D-Leu5]-enkephalin, [D-Ala2, D-Leu5-OMe]-enkephalin and [D-Ala2, D-Leu5-NMe2]-enkephalin. In the tail immersion test all analogs did not exhibit analgesic activity.

UI MeSH Term Description Entries
D008297 Male Males
D009422 Nervous System Diseases Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle. Neurologic Disorders,Nervous System Disorders,Neurological Disorders,Disease, Nervous System,Diseases, Nervous System,Disorder, Nervous System,Disorder, Neurologic,Disorder, Neurological,Disorders, Nervous System,Disorders, Neurologic,Disorders, Neurological,Nervous System Disease,Nervous System Disorder,Neurologic Disorder,Neurological Disorder
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D004743 Enkephalin, Leucine One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN. Leucine Enkephalin,5-Leucine Enkephalin,Leu(5)-Enkephalin,Leu-Enkephalin,5 Leucine Enkephalin,Enkephalin, 5-Leucine,Leu Enkephalin
D004744 Enkephalin, Methionine One of the endogenous pentapeptides with morphine-like activity. It differs from LEU-ENKEPHALIN by the amino acid METHIONINE in position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN. Methionine Enkephalin,5-Methionine Enkephalin,Met(5)-Enkephalin,Met-Enkephalin,5 Methionine Enkephalin,Enkephalin, 5-Methionine,Met Enkephalin
D005260 Female Females
D000700 Analgesics Compounds capable of relieving pain without the loss of CONSCIOUSNESS. Analgesic,Anodynes,Antinociceptive Agents,Analgesic Agents,Analgesic Drugs,Agents, Analgesic,Agents, Antinociceptive,Drugs, Analgesic
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
D016308 Enkephalin, Leucine-2-Alanine A delta-selective opioid (ANALGESICS, OPIOID). It can cause transient depression of mean arterial blood pressure and heart rate. 2-Alanyl-Leucine Enkephalin,5-Leucine-2-Alanine Enkephalin,D-Ala(2)-D-Leu(5)-Enkephalin,Enkephalin-Leu,Ala(2),Leucine Enkephalin-2-Alanine,BW-180C,DADLE,Leu-Enkephalin-2-Ala,2 Alanyl Leucine Enkephalin,5 Leucine 2 Alanine Enkephalin,BW 180C,BW180C,Enkephalin, 2-Alanyl-Leucine,Enkephalin, 5-Leucine-2-Alanine,Enkephalin, Leucine 2 Alanine,Enkephalin-2-Alanine, Leucine,Leu Enkephalin 2 Ala,Leucine Enkephalin 2 Alanine,Leucine-2-Alanine Enkephalin
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

Related Publications

K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
June 1983, Life sciences,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
January 1984, Polish journal of pharmacology and pharmacy,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
June 1996, Acta crystallographica. Section C, Crystal structure communications,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
January 1991, Polish journal of pharmacology and pharmacy,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
September 1983, The Journal of biological chemistry,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
October 1983, Il Farmaco; edizione scientifica,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
November 1985, Pain,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
October 1981, Life sciences,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
January 1982, International journal of peptide and protein research,
K Rolka, and K Kolasa, and Z Kleinrok, and G Kupryszewski
August 1984, Biulleten' eksperimental'noi biologii i meditsiny,
Copied contents to your clipboard!