The dermorphin peptide family

被引:79
作者
Melchiorri, P
Negri, L
机构
[1] Institute of Medical Pharmacology, University of Rome, La Sapienza, Rome
来源
GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1996年 / 27卷 / 07期
关键词
demorphins; peptides; analgesics; morphine;
D O I
10.1016/0306-3623(95)02149-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. In 1980, the skin of certain frogs belonging to the genus Phyllomedusinae was found to contain two new peptides that proved to be selective mu-opioid agonists. Given the name dermorphins, these were the first members of a peptide family that in the past 15 years has grown to reach a total of seven naturally occurring peptides and nearly 30 synthetic analogs. 2. Dermorphin peptides are potent analgesics in rodents and primates, including man. Some dermorphins can enter the blood-brain barrier and produce central antinociception after peripheral administration. 3. The dermorphin family also includes mu(1)-opioid receptor selective agonists that produce intense opioid analgesia, but stimulate pulmonary ventilation. 4. Experiments in rats and mice chronically exposed to dermorphins have shown that not only do they have higher antinociceptive efficacy and potency than morphine, but they are also less likely than morphine to produce tolerance, dependence and opiate side effects. Copyright (C) 1996 Elsevier Science Inc.
引用
收藏
页码:1099 / 1107
页数:9
相关论文
共 95 条
[1]  
ALLEGRA SP, 1982, EUR J PHARMACOL, V82, P223
[2]  
Aloisi F, 1982, Ann Ist Super Sanita, V18, P1
[3]  
AMBO A, 1994, CHEM PHARM BULL, V42, P888
[4]   PEPTIDE-TRANSPORT SYSTEMS FOR OPIATES ACROSS THE BLOOD-BRAIN-BARRIER [J].
BANKS, WA ;
KASTIN, AJ .
AMERICAN JOURNAL OF PHYSIOLOGY, 1990, 259 (01) :E1-E10
[5]   PASSAGE OF TYR-MIF-1 FROM BLOOD TO BRAIN [J].
BARRERA, CM ;
BANKS, WA ;
KASTIN, AJ .
BRAIN RESEARCH BULLETIN, 1989, 23 (06) :439-442
[6]   INTRATHECAL DERMORPHINE IN POSTOPERATIVE ANALGESIA [J].
BASSO, N ;
MARCELLI, M ;
GINALDI, A ;
DEMARCO, M .
PEPTIDES, 1985, 6 :177-179
[7]   DERMORPHIN, A NEW PEPTIDE FROM AMPHIBIAN SKIN, INHIBITS THE NOCICEPTIVE THALAMIC NEURONS FIRING RATE EVOKED BY NOXIOUS STIMULI [J].
BRAGA, PC ;
TIENGO, M ;
BIELLA, G ;
DALLOGLIO, G ;
FRASCHINI, F .
NEUROSCIENCE LETTERS, 1984, 52 (1-2) :165-169
[8]   PHARMACOLOGICAL DATA ON DERMORPHINS, A NEW CLASS OF POTENT OPIOID-PEPTIDES FROM AMPHIBIAN SKIN [J].
BROCCARDO, M ;
ERSPAMER, V ;
FALCONIERIERSPAMER, G ;
IMPROTA, G ;
LINARI, G ;
MELCHIORRI, P ;
MONTECUCCHI, PC .
BRITISH JOURNAL OF PHARMACOLOGY, 1981, 73 (03) :625-631
[9]   EFFECTS OF DERMORPHIN ON GASTROINTESTINAL TRANSIT IN RATS [J].
BROCCARDO, M ;
IMPROTA, G ;
NARGI, M ;
MELCHIORRI, P .
REGULATORY PEPTIDES, 1982, 4 (02) :91-96
[10]   CROSS-TOLERANCE BETWEEN DERMORPHIN AND MORPHINE TO ANALGESIA AND CATALEPSY IN RATS [J].
BROCCARDO, M ;
IMPROTA, G .
PEPTIDES, 1985, 6 :165-169