DACTINOMYCIN(R) ANALOGS AS NEUROKININ-2 RECEPTOR ANTAGONISTS

被引：4

作者：

AUBERSON, S

MAUGER, AB

LUNDBERG, JM

机构：

[1] MED RES INST,WASHINGTON,DC 20010

[2] CANTONAL UNIV HOSP,OTORHINOLARYNGOL CLIN & POLICLIN,CH-1211 GENEVA,SWITZERLAND

来源：

PHARMACOLOGY & TOXICOLOGY | 1993年 / 73卷 / 06期

关键词：

D O I：

10.1111/j.1600-0773.1993.tb01357.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Dactinomycin(R) has recently been shown to be a competitive neurokinin-2 receptor antagonist in addition to its inhibiting action on DNA replication. We investigated in the isolated guinea-pig bronchi the action of 3 Dactinomycin analogues on the contractions evoked by the selective neurokinin-2 receptor agonist [Nle10] neurokinin A(4-10). These analogues included 4,4'-Gly-Dactinomycin and the single peptide lactone of dactinomycin which are inactive on DNA replication and 5,5'-MeLeu-Dactinomycin, which has potent antitumour activity. Independently of their known effect on DNA replication, the three analogues showed neurokinin-2 antagonistic activity which was lower than for Dactinomycin.

引用

收藏

页码：311 / 314

页数：4

相关论文

共 18 条

[1] THE TACHYKININS - A FAMILY OF PEPTIDES WITH A BROOD OF RECEPTORS [J].

BUCK, SH ;

BURCHER, E .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1986, 7 (02) :65-68

[2]

CASINI A, 1989, N-S ARCH PHARMACOL, V339, P354

[3] DACTINOMYCIN IS A COMPETITIVE NEUROKININ-2 RECEPTOR ANTAGONIST [J].

DELAYGOYET, P ;

LUNDBERG, JM .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 180 (03) :1342-1349

[4] A POTENT AND SELECTIVE NONPEPTIDE ANTAGONIST OF THE NEUROKININ-A (NK2) RECEPTOR [J].

EMONDSALT, X ;

VILAIN, P ;

GOULAOUIC, P ;

PROIETTO, V ;

VANBROECK, D ;

ADVENIER, C ;

NALINE, E ;

NELIAT, G ;

LEFUR, G ;

BRELIERE, JC .

LIFE SCIENCES, 1992, 50 (15) :PL101-PL106

[5] EFFECTS OF ACTINOMYCIN-D ON AIRWAY CONSTRICTION INDUCED BY TACHYKININS AND CAPSAICIN IN GUINEA-PIGS [J].

FUJII, T ;

MURAI, M ;

MORIMOTO, H ;

NISHIKAWA, M ;

KIYOTOH, S .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 194 (2-3) :183-188

[6]

GLAUBIGER D, 1982, PHARM PRINCIPLES CAN, P402

[7]

KERSTEN H, 1974, INHIBITORS NUCLEIC A, P40

[8] SELECTIVE-INHIBITION BY DACTINOMYCIN OF NANC SENSORY BRONCHOCONSTRICTION AND [I-125] NKA BINDING DUE TO NK-2 RECEPTOR ANTAGONISM [J].

LOU, YP ;

DELAYGOYET, P ;

LUNDBERG, JM .

ACTA PHYSIOLOGICA SCANDINAVICA, 1992, 144 (03) :221-231

[9] DACTINOMYCIN INHIBITS NONCHOLINERGIC BRONCHOCONSTRICTION BY CAPSAICIN-SENSITIVE SENSORY NERVES IN THE GUINEA-PIG BY ANTAGONIZING NEUROKININ-2 RECEPTOR ACTIVATION [J].

LUNDBERG, JM ;

LOU, YP .

ACTA PHYSIOLOGICA SCANDINAVICA, 1991, 141 (01) :141-142

[10] SYNTHESIS AND PROPERTIES OF SOME PEPTIDE ANALOGS OF ACTINOMYCIN-D [J].

MAUGER, AB ;

STUART, OA ;

KATZ, E .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (04) :1297-1301