Dactinomycin® Analogues as Neurokinin-2 Receptor Antagonists
| Autor: | A. B. Mauger, Jan M. Lundberg, Serge Auberson |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
DNA Replication
Male Agonist medicine.drug_class Health Toxicology and Mutagenesis Guinea Pigs Bronchi In Vitro Techniques Biology Toxicology chemistry.chemical_compound medicine Animals Receptor Pharmacology Dactinomycin DNA replication Biological activity Receptors Neurokinin-2 respiratory system Receptor antagonist nervous system chemistry Mechanism of action Biochemistry Female Neurokinin A medicine.symptom Muscle Contraction circulatory and respiratory physiology medicine.drug |
| Zdroj: | Pharmacology & Toxicology. 73:311-314 |
| ISSN: | 1600-0773 0901-9928 |
| DOI: | 10.1111/j.1600-0773.1993.tb01357.x |
| Popis: | Dactinomycin® 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. |
| Databáze: | OpenAIRE |
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