1 Mice lacking the mu-opioid receptor have been recently generated. Centrally mediated responses of mu-opioid agonists are suppressed whereas some of the delta-opioid responses are preserved in these mutant mice. 2 The vas deferens bioassay has been used in this study to investigate the functional activity at a peripheral level of mu- and delta-opioid agonists in mice lacking mu-opioid receptors. 3 The different mu-opioid agonists evaluated, morphine, DAMGO, dermorphin and [Lys(7)]dermorphin produced an inhibitory response in vas deferens from wild-type mice but had no relevant activity on vas deferens from mutant mice. 4 The selective delta-opioid agonists DPDPE, BUBU, deltorphin I, deltorphin II and [D-Met(2)]deltorphin induced inhibitory effects in vas deferens from both wild-type and mutant mice. However, the biological activities of these ligands were slightly reduced in preparations from mutant mice. The inhibitory responses of all these delta-opioid agonists were prevented by the administration of the selective delta-opioid antagonist naltrindole. 5 These data indicate that delta-opioid agonists, but not mu-opioid agonists, are biologically active in vas deferens from mice lacking mu-opioid receptors. The decreased response of delta-agonists in mutant mice suggests that some cooperativity may exist between mu- and delta-opioid receptors in these vas deferens preparations.

Activity of mu- and delta-opioid agonists in vas deferens from mice deficient in MOR gene / Rafael, Maldonado; Cintia, Severini; Hans W. D., Matthes; Brigitte L., Kieffer; Melchiorri, Pietro; Negri, Lucia. - In: BRITISH JOURNAL OF PHARMACOLOGY. - ISSN 0007-1188. - STAMPA. - 132:7(2001), pp. 1485-1492. [10.1038/sj.bjp.0703966]

Activity of mu- and delta-opioid agonists in vas deferens from mice deficient in MOR gene

MELCHIORRI, Pietro;NEGRI, Lucia
2001

Abstract

1 Mice lacking the mu-opioid receptor have been recently generated. Centrally mediated responses of mu-opioid agonists are suppressed whereas some of the delta-opioid responses are preserved in these mutant mice. 2 The vas deferens bioassay has been used in this study to investigate the functional activity at a peripheral level of mu- and delta-opioid agonists in mice lacking mu-opioid receptors. 3 The different mu-opioid agonists evaluated, morphine, DAMGO, dermorphin and [Lys(7)]dermorphin produced an inhibitory response in vas deferens from wild-type mice but had no relevant activity on vas deferens from mutant mice. 4 The selective delta-opioid agonists DPDPE, BUBU, deltorphin I, deltorphin II and [D-Met(2)]deltorphin induced inhibitory effects in vas deferens from both wild-type and mutant mice. However, the biological activities of these ligands were slightly reduced in preparations from mutant mice. The inhibitory responses of all these delta-opioid agonists were prevented by the administration of the selective delta-opioid antagonist naltrindole. 5 These data indicate that delta-opioid agonists, but not mu-opioid agonists, are biologically active in vas deferens from mice lacking mu-opioid receptors. The decreased response of delta-agonists in mutant mice suggests that some cooperativity may exist between mu- and delta-opioid receptors in these vas deferens preparations.
2001
delta-opioid receptor; deltorphins; dermorphins; knock out mice; morphine; mu-opioid receptor; synthetic peptides; vas deferens
01 Pubblicazione su rivista::01a Articolo in rivista
Activity of mu- and delta-opioid agonists in vas deferens from mice deficient in MOR gene / Rafael, Maldonado; Cintia, Severini; Hans W. D., Matthes; Brigitte L., Kieffer; Melchiorri, Pietro; Negri, Lucia. - In: BRITISH JOURNAL OF PHARMACOLOGY. - ISSN 0007-1188. - STAMPA. - 132:7(2001), pp. 1485-1492. [10.1038/sj.bjp.0703966]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/254021
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