morphine and neurotensin-(8-13)

morphine has been researched along with neurotensin-(8-13)* in 1 studies

Other Studies

1 other study(ies) available for morphine and neurotensin-(8-13)

Article	Year
Identification and functional characterization of a stable, centrally active derivative of the neurotensin (8-13) fragment as a potential first-in-class analgesic. Journal of medicinal chemistry, 2010, Jun-24, Volume: 53, Issue:12 The neurotensin hexapapetide fragment NT(8-13) is a potent analgesic when administered directly to the central nervous system but does not cross the blood-brain barrier. A total of 43 novel derivatives of NT(8-13) were evaluated, with one, ABS212 (1), being most active in four rat models of pain when administered peripherally. Compound 1 binds to human neurotensin receptors 1 and 2 with IC(50) of 10.6 and 54.2 nM, respectively, and tolerance to the compound in a rat pain model did not develop after 12 days of daily administration. When it was administered peripherally, serum levels and neurotensin receptor binding potency of 1 peaked within 5 min and returned to baseline within 90-120 min; however, analgesic activity remained near maximum for >240 min. This could be due to its metabolism into an active fragment; however, all 4- and 5-mer hydrolysis products were inactive. This pharmacokinetic/pharmacodynamic dichotomy is discussed. Compound 1 is a candidate for development as a first-in-class analgesic. Topics: Analgesics; Animals; Binding, Competitive; Body Temperature; Calcium; Cell Line; Drug Tolerance; Humans; Male; Neurotensin; Oligopeptides; Pain Measurement; Peptide Fragments; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, Neurotensin; Structure-Activity Relationship	2010

Article

Year

Identification and functional characterization of a stable, centrally active derivative of the neurotensin (8-13) fragment as a potential first-in-class analgesic.

Journal of medicinal chemistry, 2010, Jun-24, Volume: 53, Issue:12

The neurotensin hexapapetide fragment NT(8-13) is a potent analgesic when administered directly to the central nervous system but does not cross the blood-brain barrier. A total of 43 novel derivatives of NT(8-13) were evaluated, with one, ABS212 (1), being most active in four rat models of pain when administered peripherally. Compound 1 binds to human neurotensin receptors 1 and 2 with IC(50) of 10.6 and 54.2 nM, respectively, and tolerance to the compound in a rat pain model did not develop after 12 days of daily administration. When it was administered peripherally, serum levels and neurotensin receptor binding potency of 1 peaked within 5 min and returned to baseline within 90-120 min; however, analgesic activity remained near maximum for >240 min. This could be due to its metabolism into an active fragment; however, all 4- and 5-mer hydrolysis products were inactive. This pharmacokinetic/pharmacodynamic dichotomy is discussed. Compound 1 is a candidate for development as a first-in-class analgesic.

Topics: Analgesics; Animals; Binding, Competitive; Body Temperature; Calcium; Cell Line; Drug Tolerance; Humans; Male; Neurotensin; Oligopeptides; Pain Measurement; Peptide Fragments; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, Neurotensin; Structure-Activity Relationship

2010