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The toad, ugly and venomous, wears yet a precious jewel in his skin
Current research on opioid receptor function.
The use of opioid analgesics has a long history in clinical settings, although the comprehensive action of opioid receptors is still less understood. Nonetheless, recent studies have generated freshExpand
Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide.
Nociceptin (NC) and some of its fragments as well as nociceptin-(1-13)-peptide amide [NC- (1-13)-NH2] and a series of its analogues were prepared and tested in the mouse vas deferens in an attempt toExpand
Human lung small-cell carcinoma contains bombesin.
The presence of immunoreactive bombesin in a human lung small-cell carcinoma grown in nude mice was established by several criteria: (i) Radioimmunoassay of tissue extracts for bombesin revealedExpand
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
Conversion of delta-opioid receptor antagonists containing the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) pharmacophore into potent delta-agonists requiredExpand
Synthesis of stereoisomeric analogues of endomorphin-2, H-Tyr-Pro-Phe-Phe-NH(2), and examination of their opioid receptor binding activities and solution conformation.
All sixteen stereoisomeric analogues of endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH(2)) were synthesized by Fmoc-strategy using solid phase methods. Although synthetic endomorphin-2 exhibited similar mu- andExpand
Selective d‐opioid receptor antagonist N,N(CH 3) 2 ‐Dmt‐Tic‐OH does not reduce ethanol intake in alcohol‐preferring AA rats
We studied the effect of a novel δ‐opioid receptor antagonist N,N(CH 3) 2 Dmt‐Tic‐OH (Me 2 ‐Dmt‐Tic‐OH) on voluntary ethanol intake in an alcohol‐preferring AA (Alko, Alcohol) rat line using a 4‐hourExpand
Physalaemin: an amphibian tachykinin in human lung small-cell carcinoma.
Immunoreactivity to the amphibian peptide physalaemin was characterized from extracts of a human lung small-cell carcinoma by immunological, chemical, and pharmacological means. Tumor-related peptideExpand
δ Opioidmimetic Antagonists: Prototypes for Designing a New Generation of Ultraselective Opioid Peptides
BackgroundTyr-Tic (1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) and Tyr-Tic-Ala were the first peptides with δ opioid antagonist activity lacking Phe, considered essential for opioid activityExpand
Evaluation of the Dmt-Tic pharmacophore: Conversion of a potent δ-opioid receptor antagonist into a potent δ agonist and ligands with mixed properties
Analogues of the 2‘,6‘-dimethyl-l-tyrosine (Dmt)−1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) pharmacophore were prepared to test the hypothesis that a “spacer” and a third aromatic centerExpand