DADLE

Development in Dadle Steelmaking and Continuous Casting, Canadian Institute of Mining, Metallurgy and Petroleum, Montreal, Quebec, Canada, 1990. 

R. J. Fmehan, Dadle Metallurgy Principles and Practices, Iron and Steel Society, Warrendale, Pa., 1985. 

Inhibition constants (Kj) of 26 narcotic analgesic agonists and antagonists as obtained in 4 receptor binding tests (EKC, DHM, DADLE and NAL) [45],... 

Fig. 37.4. Spectral map of the 26 opioid agonists and antagonists in 4 receptor binding tests, as described by Table 37.7 [45, 46]. Circles refer to the compounds. Squares represent the binding tests. Areas of circles and squares are proportional to the marginal mean affinities in the table. The lines that join the three poles (DHM, DADLE and EKC) of the map represent axes of contrast between the p-, 8-and K-opioid receptors. The horizontal and vertical components represent 18 and 79%, respectively, of the interaction in the data.

The spectral map shows three distinct poles of specificity. These are respectively the p-receptor (DHM), the 6-receptor (DADLE) and the K-receptor (EKC). The naloxone receptor (NAL) appears to be strongly correlated with the p-receptor (DHM) and, hence, provides little additional information. In spectral map analysis, correlation between variables, as well as similarity between compounds, is evidenced by the proximity of their corresponding symbols. The lines drawn through the three poles of the map represent bipolar axes of contrast. A contrast is defined in this context as a log ratio or, equivalently, as a difference of logarithms. For example, the horizontal axis through the p- and 8-receptors defines the p/6 contrast. Compounds that project on the right side of this axis bind more specifically to the p-receptor, while those that project on the left side possess more... 

Tang, F., Borchardt, R. T., Characterization of the efflux transport(s) responsible for restricting intestinal mucosa permeation of acyloxy-alkoxy-based cyclic prodrug of the opioid peptide DADLE, Pharm Res. 2002, 19, 780-786. 

DALAMID [D-Ala2]Leu-enkephalin DADL(E) [D-Ala2,D-Leu5]enkephalin DSL(E)T [D-Ser Thr enkephalin DTLET [D-Thr2,Leu5,Thr6]enkephalin... 

Uchiyama, T., Kotani, A., Tasumi, H., et al. Development of novel lipophilic derivatives of DADLE (leucine enkephalin analogue) Intestinal permeability characteristics of DADLE derivatives in rats. Pharm. Res. 17 1461-1467, 2000. 

Yang, J.Z.,W. Chen, and R.T. Borchardt. 2002. In vitro stability and in vivo pharmacokinetic studies of a model opioid peptide, H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE), and its cyclic prodrugs. 

This hypothesis of delta receptors in the mouse vas deferens was later further substantiated by the observation of the lack of cross-tolerance between a stable enkephalin analog [D-Ala2, D-leu5]enkephalin (DADLE, see below) and sulphentanyl (a mu agonist) in this tissue after chronic administration in vivo [8]. 

STABLE ENKEPHALIN ANALOGUES [D-Ala2, D-Leu5] ENKEPHALIN (DADLE) AND [D-Ala2, N-Me-Phe4, Met(0)5-ol]ENKEPHALIN (FK 33-824) ARE SELECTIVE DELTA AND MU AGONISTS, RESPECTIVELY... 

An examination of the structure-activity relationship (SAR) of a series of enkephalin analogues and morphine derivatives in competing with the binding of radioisotope labeled DADLE and FK 33-824 or opiates revealed that DADLE binds to an opioid receptor selective to Leu-enkephalin and its analogues. In contrast, FK 33-824, morphine, or naloxone binds to opioid receptors with selectivity in favor of morphine and derivatives simi-... 

W284K Decreased for DADLE and DTLET MAPK activation by DADLE... 

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