PubMed · 8666565
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G D Gammon. 1996. Incentive bias?. https://pubmed.ncbi.nlm.nih.gov/8666565/
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Derivatives of dolichyl phosphate (Dol-P) with 2-aminopyridine or 1-aminonaphtalene fluorophore groups at the omega-end of the chain were synthesized. These products serve as substrates for recombinant yeast Dol-P-mannose synthase. Fluorescence resonance energy transfer between a Trp residue of the enzyme and the 1-aminonaphtalene group of the Dol-P analogue was demonstrated.
BACKGROUND AND OBJECTIVE: We are currently working with a novel class of photoactivated 4-amino substituted 1,8-naphthalimide compounds for tissue bonding. With promising results in other tissues, we are pursuing potential vascular applications. This study focused on determining the appropriate compound formulation(s), concentration, and exposure times to optimize penetration of the heterogeneous arterial wall. STUDY DESIGN/MATERIALS AND METHODS: Segments of atheromatous rabbit carotid artery were immersed in hydrophilic or lipophilic forms of the compound, then frozen, cryosectioned, and examined by confocal microscopy. RESULTS: The hydrophilic compound exhibited preferential localization within the intima and media and limited presence in the adventitia. Conversely, the lipophilic compound concentrated in the intima and adventitia with virtual exclusion from the media. Exposure to both forms resulted in complete penetration of the arterial wall. CONCLUSION: These results extend our knowledge and permit a more practical approach to potential vascular applications using these photoactivated compounds for tissue bonding.
In early studies, we have reported the synthesis and biological activities of several cyclic imides. The present study describes the analgesic activity of 1,8-naphthalimide and 1,4,5,8-naphthalenediimide derivatives in a standard murine model of analgesia. The pharmacological results show that all compounds studied, given intraperitoneally, produced significant inhibition of acetic acid-induced abdominal constrictions. At the ID50 (micromol/kg) level, these cyclic imide derivatives were about 40-270-fold more potent in this assay than aspirin and acetaminophen, two well-known and widely used analgesics. These results extend previous studies on the analgesic activity of cyclic imides.