Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.
Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed.
Models, Chemical↗
Biomedical subjects
H Broughton
Publications and source records attributed to H Broughton.
Photoaffinity labeling of the benzodiazepine binding site of alpha1beta3gamma2 gamma-aminobutyric acidA receptors with flunitrazepam identifies a subset of ligands that interact directly with His102 of the alpha subunit and predicts orientation of these within the benzodiazepine pharmacophore.
Photoincorporation of ligands into the benzodiazepine site of native gamma-aminobutyric acidA (GABAA) receptors provides useful information about the nature of the benzodiazepine (BZ) binding site. Photoincorporation of flunitrazepam into a single population of GABAA receptors, recombinant human alpha1beta3gamma2, was investigated to probe further the mechanism and orientation of flunitrazepam and other ligands in the BZ binding site. It was concluded that the receptor is primarily derivatized with the entire, unfragmented, flunitrazepam molecule, which undergoes a conformational change during photolysis and largely vacates the benzodiazepine binding site. Investigation of the BZ site after photoincorporation of [3H]flunitrazepam confirmed that binding of other radioligands was unaffected by incorporation of flunitrazepam. This did not correlate with their efficacy but depended on the presence of particular structural features in the molecule. It was observed that affected compounds have a pendant phenyl moiety, analogous to the 5-phenyl group of flunitrazepam, which are proposed to overlap and interact with the same residue or residues in the BZ binding site. Because the major site of flunitrazepam photoincorporation has been shown to be His102, we propose that this group of compounds interacts directly with His 102, whereas compounds of other structural types have no direct interaction with this amino acid. The orientation of ligands within the BZ binding site and their specific interaction with identified amino acids are not well understood. The data in the current study indicate that His102 interacts directly with the pendant phenyl group of diazepam, and further implications for the pharmacophore of the BZ binding site are discussed.
Azides↗
Medical knowledge systems: applications to telemedicine.
The application and form of electronically stored medical knowledge has a direct impact on the design of any healthcare delivery system. For those who plan for remote medical care or who work at the disaster relief level, there are specific requirements which will dictate the type of knowledge required and the vehicle best suited to deliver that information. The PC based multimedia biomedical library developed for NASA was originally intended for long-term space missions where complete isolation from each support was a distinct possibility. The library is a combination of traditional references and secondary databases structured within a primary care physician's workstation. The integration of the library and a point-of-care system allows optimal use of both resources and provides a basic building block for telemedicine networking.
Artificial Intelligence↗
Valuing life and death.
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Attitude to Death↗
The shift to wellness.
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Attitude to Health↗
Straight ahead.
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Anniversaries and Special Events↗
Winning isn't everything.
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Athletic Injuries↗
Earthbound applications for NASA's physician workstation.
The dream of a space probe to Mars or an astronaut colony on the moon persists. Despite years of setbacks and delays, NASA continues to lay the foundation for a new frontier in space. The necessity of a self contained health maintenance facility is an integral part of this stellar venture. As a subsystem of this health maintenance facility, the physician or astronaut workstation was envisioned as the vehicle of interface between the computer resources of the space station and the care provider. Our efforts to define and build this interface have resulted in a series of programs which can now be tested and refined using earth-based applications. The modules which have dual-use application from the NASA workstation include: patient scheduling and master patient index, pharmacy, laboratory, medical library, problem list/progress notes, and digital medical records. Our current plan is to develop these tools as objects that can be assembled in a variety of configurations. This will allow the technology to be used by the private sector where each doctor can select the starting point of his outpatient office system and add modules as he makes progress in system integration and training.
Aerospace Medicine↗
Beyond comprehension.
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Fatigue Syndrome, Chronic↗
Social security benefits [continuing nursing education].
There is a wide range of benefits available for patients, clients and carers, and, in April this year two new benefits for disabled people were introduced together with new ways of claiming them. Is a knowledge of benefits necessary for a few nurse specialists only, or is it an integral part of professional practice for all?
Education, Nursing, Continuing↗