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Ken Jones

Publications and source records attributed to Ken Jones.

6 recordsLinked to original sources

New highly potent and selective adenosine A(3) receptor antagonists.

A class of potent, selective adenosine A(3) receptor antagonists was obtained via optimisation of the screening hit N-[4-(4-methoxyphenyl)-thiazol-2-yl]-acetamide. Structural modifications of this hit revealed very quickly that a 5-(pyridin-4-yl) substituent on the 2-aminothiazole ring was optimal for high potency at the adenosine A(3) receptor. Structure activity relationship studies led to both potent and selective A(3) receptor antagonists, including N-[5-pyridin-4-yl-4-(3,4,5-trimethoxyphenyl)-thiazol-2-yl]-acetamide, a highly potent aden-osine A(3) receptor antagonist with greater than 100- fold selectivity against the related adenosine receptors. As well as demonstrating selective in vitro binding on the human A(3) adenosine receptor, this compound was also shown to selectively block the rat A(3) receptor in vivo. This important new compound can be readily synthesised in four steps from commercially available starting materials.

Acetamides↗

I, too, have a dream.

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Dentist-Patient Relations↗

Modulation of melanogenesis by aloesin: a competitive inhibitor of tyrosinase.

Aloesin, [2-acetonyl-8-beta-d-glucopyranosyl-7-hydroxy-5-methylchromone], a compound isolated from the Aloe plant, is shown in these studies to modulate melanogenesis via competitive inhibition of tyrosinase. Aloesin inhibits purified tyrosinase enzyme and specifically inhibits melanin production in vitro. Enzyme kinetics studies using normal human melanocyte cell lysates and cell-based melanin production demonstrated that aloesin is a competitive inhibitor of tyrosinase from mushroom, human and murine sources. Tyrosine hydroxylase and 3,4-dihydroxyphenylalanine (DOPA) oxidase activities of tyrosinase from normal human melanocyte cell lysates were inhibited by aloesin in a dose dependent manner. In a percutaneous absorption study a finite dose of aloesin penetrated the skin slowly and was recovered primarily in the surface wash. Aloesin shows promise as a pigmentation-altering agent for cosmetic or therapeutic applications.

Absorption↗

Shrinking away from psychiatry? A survey of Australian medical students' interest in psychiatry.

OBJECTIVE: We sought to examine the attitudes of newly recruited medical students towards psychiatry and other specialties to determine what factors influence their career choice options. METHOD: We surveyed the attitudes of 655 medical students using a 31-item self-report questionnaire. RESULTS: Australian medical students rated the ability to help patients as the most important aspect of a specialty in determining their choice. Attraction to psychiatry was based on the specialty being interesting and intellectually challenging,and providing a career that promised job satisfaction with good prospects and enjoyable work. Females expressed a greater interest in psychiatry and were more likely to consider pursuing it as a career, principally due to a greater interest in the subject matter and a stronger desire for interaction with patients. The least attractive aspects of psychiatry were its lack of prestige among the medical community and a perceived absence of a scientific foundation. CONCLUSION: The attitudes of medical students can perhaps be modified and recruitment into psychiatry enhanced by presenting the reality of psychiatry today - namely the wide range of available therapeutic processes, the predominantly positive outcomes, the interesting and intellectually challenging nature of the subject and its nurturing and accommodating work environment.

Adult↗