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Biomedical subjects

M A Ashwell

Publications and source records attributed to M A Ashwell.

7 recordsLinked to original sources
PubMed2001

4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor.

The preparation and structure-activity relationships (SARs) of potent agonists of the human beta(3)-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human beta(3)-AR potency with selectivity over human beta(1)-AR and/or human beta(2)-AR agonism. Compound 29s was identified as a potent (EC(50)=1nM) and selective (greater than 400-fold over beta(1)- with no beta(2)-AR agonism) full beta(3)-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.

Adrenergic beta-3 Receptor Agonists↗
PubMed2000

The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.

Ionizable groups were introduced onto the 10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine scaffold of the vasopressin V2-antagonist WAY-VPA-985 in the search for molecules optimized for parenteral formulation. The synthesis and structure activity relationships (SAR) are presented together with solubility data in a model parenteral system. The amine, WAY-140288 (4f), was chosen for further development. p6

Antidiuretic Hormone Receptor Antagonists↗
PubMed1980

Predisposition to obesity.

65 women whose build ranged from normal to grossly obese were investigated to test the hypothesis that obese people, especially those with a genetic predisposition to obesity (manifest by early onset and family history of obesity), have a low energy expenditure. For the group as a whole, resting metabolic rate was related to obesity index, but the age of onset and family history of obesity had no effect on this relationship. The findings suggest that a familial predisposition to obesity is more likely to relate to energy intake than to energy expenditure.

Adolescent↗