MEDICINAL CHEMISTRY APPLIED TO PROBLEMS PROMINENT IN SENESCENCE

将哌唑嗪烷基化，该化合物是在 部分，并有可能永久绑定 肾上腺素能受体的α 1型，目前是 评估。 发现该化合物可逆地结合所有 这种类型的受体，但永久性结合仅建立在 一小部分人。 结果表明，α 1- 肾上腺素受体不是一个同质的群体， 分组将是必要的。 一种喹诺酮衍生物， 结合β-肾上腺素能受体。 这 这种化合物会触发受体，受体负责 “战或逃”的反应，并保持扣下扳机 在此期间。 在佛罗里达大学工作， 设计的正确性。 当β-肾上腺素受体 被这种化合物激活，它们不能被 加入β-受体阻滞剂，当 天然的可逆作用激素用于活化。 在哺乳动物的血液循环中， 在持续几集的背景水平之上， 小时，每天发生。 通过给予水溶性 睾酮的药物形式，在该科开发， 这些情节可以被模仿。 大学的研究人员 密苏里州利用这一准备工作， 雄激素敏感行为的睾酮发作， physiology.

Alkylating prazosin, a compound which was prepared in the Section last year and which has the potential to bind permanently to adrenergic receptors of the alpha1 type, was presently evaluated. This compound was found to bind reversibly to all receptors of this type but permanent binding was established only to a fraction of them. The results show that alpha1- adrenoceptors are not a homogenous group and division of these into subgroups will be necessary. A carbostyril derivative which fully activated and permanently binds to beta-adrenoceptors was designed and synthesized. This compound pulls the trigger of receptors, which are in charge of the "fight or flight" reaction, and keeps the trigger pulled down for the duration. Work at the University of Florida established the correctness of the design. When beta-adrenoceptors were activated by this compound they could not be deactivated by the addition of a beta-blocker, a deactivation which occurred when natural, reversibly acting hormones were used for the activation. Testosterone in the circulation of mammals rises several fold above its background levels during episodes lasting a couple of hours and occurring daily. By administration of the water soluble pharmaceutical form of testosterone, developed in the Section, these episodes may be imitated. Researchers at the University of Missouri used this preparation to establish the importance of testosterone episodes for androgen-sensitive behavior and physiology.