Medicinal Chemistry

source of progesterone as well as estrogens. Through its feedback effect on the hypothalamus, progesterone prevents ovulation an ...

and increases its oral potency. These medicinal chemistry advances were crucial to the design of oral contraceptive agents. Oral ...

Reduced incidence of cancer of the endometrium Reduced incidence of benign breast disease Reduced likelihood of functional ovar ...

effect). Androgens also control metabolic effects during growth in adolescence and stimulate protein synthesis (causing “nitroge ...

androgen that has been useful in the treatment of breast cancer in young women is the 2-methyl derivative of testosterone propio ...

scale. Testosterone enantate injections produced azoospermia in only 65% of males in a pivotal multicentre study. Danazol (5.59) ...

differing bioactivities, most clinical studies have been done on racemic mixtures. The optical isomers arise from the restricted ...

hormone-sensitive lipase and thus lipolysis. By promoting the supply of glucose from gluconeogenesis, inhibiting peripheral gluc ...

(and anti-inflammatory) actions but lacking in mineralocorticoid effects and side effects. Substituents added to the cortisol mo ...

the form of its acetomide (an acetone ketal), shows a 9α-fluoro group in addition to ∆^1 unsaturation, and a 16α-OH. It is used ...

syndrome of hypoadrenalism, called Addison’s disease, is lethal if not treated. The symptoms of this disease are weakness, anemi ...

to inhalation of a toxic chemical may cause so much swelling in the bronchial lining that the flow of air into the lung is block ...

5.14 PEPTIDE HORMONES: INTRODUCTION Peptides are polymers of amino acids. Each amino acid contributes three atoms (-N(-H)-Cα(-H, ...

into the single unified field of neuroendocrinology. Neuropeptides can mediate communication between neurons, either directly or ...

physiology provide drug designers with ample opportunities for interference with these processes. A final interesting facet conc ...

releasing factor, and prolactin inhibiting factor. A number of these hypothalamic hormones are important to the medicinal chemis ...

analogs can differentiate between pituitary and CNS receptors: homo-pyroGlu-His- Pro-NH 2 (5.70) is equipotent to TRH in the pit ...

GnRH agonists have a number of clinical uses. They induce ovulation and spermatogenesis, increasing gonadotropin and sex-steroid ...

5.15.2.5 Somatostatin Somatostatin (SS, growth hormone release-inhibiting hormone, GH-RIH) is perhaps the best investigated and ...

manipulation of the cysteines in SS analogs. When Cys^3 is replaced by its D-enantiomer, insulin release is preferentially inhib ...