Compounds > enkephalin--ala(2)-mephe(4)-gly(5)-

enkephalin--ala(2)-mephe(4)-gly(5)- and Prostatic-Hyperplasia

enkephalin--ala(2)-mephe(4)-gly(5)- has been researched along with Prostatic-Hyperplasia* in 1 studies

Other Studies

1 other study(ies) available for enkephalin--ala(2)-mephe(4)-gly(5)- and Prostatic-Hyperplasia

Article	Year
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity. Bioorganic & medicinal chemistry letters, 1998, Sep-22, Volume: 8, Issue:18 The anti-anxiety agent ipsapirone has been shown to have modest affinity for alpha-1 receptors. We disclose the discovery of potent alpha-1a receptor subtype selective antagonists based on the ipsapirone structure which possess selectivity versus the 5-HT receptors tested. These antagonists were obtained by tethering a saccharin ring to 4-phenyl-3-carboxyethyl piperidines. The design principles which led to this structural motif are discussed. The synthesis of key analogs, their SAR, as well as results of selected in vitro and in vivo studies are described. Topics: Adrenergic alpha-1 Receptor Antagonists; Adrenergic alpha-Antagonists; Animals; Anti-Anxiety Agents; Drug Design; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalins; Humans; Male; Models, Chemical; Prostatic Hyperplasia; Pyrimidines; Rats; Receptors, Adrenergic, alpha-1; Stereoisomerism; Structure-Activity Relationship	1998

Article

Year

Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.

Bioorganic & medicinal chemistry letters, 1998, Sep-22, Volume: 8, Issue:18

The anti-anxiety agent ipsapirone has been shown to have modest affinity for alpha-1 receptors. We disclose the discovery of potent alpha-1a receptor subtype selective antagonists based on the ipsapirone structure which possess selectivity versus the 5-HT receptors tested. These antagonists were obtained by tethering a saccharin ring to 4-phenyl-3-carboxyethyl piperidines. The design principles which led to this structural motif are discussed. The synthesis of key analogs, their SAR, as well as results of selected in vitro and in vivo studies are described.

Topics: Adrenergic alpha-1 Receptor Antagonists; Adrenergic alpha-Antagonists; Animals; Anti-Anxiety Agents; Drug Design; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalins; Humans; Male; Models, Chemical; Prostatic Hyperplasia; Pyrimidines; Rats; Receptors, Adrenergic, alpha-1; Stereoisomerism; Structure-Activity Relationship

1998