Identification and characterization of alpha 2-adrenergic receptors in human myometrium by [3H]rauwolscine binding.
Human myometrium contains alpha 3-adrenergic receptors which can be identified by binding of the alpha 2-adrenergic antagonist [3H]rauwolscine. Scatchard analysis of saturation binding data on myometrial membranes revealed that [3H]rauwolscine bound to a single class of noncooperative sites (262 +/- 89 fmol/mg of membrane protein) with high affinity (i.e., with an equilibrium dissociation constant of 5.3 +/- 2.2 nM). The alpha 2-adrenergic nature of these sites was derived from the order of potencies and stereospecificity of alpha-adrenergic agonists and antagonists to compete with [3H]rauwolscine binding.
D000316:Adrenergic alpha-Agonists / Q000378:metabolism; D000317:Adrenergic alpha-Antagonists / Q000378:metabolism; D001667:Binding, Competitive; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008566:Membranes / Q000378:metabolism; D009215:Myometrium / Q000378:metabolism*; D011941:Receptors, Adrenergic / Q000032:analysis*; D011942:Receptors, Adrenergic, alpha / Q000032:analysis*; D014599:Uterus / Q000378:metabolism*; D015016:Yohimbine
D000316:Adrenergic alpha-Agonists; D000317:Adrenergic alpha-Antagonists; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D015016:Yohimbine