Identification and regulation of alpha 2-adrenergic receptors in rabbit ileal mucosa.
The alpha 2-adrenergic receptors in rabbit ileal mucosal membranes can be identified by using [3H]clonidine. [3H]Clonidine bound to a homogeneous population of sites (30-120 fmoles/mg protein) with a KD of 2.2 nM at 25 degrees. Alpha-adrenergic agonists and antagonists competed with [3H] clonidine for the binding sites with an order of potency typical for alpha 2-receptors. Mg2+, Ca2+, or Mn2+ (2.4 mM) markedly increased the binding of [3H]clonidine. At the maximally effective concentration, Mg2+ increased both the binding affinity of [3H]clonidine and the number of receptor sites. Both NaCl and GppNHp, the guanyl nucleotide, inhibited [3H]clonidine binding. NaCl decreased the binding affinity of [3H]clonidine, with no appreciable effect on the number of receptor sites. These findings indicate that ileal mucosal alpha 2-receptors can exist in multiple affinity states, which can be regulated by divalent cations, NaCl, and guanyl nucleotides. It appears that NaCl and GppNHp regulate alpha 2-receptors in ileal mucosa by different mechanisms.
D000818:Animals; D002118:Calcium / Q000494:pharmacology; D003000:Clonidine / Q000378:metabolism; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology; D007082:Ileum / Q000032:analysis*; D007413:Intestinal Mucosa / Q000032:analysis; D008274:Magnesium / Q000494:pharmacology; D008297:Male; D008345:Manganese / Q000494:pharmacology; D011817:Rabbits; D011942:Receptors, Adrenergic, alpha / Q000032:analysis* / Q000187:drug effects; D012965:Sodium Chloride / Q000494:pharmacology; D014316:Tritium
D011942:Receptors, Adrenergic, alpha; D014316:Tritium; D006165:Guanylyl Imidodiphosphate; D008345:Manganese; D012965:Sodium Chloride; D008274:Magnesium; D003000:Clonidine; D002118:Calcium