ISSN:
1432-1912
Keywords:
α1Adrenoceptors
;
3H-WB 4101 binding
;
Prazosin
;
Desipramine
;
Rat vas deferens
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary 1. The binding of the α-adrenoceptor antagonist ligand, 3H-WB 4101, to membranes prepared from rat vas deferens is rapid, saturable and reversible. 2. Scatchard analyses of the data show the maximal number of binding sites (B max) to be 1.528±0.060 pmoles/g original wet tissue weight and a dissociation constant (Kd) of 0.84±0.07 nM. 3. Hill plots of the binding data revealed that 3H-WB 4101 binds to a single population of independent sites with no cooperative interactions. 4. The relative order of potencies of α-adrenoceptor antagonists for the inhibition of 3H-WB 4101 binding, prazosin 〉 phentolamine 〉 yohimbine, follows the pattern expected for the α1-type of adrenoceptors. 5. After repeated administration of prazosin to rats (0.4 mg/kg/day for 21 days), 3H-WB 4101 binding showed a significant increase in the density of α1-andrenoceptors (122% of controls). 6. Chronic treatment with desipramine (13.6 mg/kg/day for 22 days) resulted in a significant decrease in the number of α1-adrenoceptors (79% of controls).
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00503814
