ISSN:
0739-4462
Keywords:
housefly muscle
;
phencyclidine
;
calcium channel antagonists
;
Chemistry
;
Food Science, Agricultural, Medicinal and Pharmaceutical Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Biology
Notes:
The binding of [3H]phencyclidine ([3H]PCP) to a preparation of housefly thoracic muscle membranes was studied. Specific [3H]PCP binding saturated with both time and at concentrations of the radiolabeled ligand greater than 20 nM. One binding site with a KD of 10.7 nM and a Bmax of 3.9 pmol/mg protein was observed. Specific [3H]PCP binding was also readily reversible with a half-time of dissociation (t1/2) of 13.8 min and varied proportionately with tissue concentration. Of the drugs tested, specific [3H]PCP binding was inhibited by PCP analogs, antipsychotics, antidepressants, Ca2+ channel antagonists, and K+ channel blockers. [3H]PCP binding was unaffected by addition of carbamylcholine or L-glutamate in absence or presence of ATP, GTP, cAMP, or cGMP. Though the identity of the [3H]PCP binding protein in housefly muscle membranes is still unclear, it is more likely to be an ionic channel such as K+ or Ca2+ channels than a neurotransmitter receptor.
Additional Material:
4 Ill.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/arch.940020206
