TY - JOUR
T1 - Amitriptyline
T2 - Long-term treatment elevates α-adrenergic and muscarinic receptor binding in mouse brain
AU - Rehavi, Moshe
AU - Ramot, Orly
AU - Yavetz, Bella
AU - Sokolovsky, Mordechai
PY - 1980/8/4
Y1 - 1980/8/4
N2 - The effects of long-term treatment of the tricyclic antidepressant drug, amitriptyline, on α-adrenergic, muscarinic and dopaminergic receptor binding were studied in mouse brain. No changes could be observed after 7 or 14 days of amitriptyline administration, but after 21 days a two-fold increase in α-adrenergic binding was detected in the medulla pons and in the hippocampus using [3H]WB-4101 as the binding ligand. In the same regions, a moderate increase in muscarinic receptor binding (25%) as measured by [3H]4NMPB was seen, while no change was detected in dopaminergic receptor binding measured by [3H]spiperone. Scatchard analysis reveals that the increases in receptor densities are not a result of changes in the dissociation constants of the tritiated drugs for their receptors. It is suggested that the increase in α-adrenergic as well as in muscarinic binding is a consequence of a chronic blockade of these two types of receptors by amitriptyline in vivo.
AB - The effects of long-term treatment of the tricyclic antidepressant drug, amitriptyline, on α-adrenergic, muscarinic and dopaminergic receptor binding were studied in mouse brain. No changes could be observed after 7 or 14 days of amitriptyline administration, but after 21 days a two-fold increase in α-adrenergic binding was detected in the medulla pons and in the hippocampus using [3H]WB-4101 as the binding ligand. In the same regions, a moderate increase in muscarinic receptor binding (25%) as measured by [3H]4NMPB was seen, while no change was detected in dopaminergic receptor binding measured by [3H]spiperone. Scatchard analysis reveals that the increases in receptor densities are not a result of changes in the dissociation constants of the tritiated drugs for their receptors. It is suggested that the increase in α-adrenergic as well as in muscarinic binding is a consequence of a chronic blockade of these two types of receptors by amitriptyline in vivo.
KW - amitriptyline
KW - chronic treatment
KW - muscarinic
KW - α-adrenoreceptor
UR - http://www.scopus.com/inward/record.url?scp=0018885797&partnerID=8YFLogxK
U2 - 10.1016/0006-8993(80)91224-X
DO - 10.1016/0006-8993(80)91224-X
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AN - SCOPUS:0018885797
SN - 0006-8993
VL - 194
SP - 443
EP - 453
JO - Brain Research
JF - Brain Research
IS - 2
ER -