Desipramine modulation of sigma and opioid peptide receptor expression in glial cells.
Exposure of C6 glial cell cultures to desipramine induced the appearance of opioid receptors and up-regulated sigma receptors. Opioid binding was demonstrated with 3H-etorphine and 3H-dihydromorphine (DHM), but was not observed with the mu, delta and kappa ligands 3H-DAMGE, 3H-DADLE or 3H-(-)ethylketocyclazocine in the presence of specific blockers, respectively. Competition experiments with 3H-DHM and either (-)naloxone or (+)naloxone indicated the presence of authentic opioid receptors. In similar studies with beta-endorphin, its truncated form (1-27) or their N-acetyl derivatives, beta-endorphin proved to have the highest affinity. Opioid receptors in glial cell aggregates were primarily kappa, with few mu and delta sites. Desipramine increased Bmax values for kappa but not mu and delta.
Barg
J
J
E. A. Doisy Department of Biochemistry and Molecular Biology, St. Louis University School of Medicine, MO 63104.
Belcheva
M M
MM
Bem
W T
WT
Lambourne
B
B
McLachlan
J A
JA
Tolman
K C
KC
Johnson
F E
FE
Coscia
C J
CJ
D000818:Animals; D001665:Binding Sites; D003891:Desipramine / Q000494:pharmacology*; D004090:Dihydromorphine / Q000378:metabolism; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D016308:Enkephalin, Leucine-2-Alanine / Q000378:metabolism; D004745:Enkephalins / Q000378:metabolism; D016314:Ethylketocyclazocine / Q000378:metabolism; D005048:Etorphine / Q000378:metabolism; D009457:Neuroglia / Q000166:cytology / Q000187:drug effects*; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects* / Q000378:metabolism; D017473:Receptors, Opioid, kappa; D017480:Receptors, sigma; D015854:Up-Regulation
D004745:Enkephalins; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D017480:Receptors, sigma; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D005048:Etorphine; D016314:Ethylketocyclazocine; D016308:Enkephalin, Leucine-2-Alanine; D004090:Dihydromorphine; D003891:Desipramine