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Role of the σ receptor in the inhibition of [ 3 H]‐noradrenaline uptake in brain synaptosomes and adrenal chromaffin cells
Author(s) -
Rogers Cheryl,
Lemaire Simon
Publication year - 1991
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1991.tb12352.x
Subject(s) - phencyclidine , sigma receptor , haloperidol , receptor , chemistry , spiperone , chromaffin cell , endocrinology , medicine , dopamine , adrenal medulla , biology , biochemistry , dopamine receptor , catecholamine , nmda receptor
1 Rat brain synaptosomes and cultured bovine adrenal chromaffin cells were used to monitor the inhibitory effects of phencyclidine (PCP) and sigma (σ)‐receptor ligands on the uptake of [ 3 H]‐noradrenaline ([ 3 H]‐NA). 2 A Na + ‐dependent high affinity uptake was observed in synaptosomes (30°C) and chromaffin cells (37°C) with K m of 0.22 and 0.56 μ m and V max of 2.5 pmol min −1 mg −1 protein and 0.7 pmol min −1 per 10 6 cells, respectively. 3 PCP and haloperidol inhibited the high affinity uptake with IC 50 of 0.17 and 0.42 μ m , respectively in synaptosomes and 0.24 and 0.47 μ m , respectively in adrenal chromaffin cells. 4 A close correlation ( r = 0.96) was established between the ability of various PCP and σ‐receptor ligands to inhibit [ 3 H]‐NA uptake in both systems: PCP > TCP > haloperidol > 3‐(+)‐PPP > MK‐801 ≥ (−)‐butaclamol > (+)‐SKF‐10047 > DTG. Spiperone and opioid receptor ligands were ineffective at 20 μ m . 5 These results indicate that the central and peripheral inhibitory effects of PCP and σ‐receptor ligands on [ 3 H]‐NA uptake involves a receptor (σ 1 ‐like) which is distinct from that (PCP 2 ) recognized for the inhibition of [ 3 H]‐dopamine uptake by PCP.