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Abstract

Labeling by [3H]1,3-di(2-tolyl)guanidine of two high affinity binding sites in guinea pig brain: evidence for allosteric regulation by calcium channel antagonists and pseudoallosteric modulation by sigma ligands.

R B Rothman, A Reid, A Mahboubi, C H Kim, B R De Costa, A E Jacobson and K C Rice
Molecular Pharmacology February 1991, 39 (2) 222-232;
R B Rothman
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A Reid
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A Mahboubi
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C H Kim
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B R De Costa
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A E Jacobson
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K C Rice
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Abstract

Equilibrium binding studies with the sigma receptor ligand [3H]1,3-di(2-tolyl)guanidine ([3H]DTG) demonstrated two high affinity binding sites in membranes prepared from guinea pig brain. The apparent Kd values of DTG for sites 1 and 2 were 11.9 and 37.6 nM, respectively. The corresponding Bmax values were 1045 and 1423 fmol/mg of protein. Site 1 had high affinity for (+)-pentazocine, haloperidol, (R)-(+)-PPP, carbepentane, and other sigma ligands, suggesting a similarity with the dextromethorphan/sigma 1 binding site described by Musacchio et al. [Life Sci. 45:1721-1732 (1989)]. Site 2 had high affinity for DTG and haloperidol (Ki = 36.1 nM) and low affinity for most other sigma ligands. Kinetic experiments demonstrated that [3H]DTG dissociated in a biphasic manner from both site 1 and site 2. DTG and haloperidol increased the dissociation rate of [3H]DTG from site 1 and site 2, demonstrating the presence of pseudoallosteric interactions. Inorganic calcium channel blockers such as Cd2+ selectively increased the dissociation rate of [3H]DTG from site 2, suggesting an association of this binding site with calcium channels.

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Molecular Pharmacology
Vol. 39, Issue 2
1 Feb 1991
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Abstract

Labeling by [3H]1,3-di(2-tolyl)guanidine of two high affinity binding sites in guinea pig brain: evidence for allosteric regulation by calcium channel antagonists and pseudoallosteric modulation by sigma ligands.

R B Rothman, A Reid, A Mahboubi, C H Kim, B R De Costa, A E Jacobson and K C Rice
Molecular Pharmacology February 1, 1991, 39 (2) 222-232;

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Abstract

Labeling by [3H]1,3-di(2-tolyl)guanidine of two high affinity binding sites in guinea pig brain: evidence for allosteric regulation by calcium channel antagonists and pseudoallosteric modulation by sigma ligands.

R B Rothman, A Reid, A Mahboubi, C H Kim, B R De Costa, A E Jacobson and K C Rice
Molecular Pharmacology February 1, 1991, 39 (2) 222-232;
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