Pharmacological Characterization of Sigma Binding Sites in Guinea Pig Brain Membranes

1991 ◽  
pp. 51-59 ◽  
Author(s):  
E. W. Karbon ◽  
S. J. Enna
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Pharmacological Characterization ◽  
Brain Membranes ◽  
Pig Brain ◽  
Guinea Pig Brain

Pharmacological characterization of the binding of [3H]bremazocine in guinea-pig brain: evidence for multiplicity of the κ-opioid receptors

1989 ◽  
Vol 67 (10) ◽  
pp. 1336-1344 ◽  
Author(s):  
Mario Tiberi ◽  
Jacques Magnan
Keyword(s):  
Guinea Pig ◽  
Opioid Receptors ◽  
Binding Sites ◽  
Binding Capacity ◽  
Pharmacological Characterization ◽  
Homogeneous Population ◽  
Site Model ◽  
Pig Brain ◽  
Guinea Pig Brain

In guinea-pig brain, [3H]bremazocine has a binding capacity of 27.2 pmol/g wet tissue, which is statistically different from that of [3H]ethylketazocine (14.7 pmol/g wet tissue) or the sum of the individual binding capacities of μ-, δ-, and κ-selective ligands (15.0 pmol/g wet tissue). Saturation studies of [3H]bremazocine performed in the presence of unlabelled μ-, δ-, and κ-blockers still reveal a homogeneous population of binding sites. [3H]Bremazocine under suppressed conditions displays at these sites a Kd of 2.51 nM with a binding capacity of 9.15 pmol/g wet tissue. We have performed the pharmacological characterization of these additional opioid binding sites. Displacement curves measured with a number of opioid substances were all best fitted to a one-site model. The stereoselectivity of these additional sites was demonstrated by using two groups of stereoisomers. Oripavine and benzomorphan opioids were among the most potent drugs at the [3H]bremazocine sites (μ + δ + κ suppressed). Diprenorphine, bremazocine, cyclazocine, and ethylketazocine displayed apparent affinities constants (1/Ka) of 8.66, 7.57, 21.4, and 38.0 nM, respectively at those sites. The κ-selective drugs U50488, U69593, PD117302, and tifluadom were inhibitors of the binding of [3H]bremazocine at these sites with apparent affinities of 113, 268, 76.9, and 47.9 nM. All μ- or δ-selective drugs tested in this study have caused weak or no inhibition of the binding. Correlation analyses were done between the different affinities measured at the [3H]bremazocine sites (μ + δ + κ suppressed) and those observed at the known μ-, δ-, and κ-sites of the guinea-pig brain. The results were highly and significantly correlated with the κ-binding profile, while no correlation could be established with the μ,- or δ-binding profiles. Moreover, the results reported here do not correspond to a pharmacological profile that belongs to the σ- or ε-receptors. Thus, it is likely that in the guinea-pig brain the [3H]bremazocine sites (μ + δ + κ suppressed) are a subtype of κ-site family, namely κ2-sites. Finally, apparent affinities displayed at those sites are correlated with the biological activity of opioids in the guinea-pig ileum and rat vas deferens, suggesting that those sites could be considered as receptors.Key words: opioid receptors, kappa subtype, guinea-pig brain.

Distribution and characterization of 5-HT1D binding sites in the guinea-pig brain: an autoradiographic analysis

1990 ◽  
Vol 183 (3) ◽  
pp. 1109-1110
Author(s):  
H. Sijbesma ◽  
J.C.H.M. Cornelissen ◽  
E.R. de Kloet ◽  
J. Schipper
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Pig Brain ◽  
Autoradiographic Analysis ◽  
Guinea Pig Brain

scholarly journals Binding of [3H]FH-510 to sigma ligand binding sites in guinea pig brain membranes.

1993 ◽  
Vol 61 ◽  
pp. 279
Author(s):  
Makoto Tanaka ◽  
Shinsuke Kaku ◽  
Makoto Muramatu ◽  
Susumu Otomo
Keyword(s):  
Guinea Pig ◽  
Ligand Binding ◽  
Binding Sites ◽  
Brain Membranes ◽  
Pig Brain ◽  
Ligand Binding Sites ◽  
Guinea Pig Brain ◽  
Sigma Ligand

Ifenprodil potently interacts with [3H](+)-3-PPP-labeled σ binding sites in guinea pig brain membranes

1990 ◽  
Vol 176 (2) ◽  
pp. 247-248 ◽  
Author(s):  
E.William Karbon ◽  
Raymond J. Patch ◽  
Michael J. Pontecorvo ◽  
John W. Ferkany
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Brain Membranes ◽  
Pig Brain ◽  
Guinea Pig Brain

Solubilization and Characterization of ?-Receptors from Guinea Pig Brain Membranes

1989 ◽  
Vol 53 (5) ◽  
pp. 1575-1580 ◽  
Author(s):  
M. P. Kavanaugh ◽  
J. Parker ◽  
D. H. Bobker ◽  
J. F. W. Keana ◽  
E. Weber
Keyword(s):  
Guinea Pig ◽  
Brain Membranes ◽  
Pig Brain ◽  
Guinea Pig Brain

[3H]DTG and [3H](+)-3-PPP label pharmacologically distinct σ binding sites in guinea pig brain membranes

1991 ◽  
Vol 193 (1) ◽  
pp. 21-27 ◽  
Author(s):  
E. William Karbon ◽  
Karen Naper ◽  
Michael J. Pontecorvo
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Brain Membranes ◽  
Pig Brain ◽  
Guinea Pig Brain

Autoradiographic characterization of binding sites for [3H]NE-100 in guinea pig brain

Life Sciences ◽  
1995 ◽  
Vol 57 (21) ◽  
pp. PL333-PL337 ◽  
Author(s):  
Shigeru Okuyama ◽  
Shigeyuki Chaki ◽  
Tetsuji Yae ◽  
Atsuro Nakazato ◽  
Makoto Muramatsu
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Pig Brain ◽  
Guinea Pig Brain

scholarly journals Autoradiographic and biochemical characterization of binding sites for [3H]NE-100 in guinea pig brain.

1996 ◽  
Vol 71 ◽  
pp. 187
Author(s):  
Shigeru Okuyama ◽  
Shigeyuki Chaki ◽  
Makoto Tanaka ◽  
Tetsuji Yae ◽  
Atsuro Nakazato ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Biochemical Characterization ◽  
Pig Brain ◽  
Guinea Pig Brain

Comparison of binding parameters of σ1 and σ2 binding sites in rat and guinea pig brain membranes: novel subtype-selective trishomocubanes

1996 ◽  
Vol 311 (2-3) ◽  
pp. 233-240 ◽  
Author(s):  
Vu H. Nguyen ◽  
Michael Kassiou ◽  
Graham A.R. Johnston ◽  
Macdonald J. Christie
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Binding Parameters ◽  
Brain Membranes ◽  
Pig Brain ◽  
Subtype Selective ◽  
Guinea Pig Brain

Solubilization and characterization of binding sites for [3H]NE-100, a novel and potent sigma1 ligand, from guinea pig brain

Life Sciences ◽  
1996 ◽  
Vol 59 (16) ◽  
pp. 1331-1340 ◽  
Author(s):  
Shigeyuki Chakil ◽  
Shigeru Okuyama ◽  
Shinichi Ogawa ◽  
Makoto Tanaka ◽  
Makoto Muramatsu ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Binding Sites ◽  
Pig Brain ◽  
Guinea Pig Brain
Sign in / Sign up

Export Citation Format

Share Document