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Biochemical and pharmacological characterization of somatostatin receptors in rat brain.
Res Commun Chem Pathol Pharmacol. 1989 Nov; 66(2):203-18.RC

Abstract

We have characterized specific receptors for tetradecapeptide somatostatin (SS-14) of rat brain using 125I-labeled Tyr11-SS-14([125I-Tyr11]SS-14) as radioligand. [125I-Tyr11]SS-14 binding was sensitive to time, pH, temperature and ionic strength of the buffer, and was optimal in 50mM HEPES/KOH buffer, pH 7.5, at 25 degrees C for 60 minutes. Scatchard analysis indicated that the rat forebrain membranes had a single binding site with an apparent dissociation constant (Kd) of 0.522 +/- 0.044 nM and maximum binding capacity (Bmax) was 233 +/- 37 fmol/mg protein (mean +/- SEM). Ca2+, Mg2+, Mn2+ and Co2+ had a significant effect on the specific binding, which indicates that these metal ions might affect somatostatin receptor activity in the brain. Among CNS acting drugs, Ca2+ antagonists, antischizophrenic drugs, antidepressants and anticholinergic drugs had relative effects on [125I-Tyr11]SS-14 bindings to rat cerebral cortex membranes.

Authors+Show Affiliations

Sato H
Third Department of Internal Medicine, Okayama University Medical School, Japan.
Ota Z
No affiliation info available
Ogawa N
No affiliation info available

MeSH

AnimalsBrain ChemistryHydrogen-Ion ConcentrationIn Vitro TechniquesKineticsMaleNeurotransmitter AgentsProtease InhibitorsRatsRats, Inbred StrainsReceptors, NeurotransmitterReceptors, SomatostatinSubcellular FractionsSynaptic MembranesTemperature

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

2574901

Citation

Sato, H, et al. "Biochemical and Pharmacological Characterization of Somatostatin Receptors in Rat Brain." Research Communications in Chemical Pathology and Pharmacology, vol. 66, no. 2, 1989, pp. 203-18.
Sato H, Ota Z, Ogawa N. Biochemical and pharmacological characterization of somatostatin receptors in rat brain. Res Commun Chem Pathol Pharmacol. 1989;66(2):203-18.
Sato, H., Ota, Z., & Ogawa, N. (1989). Biochemical and pharmacological characterization of somatostatin receptors in rat brain. Research Communications in Chemical Pathology and Pharmacology, 66(2), 203-18.
Sato H, Ota Z, Ogawa N. Biochemical and Pharmacological Characterization of Somatostatin Receptors in Rat Brain. Res Commun Chem Pathol Pharmacol. 1989;66(2):203-18. PubMed PMID: 2574901.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biochemical and pharmacological characterization of somatostatin receptors in rat brain. AU - Sato,H, AU - Ota,Z, AU - Ogawa,N, PY - 1989/11/1/pubmed PY - 1989/11/1/medline PY - 1989/11/1/entrez SP - 203 EP - 18 JF - Research communications in chemical pathology and pharmacology JO - Res Commun Chem Pathol Pharmacol VL - 66 IS - 2 N2 - We have characterized specific receptors for tetradecapeptide somatostatin (SS-14) of rat brain using 125I-labeled Tyr11-SS-14([125I-Tyr11]SS-14) as radioligand. [125I-Tyr11]SS-14 binding was sensitive to time, pH, temperature and ionic strength of the buffer, and was optimal in 50mM HEPES/KOH buffer, pH 7.5, at 25 degrees C for 60 minutes. Scatchard analysis indicated that the rat forebrain membranes had a single binding site with an apparent dissociation constant (Kd) of 0.522 +/- 0.044 nM and maximum binding capacity (Bmax) was 233 +/- 37 fmol/mg protein (mean +/- SEM). Ca2+, Mg2+, Mn2+ and Co2+ had a significant effect on the specific binding, which indicates that these metal ions might affect somatostatin receptor activity in the brain. Among CNS acting drugs, Ca2+ antagonists, antischizophrenic drugs, antidepressants and anticholinergic drugs had relative effects on [125I-Tyr11]SS-14 bindings to rat cerebral cortex membranes. SN - 0034-5164 UR - https://www.unboundmedicine.com/medline/citation/2574901/Biochemical_and_pharmacological_characterization_of_somatostatin_receptors_in_rat_brain_ DB - PRIME DP - Unbound Medicine ER -