Radioligand Binding Detection of Receptors in Brain Membranes

2016 ◽  
pp. 59-76
Author(s):  
Fuencisla Pilar-Cuéllar ◽  
Alvaro Díaz ◽  
Emilio Garro-Martínez ◽  
Alicia Martín ◽  
Beatriz Romero ◽  
...  
Keyword(s):  
Radioligand Binding ◽  
Brain Membranes

Radioligand Binding Detection of Receptors in Brain Membranes

2021 ◽  
pp. 67-85
Author(s):  
Fuencisla Pilar-Cuéllar ◽  
Emilio Garro-Martínez ◽  
Elena Castro ◽  
Álvaro Díaz
Keyword(s):  
Radioligand Binding ◽  
Brain Membranes

Treatment of Rat Brain Membranes with Taurine Increases Radioligand Binding

1998 ◽  
pp. 377-383 ◽  
Author(s):  
Pattie Green ◽  
Ralph Dawson ◽  
David R. Wallace ◽  
Jeannie Owens
Keyword(s):  
Rat Brain ◽  
Radioligand Binding ◽  
Brain Membranes ◽  
Rat Brain Membranes

Opiate-Inhibited Adenylate Cyclase in Mammalian Brain Membranes

1986 ◽  
Author(s):  
Steven R. Childers ◽  
Peter Nijssen ◽  
Pauline Nadeau ◽  
Page Buckhannan ◽  
Phi-Van Le ◽  
...  
Keyword(s):  
Adenylate Cyclase ◽  
Mammalian Brain ◽  
Brain Membranes

Bronchospasmolytic and Adenosine Binding Activity of 8- (Proline / Pyrazole)-Substituted Xanthine Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Sneha Singh ◽  
Madhwi Ojha ◽  
Divya Yadav ◽  
Sonja Kachler ◽  
Karl-Norbert Klotz ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Radioligand Binding ◽  
Binding Activity ◽  
Receptor Subtypes ◽  
Significant Protection ◽  
Binding Studies ◽  
Standard Drug ◽  
Xanthine Derivatives ◽  
Radioligand Binding Studies ◽  
Micromolar Range

Background: ABSTRACT: Background: 8-Phenyltheophylline derivatives exhibit prophylactic effects at a specific dose but do not produce the cardiovascular or emetic side effects associated with xanthines, thereby exhibiting unique characteristics of potential therapeutic importance. Methods: Novel series of 8-(proline/pyrazole)-substituted xanthine analogs has been synthesized. The affinity and selectivity of compounds to adenosine receptors have been assessed by radioligand binding studies. The synthesized compounds also showed good bronchospasmolytic properties (increased onset of bronchospasm; decreased duration of jerks) with 100% survival of animals in comparison to the standard drug. Besides, compound 8f & 9f showed good binding affinity in comparison to other synthesized compounds in the micromolar range. Results: The maximum binding affinity of these compounds was observed for A2B receptors, which is ~ 7 or 10 times higher as compared to A1, A2A and A3 receptors. The newly synthesized derivatives 8f, 9a-f, 17g-m, and 18g-m displayed significant protection against histamine aerosol induced bronchospasm in guinea pigs. Conclusion: Newly synthesized proline/pyrazole based xanthines compounds showed a satisfactory binding affinity for adenosine receptor subtypes. Replacement or variation of substituted proline ring with substituted pyrazole scaffold at 8thposition of xanthine moiety resulted in the reduction of adenosine binding affinity and bronchospasmolytic effects.

Human Fibronectin Extra-Domain B (EDB)-Specific Aptide (APTEDB) Radiolabelling with Technetium-99m as a Potent Targeted Tumour-Imaging Agent

2018 ◽  
Vol 18 (2) ◽  
pp. 277-285 ◽  
Author(s):  
Mohsen Mohammadgholi ◽  
Nourollah Sadeghzadeh ◽  
Mostafa Erfani ◽  
Saeid Abediankenari ◽  
Seyed Mohammad Abedi ◽  
...  
Keyword(s):  
Radioligand Binding ◽  
Specific Binding ◽  
Specific Protein ◽  
Tumour Imaging ◽  
Specific Binding Ratio ◽  
Tumour Uptake ◽  
Technetium 99M ◽  
In Vivo Experiments ◽  
Human Fibronectin

Background: Human fibronectin extra-domain B (EDB) is particularly expressed during angiogenesis progression. It is, thus, a promising marker of tumour growth. Aptides are a novel class of peptides with high-affinity binding to specific protein targets. APTEDB is an antagonist-like ligand that especially interacts with human fibronectin EDB. Objective: This study was the first attempt in which the hydrazinonicotinamide (HYNIC)-conjugated APTEDB was labelled with technetium-99m (99mTc) as an appropriate radiotracer and tricine/EDDA exchange labeling. Methods: Radiochemical purity, normal saline, and serum stability were evaluated by HPLC and radio-isotope TLC scanner. Other examinations, such as protein-binding calculation, dissociation radioligand binding assay, and partition coefficient constant determination, were also carried out. The cellular-specific binding of 99mTc- HYNIC-conjugated APTEDB was assessed in two EDB-positive (U87MG) and EDB-negative (U373MG) cell lines. Bio-distribution was investigated in normal mice as well as in U87MG and U373MG tumour-bearing mice. Eventually, the radiolabelled APTEDB was used for tumour imaging using planar SPECT. Results: Radiolabelling was achieved with high purity (up to 97%) and accompanied by high solution (over 90% after overnight) and serum (80% after 2 hours) stability. The obtained cellular-specific binding ratio was greater than nine-fold. In-vivo experiments showed rapid blood clearance with mainly renal excretion and tumour uptake specificity (0.48±0.03% ID/g after 1h). The results of the imaging also confirmed considerable tumour uptake for EDB-positive cell line compared with the EDB-negative one. Conclusion: Aptides are considered to be a potent candidate for biopharmaceutical applications. They can be modified with imaging or therapeutic agents. This report shows the capability of 99mTc-HYNIC-APTEDB for human EDB-expressing tumours detection.

Rotenoids and Other Specialized Metabolites from the Roots of Mirabilis multiflora: Opioid and Cannabinoid Receptor Radioligand Binding Affinities

2021 ◽  
Vol 84 (4) ◽  
pp. 1392-1396
Author(s):  
Vimal K. Sharma ◽  
Radhakrishnan Srivedavyasasri ◽  
Zulfiqar Ali ◽  
Jordan K. Zjawiony ◽  
Samir A. Ross ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Radioligand Binding ◽  
Binding Affinities ◽  
Specialized Metabolites

scholarly journals Mechanistic Studies of the Antiallergic Activity of Phyllanthus amarus Schum. & Thonn. and Its Compounds

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 695
Author(s):  
Nur Zahirah Abd Rani ◽  
Kok Wai Lam ◽  
Juriyati Jalil ◽  
Hazni Falina Mohamad ◽  
Mohd Shukri Mat Ali ◽  
...  
Keyword(s):  
High Performance ◽  
Binding Assay ◽  
Radioligand Binding ◽  
Positive Control ◽  
Phyllanthus Amarus ◽  
H1 Receptor ◽  
Antiallergic Activity ◽  
Ketotifen Fumarate ◽  
Antihistamine Activity ◽  
Basophilic Leukemia

Phyllanthus amarus Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of P. amarus extract and its compounds. The antiallergic activity was determined by measuring the concentration of allergy markers release from rat basophilic leukemia (RBL-2H3) cells with ketotifen fumarate as the positive control. As a result, P. amarus did not stabilize mast cell degranulation but exhibited antihistamine activity. The antihistamine activity was evaluated by conducting a competition radioligand binding assay on the histamine 1 receptor (H1R). Four compounds were identified from the high performance liquid chromatography (HPLC) analysis which were phyllanthin (1), hypophyllanthin (2), niranthin (3), and corilagin (4). To gain insights into the binding interactions of the most active compound hypophyllanthin (2), molecular docking was conducted and found that hypophyllanthin (2) exhibited favorable binding in the H1R binding site. In conclusion, P. amarus and hypophyllanthin (2) could potentially exhibit antiallergic activity by preventing the activation of the H1 receptor.

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