scholarly journals Evaluation of N-Alkyl Derivatives of Radioiodinated Spiperone as Radioligands for in Vivo Dopamine D2 Receptor Studies: Effects of Lipophilicity and Receptor Affinity on the in Vivo Biodistribution.

1992 ◽  
Vol 40 (1) ◽  
pp. 165-169 ◽  
Author(s):  
Hideo SAJI ◽  
Taro TOKUI ◽  
Iwao NAKATSUKA ◽  
Akihiko SAIGA ◽  
Yasuhiro MAGATA ◽  
...  
Keyword(s):  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Receptor Affinity ◽  
Dopamine D2 ◽  
In Vivo Biodistribution ◽  
Alkyl Derivatives ◽  
Derivatives Of

C957T polymorphism of dopamine D2 receptor gene affects striatal DRD2 in vivo availability by changing the receptor affinity

Synapse ◽  
2009 ◽  
Vol 63 (10) ◽  
pp. 907-912 ◽  
Author(s):  
Mika M. Hirvonen ◽  
Aki Laakso ◽  
Kjell Någren ◽  
Juha O. Rinne ◽  
Tiina Pohjalainen ◽  
...  
Keyword(s):  
Dopamine D2 Receptor ◽  
Receptor Gene ◽  
D2 Receptor ◽  
Receptor Affinity ◽  
Dopamine D2

scholarly journals Synthesis, Structural and Thermal Studies of 3-(1-Benzyl-1,2,3,6-tetrahydropyridin-4-yl)-5-ethoxy-1H-indole (D2AAK1_3) as Dopamine D2 Receptor Ligand

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2249 ◽  
Author(s):  
Magda Kondej ◽  
Agata Bartyzel ◽  
Monika Pitucha ◽  
Tomasz Wróbel ◽  
Andrea Silva ◽  
...  
Keyword(s):  
Molecular Dynamics ◽  
Thermal Stability ◽  
Dopamine D2 Receptor ◽  
Thermal Studies ◽  
D2 Receptor ◽  
Thermal Characterization ◽  
X Ray ◽  
Good Thermal Stability ◽  
Dopamine D2

Compound D2AAK1_3 was designed as a modification of the lead structure D2AAK1 (an in vivo active multi-target compound with nanomolar affinity to a number of aminergic GPCRs) and synthesized in the reaction of 5-ethoxyindole and 1-benzyl-4-piperidone. This compound has an affinity to the human dopamine D2 receptor with Ki of 151 nM. The aim of these studies was the structural and thermal characterization of the compound D2AAK1_3. In particular; X-ray studies; molecular docking and molecular dynamics as well as thermal analysis were performed. The studied compound crystallizes in orthorhombic system; in chiral space group P212121. The compound has a non-planar conformation. The studied compound was docked to the novel X-ray structure of the human dopamine D2 receptor in the inactive state (PDB ID: 6CM4) and established the main contact between its protonatable nitrogen atom and Asp (3.32) of the receptor. The obtained binding pose was stable in molecular dynamics simulations. Thermal stability of the compound was investigated using the TG-DSC technique in the air atmosphere, while TG-FTIR analyses in air and nitrogen atmospheres were also performed. The studied compound is characterized by good thermal stability. The main volatile products of combustion are the following gases: CO2; H2O toluene and CO while in the case of pyrolysis process in the FTIR spectra; the characteristic bands of NH3; piperidine and indole are additionally observed.

Dopamine D2 Receptor Blockade and Antimigraine Action of Flunarizine

Cephalalgia ◽  
1994 ◽  
Vol 14 (3) ◽  
pp. 235-240 ◽  
Author(s):  
C Wöber ◽  
T Brücke ◽  
C Wöber-Bingöl ◽  
S Asenbaum ◽  
P Wessely ◽  
...  
Keyword(s):  
Single Photon ◽  
Dopamine D2 Receptor ◽  
Photon Emission ◽  
D2 Receptor ◽  
High Specificity ◽  
D2 Receptors ◽  
Binding Potential ◽  
Receptor Blockade ◽  
Dopamine D2

We studied in vivo the influence of flunarizine on dopamine D2 receptors and investigated whether dopamine D2 receptor blockade is involved in its antimigraine action. Eleven migraine patients, treated with flunarizine, 10 mg per day, underwent single photon emission computer tomography (SPECT) using [123I] labeled iodobenzamide, a ligand with high affinity and high specificity for D2 receptors. There was a reduction of the dopamine D2 receptor binding potential in all patients compared to age-matched controls. The efficacy of flunarizine in migraine prophylaxis failed to correlate with the degree of the dopamine D2 receptor blockade. The antimigraine action of flunarizine may not involve antidopaminergic mechanisms.

Steele-Richardson-Olszewski-Syndrome: Reduction of dopamine D2 receptor binding relates to the severity of midbrain atrophy in vivo:123IBZM SPECT and MRI study

2002 ◽  
Vol 17 (3) ◽  
pp. 557-562 ◽  
Author(s):  
Guy Arnold ◽  
Klaus Tatsch ◽  
Eduardo Kraft ◽  
Wolfgang H. Oertel ◽  
Johannes Schwarz
Keyword(s):  
Receptor Binding ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Dopamine D2 ◽  
Mri Study

scholarly journals New Dopamine D2 Receptor Agonist, [3H]MCL-536, for Detecting Dopamine D2high Receptors in Vivo

2018 ◽  
Vol 9 (6) ◽  
pp. 1283-1289
Author(s):  
Sivan Subburaju ◽  
Anna W. Sromek ◽  
Philip Seeman ◽  
John L. Neumeyer
Keyword(s):  
Receptor Agonist ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Dopamine D2 ◽  
D2 Receptor Agonist

C957T polymorphism of the human dopamine D2 receptor gene predicts extrastriatal dopamine receptor availability in vivo

2009 ◽  
Vol 33 (4) ◽  
pp. 630-636 ◽  
Author(s):  
Mika M. Hirvonen ◽  
Ville Lumme ◽  
Jussi Hirvonen ◽  
Ullamari Pesonen ◽  
Kjell Någren ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Dopamine D2 Receptor ◽  
Receptor Gene ◽  
D2 Receptor ◽  
Dopamine D2
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