Dopamine/Serotonin Receptor Ligands. 10:1SAR Studies on Azecine-type Dopamine Receptor Ligands by Functional Screening at Human Cloned D1, D2L, and D5Receptors with a Microplate Reader Based Calcium Assay Lead to a Novel Potent D1/D5Selective Antagonist

2006 ◽  
Vol 49 (2) ◽  
pp. 760-769 ◽  
Author(s):  
Barbara Hoefgen ◽  
Michael Decker ◽  
Patrick Mohr ◽  
Astrid M. Schramm ◽  
Sherif A. F. Rostom ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Serotonin Receptor ◽  
Functional Screening ◽  
Receptor Ligands ◽  
Microplate Reader

Dopamine/Serotonin Receptor Ligands. Part 4. Synthesis and Pharmacology of Novel 3-Benzazecines and 3-Benzazonines as Potential 5-HT2A and Dopamine Receptor Ligands.

ChemInform ◽  
2003 ◽  
Vol 34 (13) ◽  
Author(s):  
Hussein El-Subbagh ◽  
Thomas Wittig ◽  
Michael Decker ◽  
Sigurd Elz ◽  
Martin Nieger ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Serotonin Receptor ◽  
Receptor Ligands

Adding perphenazine to increase effectiveness of standard glioblastoma chemoirradiation. (Preprint)

2020 ◽  
Author(s):  
Richard Kast
Keyword(s):  
Dopamine Receptor ◽  
Subventricular Zone ◽  
Serotonin Receptor ◽  
Treatment Effectiveness ◽  
Short Note ◽  
Recurrent Glioblastoma ◽  
Current Standard ◽  
Medically Ill ◽  
Current Standard Treatment ◽  
Protein Phosphatase 2

UNSTRUCTURED In the effort to improve treatment effectiveness in glioblastoma, this short note reviewed collected data on the pathophysiology of glioblastoma with particular reference to intersections with the pharmacology of perphenazine. That study identified five areas of potentially beneficial intersection. Data showed seemingly 5 independent perphenazine attributes of benefit to glioblastoma treatment - i) blocking dopamine receptor 2, ii) reducing centrifugal migration of subventricular zone cells by blocking dopamine receptor 3, iii) blocking serotonin receptor 7, iv) activation of protein phosphatase 2, and v) nausea reduction. Perphenazine is fully compatible with current chemoirradiation protocols and with the commonly used ancillary medicines used in clinical practice during the course of glioblastoma. All these attributes argue for a trial of perphenazine’s addition to current standard treatment with temozolomide and irradiation. The subventricular zone seeds the brain with mutated cells that become recurrent glioblastoma after centrifugal migration. The current paper shows how perphenazine might reduce that contribution. Perphenazine is an old, generic, cheap, phenothiazine antipsychotic drug that has been in continuous clinical use worldwide since the 1950’s. Clinical experience and research data over these decades have shown perphenazine to be well-tolerated in psychiatric populations, in normals, and in non-psychiatric, medically ill populations for whom perphenazine is used to reduce nausea. For now (Summer, 2020) the nature of glioblastoma requires a polypharmacy approach until/unless a core feature and means to address it can be identified in the future. Conclusions: Perphenazine possesses a remarkable constellation of attributes that recommend its use in GB treatment.

Conformational analysis and molecular modeling of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as D1 dopamine receptor ligands

1989 ◽  
Vol 32 (9) ◽  
pp. 2050-2058 ◽  
Author(s):  
Paul S. Charifson ◽  
J. Phillip Bowen ◽  
Steven D. Wyrick ◽  
Andrew J. Hoffman ◽  
Michael Cory ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Conformational Analysis ◽  
Dopamine Receptor ◽  
Receptor Ligands ◽  
D1 Dopamine Receptor
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