Rationally Based Efficacy Tuning of Selective Dopamine D4 Receptor Ligands Leading to the Complete Antagonist 2-[4-(4-Chlorophenyl)piperazin-1- ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213)

Stefan Löber; Harald Hübner; Wolfgang Utz; Peter Gmeiner

doi:10.1021/jm015522j

Rationally Based Efficacy Tuning of Selective Dopamine D4 Receptor Ligands Leading to the Complete Antagonist 2-[4-(4-Chlorophenyl)piperazin-1- ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213)

Journal of Medicinal Chemistry ◽

10.1021/jm015522j ◽

2001 ◽

Vol 44 (17) ◽

pp. 2691-2694 ◽

Cited By ~ 67

Author(s):

Stefan Löber ◽

Harald Hübner ◽

Wolfgang Utz ◽

Peter Gmeiner

Keyword(s):

Dopamine D4 Receptor ◽

Receptor Ligands ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

Recent findings leading to the discovery of selective dopamine D4 receptor ligands for the treatment of widespread diseases

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2020.113141 ◽

2021 ◽

Vol 212 ◽

pp. 113141

Author(s):

Gianfabio Giorgioni ◽

Fabio Del Bello ◽

Pegi Pavletić ◽

Wilma Quaglia ◽

Luca Botticelli ◽

...

Keyword(s):

Dopamine D4 Receptor ◽

Receptor Ligands ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

ChemInform Abstract: Piperidinylpyrroles: Design, Synthesis, and Binding Properties of Novel and Selective Dopamine D4 Receptor Ligands.

ChemInform ◽

10.1002/chin.200008156 ◽

2010 ◽

Vol 31 (8) ◽

pp. no-no

Author(s):

Christian Haubmann ◽

Harald Huebner ◽

Peter Gmeiner

Keyword(s):

Dopamine D4 Receptor ◽

Receptor Ligands ◽

Binding Properties ◽

Design Synthesis ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

Synthesis and in vitro evaluation of iodine labelled pyrazolo[1,5-a]pyridines as highly selective dopamine D4 receptor ligands

Journal of Labelled Compounds and Radiopharmaceuticals ◽

10.1002/jlcr.508 ◽

2001 ◽

Vol 44 (12) ◽

pp. 849-858 ◽

Cited By ~ 9

Author(s):

O. Prante ◽

S. Löber ◽

H. Hübner ◽

P. Gmeiner ◽

T. Kuwert

Keyword(s):

Dopamine D4 Receptor ◽

Receptor Ligands ◽

In Vitro Evaluation ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

Piperidinylpyrroles: Design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/s0960-894x(99)00540-5 ◽

1999 ◽

Vol 9 (21) ◽

pp. 3143-3146 ◽

Cited By ~ 32

Author(s):

Christian Haubmann ◽

Harald Hübner ◽

Peter Gmeiner

Keyword(s):

Dopamine D4 Receptor ◽

Receptor Ligands ◽

Binding Properties ◽

Design Synthesis ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

ChemInform Abstract: 2,2-Dicyanovinyl as a Nonaromatic Aryl Bioisostere: Synthesis, Binding Experiments, and SAR Studies of Highly Selective Dopamine D4 Receptor Ligands.

ChemInform ◽

10.1002/chin.199943280 ◽

2010 ◽

Vol 30 (43) ◽

pp. no-no

Author(s):

Christian Haubmann ◽

Harald Huebner ◽

Peter Gmeiner

Keyword(s):

Dopamine D4 Receptor ◽

Receptor Ligands ◽

Sar Studies ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

2,2-dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/s0960-894x(99)00302-9 ◽

1999 ◽

Vol 9 (14) ◽

pp. 1969-1972 ◽

Cited By ~ 20

Author(s):

Christian Haubmann ◽

Harald Hübner ◽

Peter Gmeiner

Keyword(s):

Dopamine D4 Receptor ◽

Receptor Ligands ◽

Sar Studies ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

ChemInform Abstract: Synthesis, SAR and Pharmacology of CP-293,019: A Potent, Selective Dopamine D4 Receptor Antagonist.

ChemInform ◽

10.1002/chin.199830180 ◽

2010 ◽

Vol 29 (30) ◽

pp. no-no

Author(s):

M. A. SANNER ◽

ET AL. ET AL.

Keyword(s):

Receptor Antagonist ◽

Dopamine D4 Receptor ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

Blockade of the expression of behavioral sensitization to amphetamine by the selective dopamine D4 receptor antagonist, PNU-101387G

Schizophrenia Research ◽

10.1016/s0920-9964(97)82217-7 ◽

1997 ◽

Vol 24 (1-2) ◽

pp. 80

Author(s):

Lana M. Needham ◽

Kalpana M. Merchant

Keyword(s):

Receptor Antagonist ◽

Behavioral Sensitization ◽

Dopamine D4 Receptor ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

Synthesis and functional activity of (2-aryl-1-piperazinyl)-N-(3-methylphenyl)acetamides: selective dopamine D4 receptor agonists

Bioorganic & Medicinal Chemistry ◽

10.1016/s0968-0896(04)00337-2 ◽

2004 ◽

Author(s):

M MATULENKO

Keyword(s):

Functional Activity ◽

Dopamine D4 Receptor ◽

Receptor Agonists ◽

D4 Receptor ◽

Selective Dopamine

Download Full-text

2.217 PHARMACOKINETIC PROFILE OF THE SELECTIVE DOPAMINE D4 RECEPTOR ANTAGONIST L-745,870 IN THE MPTP-LESIONED NON-HUMAN PRIMATE MODEL OF PARKINSON'S DISEASE

Parkinsonism & Related Disorders ◽

10.1016/s1353-8020(11)70541-7 ◽

2012 ◽

Vol 18 ◽

pp. S119

Author(s):

P. Huot ◽

J.B. Koprich ◽

T.H. Johnston ◽

S.H. Fox ◽

J.M. Brotchie

Keyword(s):

Parkinson’S Disease ◽

Parkinson's Disease ◽

Receptor Antagonist ◽

Pharmacokinetic Profile ◽

Dopamine D4 Receptor ◽

Primate Model ◽

D4 Receptor ◽

Selective Dopamine ◽

Human Primate

Download Full-text