Dopamine/Serotonin Receptor Ligands VI. Dibenz[g,j]-1-oxa-4-azacycloundecene and Dibenz[d,g]-2-azacycloundecene: Synthesis of Two New Heterocyclic Ring Systems as Potential Ligands for Dopamine Receptor Subtypes

Heterocycles ◽  
2003 ◽  
Vol 60 (4) ◽  
pp. 887 ◽  
Author(s):  
Jochen Lehmann ◽  
Thomas W. Wittig ◽  
Christoph Enzensperger
Keyword(s):  
Dopamine Receptor ◽  
Serotonin Receptor ◽  
Heterocyclic Ring ◽  
Receptor Subtypes ◽  
Receptor Ligands ◽  
Dopamine Receptor Subtypes ◽  
Ring Systems

Dopamine Receptor Subtypes and Orofacial Movement Topographies: Studies with Mutant Models

2010 ◽  
Vol 52 (4) ◽  
pp. 336-343
Author(s):  
Noriaki Koshikawa ◽  
Katsunori Tomiyama ◽  
John L. Waddington
Keyword(s):  
Dopamine Receptor ◽  
Receptor Subtypes ◽  
Dopamine Receptor Subtypes ◽  
Orofacial Movement

Effect of aging on striatal dopamine receptor subtypes in Wistar rats

1986 ◽  
Vol 7 (5) ◽  
pp. 357-361 ◽  
Author(s):  
Jacquelyn M. Henry ◽  
Charles R. Filburn ◽  
James A. Joseph ◽  
George S. Roth
Keyword(s):  
Dopamine Receptor ◽  
Wistar Rats ◽  
Striatal Dopamine ◽  
Receptor Subtypes ◽  
Dopamine Receptor Subtypes ◽  
Striatal Dopamine Receptor

Stereochemistry of serotonin receptor ligands from crystallographic data. Crystal structures of NAN-190.HBr, 1-phenylbiguanide, MDL 72222 and mianserin.HCl and selectivity criteria towards 5-HT1, 5-HT2 and 5-HT3 receptor subtypes

1996 ◽  
Vol 52 (3) ◽  
pp. 509-518 ◽  
Author(s):  
A. Dalpiaz ◽  
V. Ferretti ◽  
P. Gilli ◽  
V. Bertolasi
Keyword(s):  
Structural Analysis ◽  
Serotonin Receptor ◽  
Molecular Structures ◽  
Receptor Subtypes ◽  
Receptor Ligands ◽  
Endogenous Ligand ◽  
Constant Length ◽  
Mdl 72222 ◽  
Crystal And Molecular Structures ◽  
Pharmacophoric Feature

The crystal and molecular structures of the following serotoninergic drugs have been determined: (1) 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine hydrobromide hemihydrate (NAN-190.HBr), C23H28N3O3 +.Br−.1/2H2O, Mr = 483.42, monoclinic, C2/c, a = 21.916 (4), b = 15.207 (2), c = 14.052 (2) Å, β = 101.56 (1)°, V = 4588 (1) Å3, Z = 8, Dx = 1.40 Mg m−3, λ(Mo Kα) = 0.71069 Å, μ = 1.823 mm−1, F(000) = 2008, T = 295 K, R = 0.035 for 2617 observed reflections; (2) N-phenylimidocarbonimidic diamide (1-phenylbiguanide), C8H11N5, Mr = 177.21, monoclinic, P21/c, a = 9.781 (2), b = 35.040 (5), c = 11.000 (2) Å, β = 97.72 (1)°, V = 3736 (1) Å3, Z = 16, Dx = 1.26 Mg m−3, λ(Mo Kα) = 0.71069 Å, μ= 0.084 mm−1, F(000) = 1504, T = 295 K, R = 0.070 for 3407 observed reflections; (3) 8-methyl-8-azabicyclo[3.2.1.]oct-3-yl 3,5-dichlorobenzoate (MDL 72222), C15H17C12NO2, Mr = 314.21, triclinic, P{\bar 1}, a = 8.480 (3), b = 9.840 (3), c = 10.15 (4) Å, α = 90.04 (3), β = 111.77 (3), γ = 105.07 (3)°, V = 755.6 (5) Å3, Z = 2, Dx = 1.38 Mg m−3, λ(Mo Kα) = 0.71069 Å, μ = 0.430 mm−1, F(000) = 328, T = 295 K, R = 0.070 for 1685 observed reflections; (4) 1,2,3,4,10,14b-hexahydro-2-methyldibenzo[cf]pyrizino[1,2-a]azepine hydrochloride (mianserin.HCl), C18H21N2 +.Cl−, Mr = 300.83, monoclinic, P21/a, a = 9.014 (2), b = 14.917 (2), c = 12.412 (2) Å, β = 108.84 (1)°, V = 1579.5 (5) Å3, Z = 4, Dx = 1.26 Mg m−3, λ(Mo Kα) = 0.71069 Å, μ = 0.237 mm−1, F(000) = 640, T = 295 K, R = 0.063 for 1493 observed reflections. A systematic structural analysis of the present compounds and others known to interact with the 5-HT1, 5-HT2 and 5-HT3 receptors allows to identify their similarities with the endogenous ligand serotonin (5-HT) and the stereochemical differences which determine selectivity for the various receptor subtypes. The pharmacophoric feature for 5-HT receptor binding is identified in a constant-length vector linking an aromatic ring with a protonated nitrogen, while specific affinities for receptorial subtypes and the nature of the effect appear to be modulated by the dimensions of the substituents at nitrogen.

Heterogeneity and regulation of central dopamine receptor subtypes studied by cDNA cloning methodology

1992 ◽  
Vol 20 ◽  
pp. 27-32 ◽  
Author(s):  
Pierre Sokoloff ◽  
Marie-Pascalle Martres ◽  
Bruno Giros ◽  
Marie-Louise Bouthenet ◽  
Jean-Charles Schwartz
Keyword(s):  
Dopamine Receptor ◽  
Cdna Cloning ◽  
Receptor Subtypes ◽  
Dopamine Receptor Subtypes
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