Synthesis of New Dopamine D1 Antagonist SCH 23390 Analogues by the Stereoselective Stevens Rearrangement

2011 ◽  
Vol 2011 (32) ◽  
pp. 6507-6518 ◽  
Author(s):  
Manuela Ariza ◽  
Amelia Díaz ◽  
Rafael Suau ◽  
María Valpuesta
Keyword(s):  
Sch 23390 ◽  
Stevens Rearrangement ◽  
Dopamine D1 Antagonist

SCH 23390, a selective dopamine D1 antagonist, activates dopamine neurons but fails to prevent their inhibition by apomorphine

1985 ◽  
Vol 111 (3) ◽  
pp. 393-396 ◽  
Author(s):  
Giampaolo Mereu ◽  
Maria Collu ◽  
Ennio Ongini ◽  
Giovanni Biggio ◽  
Gian Luigi Gessa
Keyword(s):  
Sch 23390 ◽  
Dopamine Neurons ◽  
Dopamine D1 Antagonist ◽  
Selective Dopamine

The relaxing effect of SCH 23390 in the molluscan smooth muscle

1989 ◽  
Vol 94 (1) ◽  
pp. 341-344
Author(s):  
Hajime Murakami ◽  
Masakazu Sano ◽  
Takashi Tsukimura ◽  
Akira Yamazaki
Keyword(s):  
Smooth Muscle ◽  
Sch 23390 ◽  
Molluscan Smooth Muscle ◽  
Relaxing Effect

scholarly journals Altered heparan sulfate metabolism during development triggers dopamine-dependent autistic-behaviours in models of lysosomal storage disorders

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Maria De Risi ◽  
Michele Tufano ◽  
Filomena Grazia Alvino ◽  
Maria Grazia Ferraro ◽  
Giulia Torromino ◽  
...  
Keyword(s):  
Heparan Sulfate ◽  
Sch 23390 ◽  
Lysosomal Storage Disorders ◽  
Dopamine Neurons ◽  
Therapeutic Effects ◽  
Lysosomal Storage ◽  
Cellular Models ◽  
Mps Ii ◽  
Mps Iiia ◽  
Storage Disorders

AbstractLysosomal storage disorders characterized by altered metabolism of heparan sulfate, including Mucopolysaccharidosis (MPS) III and MPS-II, exhibit lysosomal dysfunctions leading to neurodegeneration and dementia in children. In lysosomal storage disorders, dementia is preceded by severe and therapy-resistant autistic-like symptoms of unknown cause. Using mouse and cellular models of MPS-IIIA, we discovered that autistic-like behaviours are due to increased proliferation of mesencephalic dopamine neurons originating during embryogenesis, which is not due to lysosomal dysfunction, but to altered HS function. Hyperdopaminergia and autistic-like behaviours are corrected by the dopamine D1-like receptor antagonist SCH-23390, providing a potential alternative strategy to the D2-like antagonist haloperidol that has only minimal therapeutic effects in MPS-IIIA. These findings identify embryonic dopaminergic neurodevelopmental defects due to altered function of HS leading to autistic-like behaviours in MPS-II and MPS-IIIA and support evidence showing that altered HS-related gene function is causative of autism.

DA1 dopamine receptors in renal cortical collecting duct

1991 ◽  
Vol 261 (5) ◽  
pp. F890-F895 ◽  
Author(s):  
K. Ohbu ◽  
R. A. Felder
Keyword(s):  
Adenylate Cyclase ◽  
Specific Binding ◽  
Collecting Duct ◽  
Sch 23390 ◽  
Receptor Density ◽  
Cortical Collecting Duct ◽  
Tightly Coupled ◽  
Renal Dopamine ◽  
Dissociation Constant Kd ◽  
Stimulation Of

Renal dopamine DA1 receptors are linked to the regulation of sodium transport. We have previously reported the presence of DA1 receptors in the proximal convoluted tubule (PCT) but not in the distal convoluted tubule. However, the DA1 receptor in the collecting duct, the final determinant of electrolyte transport, has not been studied. DA1 receptors were studied in the microdissected cortical collecting duct (CCD) of rats by autoradiography with use of the selective DA1 radioligand 125I-Sch 23982 and by measurement of adenylate cyclase (AC) activity. Specific binding of 125I-Sch 23982 to CCD was saturable with radioligand concentration. The dissociation constant (Kd) was 0.46 +/- 0.08 nM (n = 5), and the maximum receptor density (Bmax) was 1.41 +/- 0.43 fmol/mg protein (n = 5). The DA1 antagonist Sch 23390 was more effective than the DA1 agonist fenoldopam in competing for specific 125I-Sch 23982 binding. Fenoldopam stimulated AC activity in CCD in a concentration-dependent (10(-9)-10(-6) M) manner. The ability of fenoldopam to stimulate AC activity was similar in CCD and PCT even though DA1 receptor density was 1,000 times greater in the CCD than in the PCT. In additional studies, fenoldopam stimulation of AC activity did not influence vasopressin-stimulated AC activity. We conclude that the DA1 receptor in rat CCD is tightly coupled to AC stimulation and that there is no interaction between DA1 agonist-stimulated and vasopressin-stimulated AC activity in the CCD.

SCH 23390, but not raclopride, decreases intake of intraorally infused 10% sucrose

Appetite ◽  
1992 ◽  
Vol 19 (2) ◽  
pp. 223 ◽  
Author(s):  
A. Tyrka ◽  
G.P. Smith
Keyword(s):  
Sch 23390

Synthesis of Allyl 2-Dialkylamino-4-pentenoates and Their Analogs via Stevens Rearrangement

2003 ◽  
Vol 39 (9) ◽  
pp. 1227-1230 ◽  
Author(s):  
A. V. Babakhanyan ◽  
L. G. Shakhbazyan ◽  
Dzh. V. Grigoryan ◽  
S. T. Kocharyan
Keyword(s):  
Stevens Rearrangement

Formation of furan derivatives in the course of the Stevens rearrangement of ammonium salts containing 4-allyloxy(phenoxy)-2-butynyl group

2007 ◽  
Vol 77 (8) ◽  
pp. 1370-1372 ◽  
Author(s):  
M. O. Manukyan ◽  
A. V. Babakhanyan ◽  
G. A. Panosyan ◽  
A. Kh. Gyul’nazaryan ◽  
S. T. Kocharyan
Keyword(s):  
Ammonium Salts ◽  
Furan Derivatives ◽  
Stevens Rearrangement

Selection of a Sommelet-Hauser or a Stevens rearrangement pathway of N,N-dimethyl(substituted benzyl)ammonium N-alkylides

1992 ◽  
Vol 57 (18) ◽  
pp. 5034-5036 ◽  
Author(s):  
Tetsuya Tanaka ◽  
Naohiro Shirai ◽  
Junji Sugimori ◽  
Yoshiro Sato
Keyword(s):  
Stevens Rearrangement ◽  
Benzyl Ammonium ◽  
Ammonium N ◽  
Selection Of
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