142363-72-2Relevant academic research and scientific papers
MORPHOLINE DOPAMINE AGONISTS FOR THE TREATMENT OF PAIN
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Page/Page column 38-39, (2008/12/07)
The present invention relates to use of a compound of formula (I), (Ia), or (Ib), wherein A, B, Z, R1and R2 have the meanings given in the specification, as a medicament for the treatment of a number of pain conditions, particularly chronic or nociceptive
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route
Blagg, Julian,Allerton, Charlotte M.N.,Batchelor, David V.J.,Baxter, Andrew D.,Burring, Denise J.,Carr, Christopher L.,Cook, Andrew S.,Nichols, Carly L.,Phipps, Joanne,Sanderson, Vivienne G.,Verrier, Hugh,Wong, Stephen
, p. 6691 - 6696 (2008/03/14)
This paper reports the synthesis and biological activity of a novel series of aryl-morpholine dopamine receptor agonists. Several compounds show high levels of functional selectivity for the D3 over the D2 dopamine receptor. Compound 26 has >1000-fold functional selectivity and has been successfully progressed in vivo using an intranasal delivery route.
MORPHOLINE DERIVATIVES FOR USE AS DOPAMINE AGONISTS IN THE TREATMENT OF I.A. SEXUAL DYSFUNCTION
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Page 65-66, (2008/06/13)
The present invention provides for compounds of formula (I), (la) and (lb) Wherein: A is selected from C-X and N, B is selected from C-Y and N, R1 is selected from H and (C1-C6)alkyl R2 is selected from H and (C
Oxygen Isosteric Derivatives of 3-(3-Hydroxyphenyl)-N-n-propylpiperidine
Perrone, Roberto,Berardi, Francesco,Leopoldo, Marcello,Tortorella, Vincenzo,Lograno, Marcello D.,et al.
, p. 3045 - 3049 (2007/10/02)
Some substituted 3-phenylmorpholines (10a-e,j,k) and 3-thienylmorpholines (10f,g), isosteres of 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP), were prepared and submitted to binding assays on D-2 dopaminergic and 5-HT1 and 5-HT2 serotonergic receptors, in comparison with 3-PPP and its analogue 3a,b.The results show the loss of D-2 affinity for all morpholines, while a certain activity was still observable for piperidine derivatives.Regarding the serotonergic affinity, only chloro and methoxy derivatives (10a-d) were moderately active on the 5-HT1A receptor, either when the substituent was in the C-2 or C-3 position, whereas no tested compounds showed affinity toward the 5-HT2 receptor.
