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195055-03-9,MFCD05260874
Catalog No.:AA00AB4T

195055-03-9 | R121919

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5mg
98%
in stock  
$148.00   $104.00
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25mg
98%
in stock  
$418.00   $293.00
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100mg
98%
in stock  
$974.00   $682.00
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1000mg
98% by HPLC
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$8,787.00   $6,151.00
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  • Technical Information
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00AB4T
Chemical Name:
R121919
CAS Number:
195055-03-9
Molecular Formula:
C22H32N6
Molecular Weight:
380.5297
MDL Number:
MFCD05260874
SMILES:
CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC
Properties
Computed Properties
 
Complexity:
480  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
28  
Hydrogen Bond Acceptor Count:
5  
Rotatable Bond Count:
7  
XLogP3:
4.7  

Literature

Title: Behavioral, biological, and chemical perspectives on targeting CRF(1) receptor antagonists to treat alcoholism.

Journal: Drug and alcohol dependence 20130301

Title: Design, synthesis, and structure-activity relationships of novel pyrazolo[5,1-b]thiazole derivatives as potent and orally active corticotropin-releasing factor 1 receptor antagonists.

Journal: Journal of medicinal chemistry 20121011

Title: Effects of CB1 and CRF1 receptor antagonists on binge-like eating in rats with limited access to a sweet fat diet: lack of withdrawal-like responses.

Journal: Physiology & behavior 20120910

Title: Depressive and cardiovascular disease comorbidity in a rat model of social stress: a putative role for corticotropin-releasing factor.

Journal: Psychopharmacology 20120701

Title: Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor.

Journal: Journal of medicinal chemistry 20120614

Title: Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles.

Journal: Bioorganic & medicinal chemistry letters 20111015

Title: Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.

Journal: Journal of medicinal chemistry 20110623

Title: Persistent anxiolytic affects after chronic administration of the CRF₁ receptor antagonist R121919 in rats.

Journal: Neuropharmacology 20110601

Title: Lithium, but not fluoxetine or the corticotropin-releasing factor receptor 1 receptor antagonist R121919, increases cell proliferation in the adult dentate gyrus.

Journal: The Journal of pharmacology and experimental therapeutics 20110401

Title: [¹²⁵I]YP20: a novel radioligand specific for the extracellular domain of the CRF₁ receptor.

Journal: European journal of pharmacology 20101215

Title: Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.

Journal: Bioorganic & medicinal chemistry letters 20101215

Title: Corticotropin releasing factor-induced amygdala gamma-aminobutyric Acid release plays a key role in alcohol dependence.

Journal: Biological psychiatry 20100501

Title: Consequences of chronic social stress on behaviour and vasopressin gene expression in the PVN of DBA/2OlaHsd mice--influence of treatment with the CRHR1-antagonist R121919/NBI 30775.

Journal: Journal of psychopharmacology (Oxford, England) 20090101

Title: 2-Arylpyrimidines: novel CRF-1 receptor antagonists.

Journal: Bioorganic & medicinal chemistry letters 20080815

Title: Restraint stress and ethanol consumption in two mouse strains.

Journal: Alcoholism, clinical and experimental research 20080501

Title: CRH-sub-1 receptor antagonists for the treatment of depression and anxiety.

Journal: Experimental and clinical psychopharmacology 20071201

Title: The CRF1 receptor antagonist, R121919, attenuates the severity of precipitated morphine withdrawal.

Journal: European journal of pharmacology 20070924

Title: The CRF1 receptor antagonist R121919 attenuates the neuroendocrine and behavioral effects of precipitated lorazepam withdrawal.

Journal: Psychopharmacology 20070601

Title: Corticotropin-releasing factor 1 antagonists selectively reduce ethanol self-administration in ethanol-dependent rats.

Journal: Biological psychiatry 20070101

Title: Facilitation of cardiac vagal activity by CRF-R1 antagonists during swim stress in rats.

Journal: Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20061201

Title: Dissociation between opioid and CRF1 antagonist sensitive drinking in Sardinian alcohol-preferring rats.

Journal: Psychopharmacology 20061201

Title: Impact of state of arousal and stress neuropeptides on urodynamic function in freely moving rats.

Journal: American journal of physiology. Regulatory, integrative and comparative physiology 20060601

Title: Glucocorticoid receptor and treatment of psychotic major depression.

Journal: Yao xue xue bao = Acta pharmaceutica Sinica 20051101

Title: Enduring, handling-evoked enhancement of hippocampal memory function and glucocorticoid receptor expression involves activation of the corticotropin-releasing factor type 1 receptor.

Journal: Endocrinology 20050901

Title: Analysis of the hormone-binding domain of steroid receptors using chimeras generated by homologous recombination.

Journal: Experimental cell research 20050815

Title: Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.

Journal: Journal of medicinal chemistry 20050811

Title: The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats.

Journal: Psychopharmacology 20050701

Title: Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.

Journal: Journal of medicinal chemistry 20050616

Title: Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919).

Journal: Psychopharmacology 20050601

Title: Corticotropin-releasing hormone-mediated induction of intracellular signaling pathways and brain-derived neurotrophic factor expression is inhibited by the activation of the endocannabinoid system.

Journal: Endocrinology 20050301

Title: Antidepressant-like activity of corticotropin-releasing factor type-1 receptor antagonists in mice.

Journal: European journal of pharmacology 20040919

Title: Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.

Journal: Journal of medicinal chemistry 20040909

Title: Altered serotonergic neurotransmission but normal hypothalamic-pituitary-adrenocortical axis activity in mice chronically treated with the corticotropin-releasing hormone receptor type 1 antagonist NBI 30775.

Journal: Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20031201

Title: Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.

Journal: Bioorganic & medicinal chemistry letters 20031006

Title: Role of corticotropin-releasing factor receptors type 1 and 2 in modulating the rat adrenocorticotropin response to stressors.

Journal: Endocrinology 20030601

Title: The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress.

Journal: The Journal of pharmacology and experimental therapeutics 20030201

Title: Corticotropin-releasing hormone modulators and depression.

Journal: Current opinion in investigational drugs (London, England : 2000) 20030101

Title: The high-affinity non-peptide CRH1 receptor antagonist R121919 attenuates stress-induced alterations in plasma oxytocin, prolactin, and testosterone secretion in rats.

Journal: Pharmacopsychiatry 20030101

Title: Treatment of depression with the CRH-1-receptor antagonist R121919: endocrine changes and side effects.

Journal: Journal of psychiatric research 20030101

Title: 3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.

Journal: Bioorganic & medicinal chemistry letters 20020819

Title: Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist.

Journal: Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20020801

Title: The CRH1 receptor antagonist R121919 attenuates stress-elicited sleep disturbances in rats, particularly in those with high innate anxiety.

Journal: Journal of psychiatric research 20020101

Title: Recent advances in the neurobiology of depression.

Journal: Psychopharmacology bulletin 20020101

Title: Effects of the high-affinity corticotropin-releasing hormone receptor 1 antagonist R121919 in major depression: the first 20 patients treated.

Journal: Journal of psychiatric research 20000101

Title: Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80.

Title: Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8.

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Tags:195055-03-9 Molecular Formula|195055-03-9 MDL|195055-03-9 SMILES|195055-03-9 R121919