Naluzotan - CAS 740873-06-7
Catalog number: 740873-06-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H38N4O3S
Molecular Weight:
450.64
COA:
Inquire
Targets:
5-HT Receptor
Description:
Naluzotan is a selective 5-HT1A receptor partial agonist under the development of EPIX Pharmaceuticals. It is a serotonergic drug for the treatment of generalized anxiety disorder and major depressive disorder.
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Purity:
98%
Appearance:
Powder
Synonyms:
PRX00023;N-(3-(4-(4-((cyclohexylmethyl)sulfonamido)butyl)piperazin-1-yl)phenyl)acetamide
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
generalized anxiety disorder; major depressive disorder
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
SPWZXWDPAWDKQE-UHFFFAOYSA-N
InChI:
1S/C23H38N4O3S/c1-20(28)25-22-10-7-11-23(18-22)27-16-14-26(15-17-27)13-6-5-12-24-31(29,30)19-21-8-3-2-4-9-21/h7,10-11,18,21,24H,2-6,8-9,12-17,19H2,1H3,(H,25,28)
Canonical SMILES:
CC(=O)Nc1cccc(c1)N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2
Current Developer:
EPIX Pharmaceuticals Inc
1.Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression.
de Paulis T1. Curr Opin Investig Drugs. 2007 Jan;8(1):78-86.
EPIX Pharmaceuticals Inc (formerly Predix Pharmaceuticals Inc) is developing PRX-00023, an oral aryl piperazine 5-HT1A agonist, for the potential treatment of depression. While initially in development for generalized anxiety disorder, EPIX is now only focusing on the development of PRX-00023 for depression. In November 2006, EPIX reported that it planned to initiate a phase II trial in patients with depression in the first half of 2007.
2.Tolerability, pharmacokinetics, and neuroendocrine effects of PRX-00023, a novel 5-HT1A agonist, in healthy subjects.
Iyer GR1, Reinhard JF Jr, Oshana S, Kauffman M, Donahue S. J Clin Pharmacol. 2007 Jul;47(7):817-24. Epub 2007 May 10.
PRX-00023 is a novel, nonazapirone 5-HT1A agonist in clinical development for treatment of affective disorders. The objectives of the initial clinical phase I studies (a single ascending dose study and multiple dose-ascending and high-dose titration studies) were to measure the pharmacokinetics, pharmacodynamic (neuroendocrine) effects, and tolerability of PRX-00023 in healthy subjects. The studies evaluated 10-mg to 150-mg doses of PRX-00023 in up to 112 healthy male and female subjects aged 18 to 54 years. Single and multiple oral doses of PRX-00023 were found to be safe and well tolerated in healthy subjects. PRX-00023 was absorbed relatively rapidly, with a tmax of 0.5 to 2 hours, and eliminated with a half-life of approximately 12 hours. PRX-00023 treatment transiently increased blood prolactin levels 2 to 3 hours after administration, consistent with its mechanism as a 5-HT1A agonist.
3.Effects of PRX-00023, a novel, selective serotonin 1A receptor agonist on measures of anxiety and depression in generalized anxiety disorder: results of a double-blind, placebo-controlled trial.
Rickels K1, Mathew S, Banov MD, Zimbroff DL, Oshana S, Parsons EC Jr, Donahue SR, Kauffman M, Iyer GR, Reinhard JF Jr. J Clin Psychopharmacol. 2008 Apr;28(2):235-9. doi: 10.1097/JCP.0b013e31816774de.
PRX-00023, a serotonin 1A receptor agonist, was designed to provide high potency and selectivity for its target. To assess the possible therapeutic utility in anxiety, a randomized, double-blind, placebo-controlled trial was conducted in 311 subjects who met the criteria of the Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition, for generalized anxiety disorder. All subjects underwent a 1-week placebo run-in and were randomized to receive once-daily capsules containing either PRX-00023 (80 mg/d) or placebo for an additional 8 weeks. The primary outcome measure was the Hamilton Anxiety Scale (HAM-A). The Montgomery-Asberg Depression Rating Scale was used as a secondary endpoint to measure depressive symptoms. Statistical testing was performed with analysis of covariance, between baseline and week 8, with baseline values as a covariate. The anxiolytic effect of PRX-00023, compared with placebo, showed trends across all anxiolytic measures but failed to reach significance on the primary endpoint (HAM-A total score).
4.PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety.
Brunelli SA1, Aviles JA, Gannon KS, Branscomb A, Shacham S. Pharmacol Biochem Behav. 2009 Nov;94(1):8-15. doi: 10.1016/j.pbb.2009.06.014. Epub 2009 Jul 2.
To address the development of early anxiety disorders across the lifespan, the High USV line of rats was bred based on rates of infant ultrasonic vocalization in the 40-50 kHz range of predominant frequencies (USV) to maternal separation at postnatal day (P) 10. In this study, rates of USV in High line infants (pups: Postnatal Day 11+/-1) were compared to those of randomly-bred controls in response to EPIX compound PRX-00023, a unique serotonin (5-HT) agonist, acting exclusively at the 5-HT1A receptor, or buspirone, a nonspecific 5HT1A agonist. After testing, pups were examined for sedation and other drug-related effects. The results indicated that all doses of buspirone reduced USV rates in isolation, consistent with other reports. PRX-00023 significantly reduced USV rates at the lowest doses (0.01-0.05 mg/kg). None of the PRX-00023 doses produced sedation, whereas all but the lowest dose of buspirone (0.1 mg/kg) produced sedation effects.
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CAS 740873-06-7 Naluzotan

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