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.
Publictions citing BOC Sciences Products
  • >> More
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related 5-HT Receptor Products


Sarizotan HCl
(CAS: 195068-07-6)

Sarizotan, also known as EMD-128130, is a full 5-HT1a agonist and a dopamine D2-like agonist/partial agonist used in clinical trials for the treatment of l-dopa...

CAS 163521-12-8 Vilazodone

Vilazodone
(CAS: 163521-12-8)

Vilazodone (EMD 68843; SB 659746A) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evalu...

CAS 78950-78-4 8-OH-DPAT

8-OH-DPAT
(CAS: 78950-78-4)

8-OH-DPAT (8-Hydroxy-DPAT) is an agonist that has selectivity for 5-HT1A receptor (pIC50 = 8.19). It was subsequently found to be a serotonin reuptake inhibitor...

CAS 17321-77-6 Clomipramine HCl

Clomipramine HCl
(CAS: 17321-77-6)

Clomipramine HCl is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) bl...

CAS 123040-16-4 Azasetron hydrochloride

Azasetron hydrochloride
(CAS: 123040-16-4)

Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

CAS 98224-03-4 Eltoprazine

Eltoprazine
(CAS: 98224-03-4)

Eltoprazine belongs the phenylpiperazine class which is a serenic or antiaggressive agent. It acts as an agonist at the 5-HT1A and 5-HT1B receptors and as an an...

CAS 143322-58-1 Eletriptan

Eletriptan
(CAS: 143322-58-1)

Eletriptan is Serotonin 1D receptor agonist originated by Pfizer. It is a second generation triptan drug. It is used as an abortive medication, blocking a migra...

CAS 158876-82-5 Rupatadine

Rupatadine
(CAS: 158876-82-5)

Rupatadine, with the potential to treat allergic rhinitis and urticaria, is a potent and long-lasting dual antagonist of PAF/H1. in vitro: Without affecting con...

CAS 135729-61-2 Palonosetron hydrochloride

Palonosetron hydrochloride
(CAS: 135729-61-2)

CAS 98206-09-8 Eltoprazine hydrochloride

Eltoprazine hydrochloride
(CAS: 98206-09-8)

Eltoprazine hydrochloride is the hydrochloride form of Eltoprazine which is a serenic or antiaggressive agent. It acts as an agonist at the 5-HT1A and 5-HT1B re...

RU-24969
(CAS: 66611-26-5)

RU 24969 is a 5-HT1A and 5-HT1B receptors act as serotonin 1A/1B receptor agonists.

Aripiprazole lauroxil
(CAS: 1259305-29-7)

Aripiprazole lauroxil is a Dopamine D2 receptor agonist, Serotonin 1A receptor agonist and ISerotonin 2A receptor antagonist under the development of Alkermes p...

CAS 64022-27-1 MK212

MK212
(CAS: 64022-27-1)

MK212 is a 5HT2C-receptor agonist. It exhibited anxiolytic activity in mice at low doses. It is a serotonin agonist. It could promote the secretion of serum pro...

CAS 152811-62-6 Piboserod

Piboserod
(CAS: 152811-62-6)

Piboserod is a highly and potent selective 5-HT4 receptor antagonist which as been studied in vitro as well as in vivo as a pharmacological tool to evaluate the...

CAS 162760-96-5 WAY-100635

WAY-100635
(CAS: 162760-96-5)

WAY-100635 is an achiral analogue of WAY-100135 which is significantly more potent and selective than the latter compound and which displays unequivocal 5-HTIA ...

CAS 367514-88-3 Lurasidone hydrochloride

Lurasidone hydrochloride
(CAS: 367514-88-3)

Lurasidone is an atypical antipsychotic, inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50 of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and ...

CAS 119193-37-2 LY 278584

LY 278584
(CAS: 119193-37-2)

LY 278584 is a 5-HT3-receptor antagonist and no detailed information has been published yet.

CAS 99614-02-5 Ondansetron

Ondansetron
(CAS: 99614-02-5)

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

CP-809101 hydrochloride
(CAS: 1215721-40-6)

The hydrochloride salt form of CP-809101 which is a selective 5-HT2C receptor agonist which probably shows antipsychotic activity and restrains amphetamine-stim...

CAS 115956-13-3 Dalasetron Mesylate

Dalasetron Mesylate
(CAS: 115956-13-3)

The mesylate salt form of Dolasetron which is a pseudopelletierine derivative and could be used to relieve the nausea and vomiting caused by chemotherapy for be...

Chemical Structure

CAS 740873-06-7 Naluzotan

Quick Inquiry

Verification code

Featured Items