CX546

Names

[ Name ]:
CX546

[Synonym ]:
CX 546
Lopac-C-271
BDP 17
GR 87
CX546

Biological Activity

[Description]:

CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.IC50 value:Target: AMPAR agonistin vitro: Treatments with the ampakine CX614 markedly and reversibly increased brain-derived neurotrophic factor (BDNF) mRNA and protein levels in cultured rat entorhinal/hippocampal slices [1]. in contrast to cyclothiazide or IDRA 21, the Ampakine CX546 binds specifically to the agonist bound nondesensitized receptor, most likely acting by destabilizing the desensitized receptor conformation [2]. In binding tests, CX546 caused an approximately 2-fold increase in the affinity for radiolabeled agonists, whereas CX516 was ineffective [3]. in vivo: Intraperitoneal injections of CX546 increased hippocampal BDNF mRNA levels in aged rats and middle-aged mice [1]. Administration of the positive modulator of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptors (AMPAR), CX546, during the conditioning phase only, improved the disrupted LI in mGluR5 knockout mice and facilitated LI in control C57BL/6J mice, given extended number of conditioning trails (four conditioning stimulus-unconditioned stimulus) [4].

[Related Catalog]:

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

[References]

[1]. Lauterborn JC, et al. Positive modulation of AMPA receptors increases neurotrophin expression by hippocampal and cortical neurons. J Neurosci. 2000 Jan 1;20(1):8-21.

[2]. Nagarajan N, et al. Mechanism and impact of allosteric AMPA receptor modulation by the ampakine CX546. Neuropharmacology. 2001 Nov;41(6):650-63.

[3]. Arai AC, et al. Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action. J Pharmacol Exp Ther. 2002 Dec;303(3):1075-85.

[4]. Lipina T, et al. The ampakine CX546 restores the prepulse inhibition and latent inhibition deficits in mGluR5-deficient mice. Neuropsychopharmacology. 2007 Apr;32(4):745-56.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.215g/cm3

[ Boiling Point ]:
422.8ºC at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₇NO₃

[ Molecular Weight ]:
247.29000

[ Flash Point ]:
209.5ºC

[ Exact Mass ]:
247.12100

[ PSA ]:
38.77000

[ LogP ]:
2.02180

[ Vapour Pressure ]:
2.34E-07mmHg at 25°C

[ Index of Refraction ]:
1.573

[ Storage condition ]:
2-8℃

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Ketamine-induced antidepressant effects are associated with AMPA receptors-mediated upregulation of mTOR and BDNF in rat hippocampus and prefrontal cortex.

Eur. Psychiatry 29(7) , 419-23, (2014)

Ketamine exerts fast acting, robust, and lasting antidepressant effects in a sub-anesthetic dose, however, the underlying mechanisms are still not fully elucidated. Recent studies have suggested that ...

Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action.

J. Pharmacol. Exp. Ther. 303 , 1075-1085, (2002)

CX516 (BDP-12) and CX546, two first-generation benzamide-type AMPA receptor modulators, were compared with regard to their influence on AMPA receptor-mediated currents, autaptic responses in cultured ...

Allosteric modulation of AMPA-type glutamate receptors increases activity of the promoter for the neural cell adhesion molecule, N-CAM.

Proc. Natl. Acad. Sci. U. S. A. 95 , 2597-2602, (1998)

To study regulation in vivo of the promoter for the neural cell adhesion molecule, N-CAM, we have used homologous recombination to insert the bacterial lacZ gene between the transcription and translat...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.