CX546 structure
|
Common Name | CX546 | ||
---|---|---|---|---|
CAS Number | 215923-54-9 | Molecular Weight | 247.29000 | |
Density | 1.215g/cm3 | Boiling Point | 422.8ºC at 760 mmHg | |
Molecular Formula | C14H17NO3 | Melting Point | N/A | |
MSDS | USA | Flash Point | 209.5ºC |
Use of CX546CX546 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]. |
Name | 2,3-dihydro-1,4-benzodioxin-6-yl(piperidin-1-yl)methanone |
---|---|
Synonym | More Synonyms |
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 | |
References |
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℃ |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
---|---|
RIDADR | NONH for all modes of transport |
HS Code | 2934999090 |
HS Code | 2934999090 |
---|---|
Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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... |
CX 546 |
Lopac-C-271 |
BDP 17 |
GR 87 |
CX546 |