HBT1 is an AMPA receptor enhancer that induces the production of brain-derived neurotrophic factor (BDNF) and has little or no excitatory effect in primary neurons. HBT1 binds to the ligand binding domain of AMPA-R in a glutamate-dependent manner.
HBT1 bound to the ligand-binding domain (LBD) of AMPA-R in a glutamate-dependent manner.?The mode of HBT1 and LY451395 binding to a pocket in the LBD of AMPA-R differed: HBT1, formed hydrogen bonds with S518 in the LBD.?Lower agonistic profile of HBT1 may associate with its lower risks of bell-shaped responses in BDNF production in primary neurons.
HBT1 Powder Base Information
Name: HBT1 powder
CAS: 489408-02-8
Purity: 98%
Chemical name: 2-(((5-Methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetyl)amino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
Synonyms: HBT1; HBT-1; HBT 1
Molecular Formula: C16H17F3N4O2S
Molecular Weight: 386.39
Melting Point: /
Form: powder
Appearance: white to beige
Solubility: DMSO: 2 mg/mL, clear
Storage Condition: 0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Application: AMPA receptor potentiator
Benefits of HBT1
AMPA-R agonists, which can activate all AMPA-Rs, including resting receptors, have been shown to induce both desensitization of AMPA-R and seizure (Yamada, 1998; Beattie et al., 2000; Ehlers, 2000). AMPA-R potentiators are considered to have better pharmacological profiles because of their selective enhancement of physiologic activation of AMPA-Rs in the brain. However, AMPA-R potentiators such as LY451646, LY451395, and S18986 are reported to elicit bell-shaped responses in various pharmacological effects: LY451646 is reported to show bell-shaped responses in in vivo BDNF induction, and the bell-shaped response of LY451395 in the radial maze task was described in the introduction section of a report about LY451395 (Mackowiak et al., 2002; Bai et al., 2003; Fowler et al., 2004; Jhee et al., 2006; Bernard et al., 2010). PF-4778574 is reported to have less than a 30-fold safety margin against seizure in rodents (Shaffer et al., 2013). Thus, discovery of AMPA-R potentiators with lower risks of these issues is needed.
Dosage form application
- Pure powder form without excipients for research use.
- Tablet or capsule for /dietary supplement/prescription /nootropics use.
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