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AVN-492 is a potent and selective 5-HT6R antagonist, binds to 5-HT6R (Ki = 91 pM). AVN-492 displays great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc. In mice, the plasma and brain concentrations of AVN-492, given IV at a dose of 2 mg/kg, decreased with time but at both time points, 15 min and 60 min, the brain/plasma ratio (mean±SEM) is nearly the same, at 13.2±0.7% and 9.0±1.5%, respectively.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 359.45 |
| Formula | C17H21N5O2S |
| CAS Number | 1220646-23-0 |
| Purity | >99% |
| Solubility | DMSO ≥ 75 mg/mL |
| Storage | at -20°C |
| Related 5-HT Receptor Products |
|---|
| NLX-101 (F-15599)
NLX-101 (F-15599) is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM. NLX-101 (F-15599) mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors. NLX-101 (F-15599) has over 1000-fold higher affinity for this target over other receptors. |
| Eucalyptol
Eucalyptol is an inhibitor of 5-HT3 receptor, potassium channel, with anti-inflammatory and antioxidant activities. |
| Lasmiditan
Lasmiditan (COL-144; LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist, showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor in vitro binding studies. |
| Paroxetine
Paroxetine is a inhibitor of serotonin uptake. |
| SAM-315
SAM-31 (WAY-255315) is selective 5-Hydroxytryptamine-6 antagonists. |
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