1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Repinotan

Repinotan (Synonyms: BAY x 3702 free base)

Cat. No.: HY-12959
Handling Instructions

Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.

For research use only. We do not sell to patients.

Repinotan Chemical Structure

Repinotan Chemical Structure

CAS No. : 144980-29-0

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Description

Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects[1].

IC50 & Target[1]

5-HT1A Receptor

0.19 nM (Ki, In calf hippocampus)

5-HT1A Receptor

0.25 nM (Ki, In rat and human cortex)

5-HT1A Receptor

0.59 nM (Ki, In rat hippocampus)

5-HT7 Receptor

6 nM (Ki)

In Vitro

Repinotan binds with lower affinity to 5-HT7 (Ki = 6 nM), α1- and α2 adrenergic (Ki = 6 nM and 7 nM, respectively), 5-HT1D (36 nM), dopamine D2 and D4 (48 nM and 91 nM, respectively), σ sites (176 nM) and 5-HT2C (310 nM) receptors[1].
Exposure to repinotan protects rat cortical and hippocampal neurons in cultures from apoptosis induced by 25 nM Staurosporine. After Staurosporine-induced apoptosis, Repinotan, at 50 pM to 1 μM, reduces the release of lactate dehydrogenase, DNA fragmentation, and apoptotic body formation in a concentration-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Repinotan (1-100 μg/kg) causes strong, dose-dependent infarct reductions in permanent middle cerebral artery occlusion, transient middle cerebral artery occlusion, and traumatic brain injury paradigms[1].
The half-life of Repinotan in plasma is relatively short (t1/2 = 0.6 h in rat; 0.4 h in rhesus monkeys), and Repinotan is extensively metabolized[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

400.49

Formula

C₂₁H₂₄N₂O₄S

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Repinotan
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HY-12959
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