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

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Repinotan hydrochloride) usually boasts enhanced water solubility and stability.

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].

MedChemExpress (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].

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

Clinical Trial
Molecular Weight

400.49

Formula

C21H24N2O4S

CAS No.
SMILES

O=C(C1=C2C=CC=C1)N(CCCCNC[C@H]3CCC4=CC=CC=C4O3)S2(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Repinotan Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Repinotan
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HY-12959
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