1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. PNU-142633

PNU-142633 

Cat. No.: HY-103131
Handling Instructions

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.

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

PNU-142633 Chemical Structure

PNU-142633 Chemical Structure

CAS No. : 187665-65-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 449 In-stock
Estimated Time of Arrival: December 31
10 mg USD 965 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy[1][2].

IC50 & Target[1]

5-HT1D Receptor

6 nM (Ki)

In Vitro

The intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT in a cytosensor cell-based assay compared with 84% for that of Sumatriptan[1].

In Vivo

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds[1].

Animal Model: Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode[1]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration: Intravenous injection
Result: Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.
Molecular Weight

422.52

Formula

C₂₄H₃₀N₄O₃

CAS No.

187665-65-2

SMILES

O=C(C1=CC=C2C(CCO[[email protected]]2CCN3CCN(C4=CC=C(C(N)=O)C=C4)CC3)=C1)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PNU-142633PNU142633PNU 1426335-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1Danti-migraineplasmaproteinextravasationInhibitorinhibitorinhibit

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PNU-142633
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HY-103131
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