1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor
  3. WAY-100635

WAY-100635 

Cat. No.: HY-10349
Handling Instructions

WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.

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

WAY-100635 Chemical Structure

WAY-100635 Chemical Structure

CAS No. : 162760-96-5

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Description

WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist[1][2][3].

IC50 & Target

5-HT1A Receptor

8.87 (pIC50)

5-HT1A Receptor

9.71 (pA2)

In Vitro

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D2L or D4.4 receptors[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D2L, D3, and D4.2 receptors, respectively. Saturation analyses demonstrat that the Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D4.4 cells with EC50 of 9.7 nM. WAY-100635 possesses high affinity for D4.4 receptor (3.3 nM) [1].

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

In Vivo

WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat[2].

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

Animal Model: Male Sprague-Dawley rats (220-240 g)[2]
Dosage: 1 mg/kg
Administration: Subcutaneous injection (Pharmacokinetic study)
Result: Reduced total abstinence score, increased immobility time and the burying behavior was increased.
Molecular Weight

422.56

Formula

C₂₅H₃₄N₄O₂

CAS No.

162760-96-5

SMILES

O=C(N(C1=NC=CC=C1)CCN2CCN(CC2)C3=CC=CC=C3OC)C4CCCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

WAY-100635WAY100635WAY 1006355-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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WAY-100635
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