2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. RO5328673

RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (Ki=0.4 nM, Ka=0.1 nM), human NK2 receptors (Ki=1.1 nM, Ka=0.9 nM), and guinea pig NK3 receptors (Ka=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia.

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RO5328673

RO5328673 Chemical Structure

CAS No. : 1310817-94-7

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RO5328673 Related Antibodies

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Description

RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (Ki=0.4 nM, Ka=0.1 nM), human NK2 receptors (Ki=1.1 nM, Ka=0.9 nM), and guinea pig NK3 receptors (Ka=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia[1].

IC50 & Target

hNK2

1.1 nM (Ki)

hNK3

0.4 nM (Ki)

In Vitro

RO5328673 (0.0003-10 μM) binds to hNK2 and hNK3 receptors with high affinity, with corresponding Ki values of 1.1 nM and 0.4 nM, respectively, while it shows weak affinity for the hNK1 receptor (Ki=52.8 nM)[1].
[3H]RO5328673 (0.01-20 nM; 23 °C for hNK2, hNK3, gpNK3 or 37 °C for gpNK3) binds with high affinity to a single saturable site on hNK2, hNK3 and gpNK3 receptors, and its binding to gpNK3 is temperature-independent[1].
RO5328673 (1-300 nM; 20 min) acts as an insurmountable antagonist of hNK3 and gpNK3 receptors, which reduces the maximal response intensity and potency of [MePhe7]NKB, with a stronger effect on gpNK3[1].

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

RO5328673 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Bioavailability CL Vss T1/2
Rat[1] 2 mg/kg i.v. / / 16 mL/min/kg 5 L/kg 3 h
Rat[1] 10 mg/kg p.o. 463 ng/mL 27 % / / /
In Vivo

RO5328673 (10-30 mg/kg; p.o.) robustly reverses senktide (HY-P0187)-induced locomotor activity in gerbils[1].

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

Animal Model: Mongolian gerbils (male and female, weight 40-70 g)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.
Result: Robustly reversed senktide-induced locomotor activity, with group mean total distance traveled reduced compared to vehicle-treated controls.
Produced plasma levels of 688 ng/mL (10 mg/kg dose) and 3508 ng/mL (30 mg/kg dose).
Produced brain levels of 360 ng/mL (10 mg/kg dose) and 1748 ng/mL (30 mg/kg dose).
Resulted in a brain/plasma ratio of 0.5 for both doses.
Molecular Weight

576.49

Formula

C29H32Cl2FN3O4
CAS No.
SMILES

FC(C=C1)=CC=C1OC(N([C@H]2[C@H](C3=CC(Cl)=C(C=C3)Cl)CN(C2)C(C4CCN(CC4)C(C5(CC5)C)=O)=O)C)=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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RO5328673 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.

Keywords:

RO53286731310817-94-7RO 5328673RO-5328673Neurokinin ReceptorNK receptorTachykinin receptor[MePhe 7 ]NKBneurokinin receptor antagonistsenktidehuman NK2 receptorschizophreniahuman NK3 receptorguinea-pig NK3 receptordopaminergic neurongerbilhuman NK1 receptor
Inhibitorinhibitorinhibit

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