1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Trap-101 hydrochloride

Trap-101 hydrochloride 

Cat. No.: HY-11052A
Handling Instructions

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.

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

Trap-101 hydrochloride Chemical Structure

Trap-101 hydrochloride Chemical Structure

CAS No. : 1216621-00-9

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Description

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases[1].

IC50 & Target

pKi: 8.65 (NOP receptor); 6.60 (μ-opioid receptor); 6.14 (κ-opioid receptor); < 5 (δ-opioid receptor)[1]

In Vitro

Trap-101 hydrochloride (3, 30, and 300 nM) is inactive per se up to 10 μM, while in the range 3-300 nM, it produces a concentration dependent rightward shift of the concentration-response curve to N/OFQ without modifications of the maximal response to the agonist. Receptor binding affinities of Trap101 (pKi values) at recombinant human NOP, and classical opioid receptors expressed in CHO cell membranes are 8.65, 6.60, 6.14 and < 5 for NOP, μ-, κ-, and δ-opioid receptors respectively[1].

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

In Vivo

Trap-101 hydrochloride (10-30 mg/kg; detected after 90 min) changes motor activity in naïve rats, it causes a delayed increase in the immobility time in the bar test at 30 mg/kg, Moreover, it increased stepping activity and rotarod performance at 10 mg/kg and reduces them at 30 mg/kg[1].
6-OHDA lesioning produces motor asymmetry mostly affecting the contralateral paw and overall reduced motor performance. Trap-101 hydrochloride (intraperitoneal injection; 10-30 mg/kg; detected after 90 min) alleviates akinesia/bradykinesia and improves overall gait ability in hemiparkinsonian rats, being effective starting at 1 mg/kg and without worsening motor deficit at 30 mg/kg[1].

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

Animal Model: 6-OHDA hemilesioned rats[1]
Dosage: 10-30 mg/kg
Administration: Intraperitoneal injection; 10-30 mg/kg; detected after 90 min
Result: Attenuated parkinsonian-like motor deficits in rat.
Molecular Weight

434.01

Formula

C₂₄H₃₆ClN₃O₂

CAS No.

1216621-00-9

SMILES

O=C1N(CC)C2=CC=CC=C2N1C3=C(CO)CN(CC4CCCCCCC4)CC3.[H]Cl

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:

Trap-101Trap101Trap 101Opioid Receptornervous?systemparkinson's diseaseNOP receptorakinesiabradykinesiaInhibitorinhibitorinhibit

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Trap-101 hydrochloride
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