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(+)-Pentazocine, [Ring-1,3-3H]-,250µCi (9.25MBq)

(+)-Pentazocine radioligand tritiated at the 1,3 position on the ring. Pentazocine is a synthetic opioid shown to bind sigma 1 receptor.

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NET1056025UC
25 µCi
621.00 USD
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NET1056250UC
250 µCi
2022.00 USD
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NET1056001MC
1 mCi
4846.00 USD
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Detail Information

Pentazocine functions as a sigma σ1 receptor agonist, where it has been shown to inhibit the outward current of potassium ions (K+). It is a known analgesic used to treat pain.

We offer both agonist and antagonist radioligands for autoradiographic visualization or performing saturation and competition assays to determine receptor expression levels (Bmax), dissociation constants (Kd), association and dissociation rates (kon and koff), and inhibitor constants (Ki) for a variety of receptors. We develop our radioligands to the highest specific activity possible and provide high purity resulting in low non-specific binding products. Each of our ultra-pure radioligands is fully characterized for pharmacological action and validated in receptor binding assays.

Radiolabeled ligands remain the most sensitive method for probing receptor binding biology; yielding unprecedented sensitivity gives results that technicians and scientists can trust. For over 50 years, PerkinElmer has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET1056:

  1. Dhwanil A. Dalwadi, Seongcheol Kim, John A. Schetz, Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia, In Neurochemistry International, Volume 105, 2017, Pages 21-31.
  2. José Luis Díaz, Ute Christmann, Ariadna Fernández, Antoni Torrens, Adriana Port, Rosalia Pascual, Inés Álvarez, Javier Burgueño, Xavier Monroy, Ana Montero, Ariadna Balada, José Miguel Vela, and Carmen Almansa. Synthesis and Structure–Activity Relationship Study of a New Series of Selective σ1 Receptor Ligands for the Treatment of Pain: 4-Aminotriazoles, In Journal of Medicinal Chemistry, Volume 58, Issue 5, 2015, Pages 2441-2451.

Specifications

Detection Method Radiometric
Label Position Specifically Labeled
Molecular Weight 285.4
Product Brand Name NEN Radiochemicals
Radioisotope H-3
Radionuclide 3H
Receptor Type Opioid
Shipping Condition Dry Ice
Special Ordering Information This is a radioactive product - shipping address must have a license to receive radioactive materials.
Therapeutic Area Pain
Unit Size 250 µCi