A κ-opioid receptor antagonist
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Product Categories

Product Type

Small Molecule Modulators
Receptor Pharmacology
Antagonists

Research Area

GNTI (hydrochloride)

Item No. 31597

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[(4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,8a,9,14,14b-octahydro-1,8a-dihydroxy-4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazol-11-yl]-guanidine, dihydrochloride
CAS Number
351183-88-5
Synonyms
  • 5'-Guanidinonaltrindole
Molecular Formula
C27H29N5O3 • 2HCl
Formula Weight
544.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 48 mg/mlWater: 40 mg/ml
SMILES
O[C@]12[C@@]34C5=C(C[C@H]2N(CC4)CC6CC6)C=CC(O)=C5O[C@@]3([H])C7=C(C8=CC(NC(N)=N)=CC=C8N7)C1.Cl.Cl
InChi Code
InChI=1S/C27H29N5O3.2ClH/c28-25(29)30-15-4-5-18-16(10-15)17-11-27(34)20-9-14-3-6-19(33)23-21(14)26(27,24(35-23)22(17)31-18)7-8-32(20)12-13-1-2-13;;/h3-6,10,13,20,24,31,33-34H,1-2,7-9,11-12H2,(H4,28,29,30);2*1H/t20-,24+,26+,27-;;/m1../s1
InChi Key
VLZVKCDTFJURGK-AWCPWCJTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    GNTI is a κ-opioid receptor antagonist (Ki = 0.18 nM).1 It is selective for κ-opioid receptors over µ- and δ-opioid receptors in radioligand binding assays (Kis = 36.9 and 70 nM, respectively). GNTI inhibits agonist-induced [35S]GTPγS binding in CHO cells expressing human κ-opioid receptors (pA2 = 10.4). In vivo, GNTI (0.3 mg/kg) induces scratching behavior in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jones, R.M., and Portoghese, P.S. 5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. Eur. J. Pharmacol. 396(1), 49-52 (2000).

    2. Lee, Y.-C., Lin, C.-H., Hung, S.-Y., et al. Manual acupuncture relieves bile acid-induced itch in mice: The role of microglia and TNF-α. Int. J. Med. Sci. 15(9), 953-960 (2018).