351183-88-5

351183-88-5 structure

Name: GNTI dihydrochloride
Chemical Name: N-[(1S,2S,13R)-22-(Cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15(25),16,18-heptaen-7-yl]imidoformamide dihydrochloride
CAS Number: 351183-88-5
Molecular Formula: C₂₇H₃₀Cl₂N₄O₃
Molecular Weight: 529.458
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2018-06-11 01:21:45
Modify Date: 2025-08-25 11:21:37
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor[1].

Name	N-[(1S,2S,13R)-22-(Cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15(25),16,18-heptaen-7-yl]imidoformamide dihydrochloride
Synonyms	Methanimidamide, N-[(4bS,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]-, hydrochloride (1:2) N-[(1S,2S,13R)-22-(Cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15(25),16,18-heptaen-7-yl]imidoformamide dihydro chloride

Description	5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
Target	human κ-opioid receptor:0.18 nM (Ki) human κ-opioid receptor:10.4 (pA2) human μ-opioid receptor:36.9 nM (Ki) human μ-opioid receptor:8.49 (pA2) human δ-opioid receptor:70.0 nM (Ki) human δ-opioid receptor:7.81 (pA2)
In Vitro	5'-Guanidinonaltrindole (5'-GNTI) also binds to human μ- and δ-opioid receptors with Kis of 36.9±2.3 nM and 70.0±0.3 nM, respectively[1]. 5'-Guanidinonaltrindole is most effective at κ-opioid receptors (pA2=10.4±0.10), with substantially lower antagonist potency at μ-opioid (pA2=8.49±0.09) and δ-opioid receptors (pA2=7.81±0.06)[1].
In Vivo	5'-Guanidinonaltrindole (5'-GNTI) (0.03-3 mg/kg; s.c.; once) induces scratching in mice[2]. Animal Model: Male Swiss-Webster mice[2] Dosage: 0.03, 0.1, 0.3, 1 and 3 mg/kg Administration: Subcutaneous injection, once Result: Induced scratching, the scratch A50 value was calculated to be 0.17 mg/kg.
References	[1]. Jones R M, et al. 5′-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. European journal of pharmacology, 2000, 396(1): 49-52. [2]. Cowan A, et al. Itching-like behavior: A common effect of the kappa opioid receptor antagonist 5′-guanidinonaltrindole and the biased kappa opioid receptor agonist 6′-guanidinonaltrindole in mice. Medicine in Drug Discovery, 2021, 11: 100097.

Molecular Formula	C₂₇H₃₀Cl₂N₄O₃
Molecular Weight	529.458
Exact Mass	528.169495

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