For research use only. Not for therapeutic Use.
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].
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].
5′-Guanidinonaltrindole (5′-GNTI) (0.03-3 mg/kg; s.c.; once) induces scratching in mice[2].
| Catalog Number | I010386 |
| CAS Number | 351183-88-5 |
| Synonyms | 2-[(1S,2S,13R,21R)-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(10),6,8,15,17,19(25)-heptaen-7-yl]guanidine;dihydrochloride |
| Molecular Formula | C27H31Cl2N5O3 |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | VLZVKCDTFJURGK-AWCPWCJTSA-N |
| SMILES | C1CC1CN2CCC34C5C6=C(CC3(C2CC7=C4C(=C(C=C7)O)O5)O)C8=C(N6)C=CC(=C8)N=C(N)N.Cl.Cl |
| Reference | [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. |
