For research use only. Not for therapeutic Use.
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control[1].
TAN-452 (1, 3, 10 mg/kg for p.o. or 0.3, 1, 3 mg/kg for s.c.) suppresses morphine-induced emesis in ferrets[1].
TAN-452 (30 mg/kg/2 mL for PO or 3 mg/kg/mL for IV) has a T1/2 of 2.1 hours[1].
TAN-452 suppresses morphine-induced small intestinal transit (SIT) inhibition in a dose-dependent manner. Administration of TAN-452 at 30 mg/kg alone does not affect SIT[1].
TAN-452 (10, 30 mg/kg; s.c.) significantly suppresses morphine-induced antinociception 30 min after administration. TAN-452 (po) produces no effect up to 300 mg/kg[1].
| Catalog Number | I036994 |
| CAS Number | 892039-23-5 |
| Synonyms | ethyl (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)-heptaene-8-carboxylate |
| Molecular Formula | C29H30N2O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H30N2O5/c1-2-35-27(33)17-5-7-18-19-13-29(34)22-12-16-6-8-21(32)25-23(16)28(29,9-10-31(22)14-15-3-4-15)26(36-25)24(19)30-20(18)11-17/h5-8,11,15,22,26,30,32,34H,2-4,9-10,12-14H2,1H3/t22-,26+,28+,29-/m1/s1 |
| InChIKey | JOJGLAWHRDFWNQ-KFDULEKRSA-N |
| SMILES | CCOC(=O)C1=CC2=C(C=C1)C3=C(N2)C4C56CCN(C(C5(C3)O)CC7=C6C(=C(C=C7)O)O4)CC8CC8 |
| Reference | [1]. Tsutomu Suzuki, et al. Pharmacological profile of TAN-452, a novel peripherally acting opioid receptor antagonist for the treatment of opioid-induced bowel syndromes. Life Sci. 2018 Dec 15;215:246-252. |
