Drug intelligence / Profile preview

naltrindole

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Intravenous
01

Overview

Naltrindole is a highly potent and selective non-peptide delta opioid receptor antagonist primarily used as a molecular probe in biomedical research, where it serves to characterize the delta opioid receptor's role in pain, reward, and addiction pathways[1][4]. Structurally, it was developed as an analog of naltrexone with an indole group, conferring high specificity for the delta opioid receptor by mimicking the address sequence of endogenous enkephalins[1][7]. Naltrindole is not approved for clinical use but is widely used in preclinical and pharmacological studies where it has been shown to block delta opioid receptor-mediated effects, modulate opioid- and stimulant-induced behaviors, suppress alcohol intake, and, in some models, exert anti-proliferative and immunosuppressive effects by both opioid receptor-dependent and -independent mechanisms[3][6][7][10]. Naltrindole is not a peptide and is a small molecule, allowing it to cross the blood–brain barrier and exhibit central nervous system effects[1].

Other names
4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9H)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, (4bS,8R,8aS,14bR)4,8-Methanobenzofuro(2,3-a)pyrido(4,3-b)carbazole-1,8a(9H)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, (8R-(4bS*,8alpha,8abeta,14bbeta))
02

Targets

DOR (Opioid Receptor Delta 1)

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