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. Author manuscript; available in PMC: 2017 Feb 11.
Published in final edited form as: J Med Chem. 2016 Mar 14;59(15):7011–7028. doi: 10.1021/acs.jmedchem.5b01499

Table 1.

Status of NOP-targeted compounds that entered clinical development

Compound
Name		 Structure NOP profile Clinical Phase (Ref) Indication
1
Cebranopadol		 graphic file with name nihms-810265-t0004.jpg NOP full
agonist-MOP
full agonist		 Ongoing
Phase III42, 43 		Various Pain
modalities
2
LY2940094		 graphic file with name nihms-810265-t0005.jpg NOP antagonist Completed
Phase II45, 46 		Major Depressive
Disorder
Alcohol
Dependence
3
MK-5757		 graphic file with name nihms-810265-t0006.jpg NOP antagonist Completed
Phase II48 		Cognitive
Impairment in
Schizophrenia
4
SCH486757		 graphic file with name nihms-810265-t0007.jpg NOP full agonist Completed
Phase I
(Discontinued)57 		Cough
5
JNJ-19385899		 Not available NOP agonist Completed Phase I
(No information)51 		Anxiety and
Depression
6
Ser100, (ZP120)		 Ac-RYYRWKKKKKKK-NH2 NOP partial
agonist		 Completed
Phase IIa56 		Treatment
resistant systolic
hypertension
7
JTC-801		 graphic file with name nihms-810265-t0008.jpg NOP antagonist Completed
Phase II59 		Neuropathic Pain
Postoperative
Pain
N/OFQ FGGFTGARKSARKLANQ Natural ligand
NOP agonist		 Completed
Exploratory Phase II60 		Neurogenic
urinary
incontinence