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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1977 1
1978 1
1980 1
1981 1
1982 1
1983 7
1984 24
1985 28
1986 34
1987 55
1988 85
1989 57
1990 62
1991 56
1992 56
1993 54
1994 47
1995 55
1996 73
1997 84
1998 97
1999 94
2000 104
2001 107
2002 94
2003 107
2004 112
2005 129
2006 161
2007 185
2008 160
2009 200
2010 254
2011 232
2012 233
2013 199
2014 213
2015 191
2016 218
2017 211
2018 215
2019 221
2020 237
2021 209
2022 190
2023 187
2024 189
2025 212
2026 124

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5,271 results

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Page 1
Development of dual GPBAR1 agonist and RORgammat inverse agonist for the treatment of inflammatory bowel diseases.
Biagioli M, Di Giorgio C, Morretta E, Bellini R, Massa C, Urbani G, Bordoni M, Marchianò S, Lachi G, Sepe V, Monti MC, Distrutti E, Zampella A, Fiorucci S. Biagioli M, et al. Pharmacol Res. 2024 Oct;208:107403. doi: 10.1016/j.phrs.2024.107403. Epub 2024 Sep 10. Pharmacol Res. 2024. PMID: 39265668 Free article.
This study evaluates the therapeutic potential of PBT002, a dual GPBAR1 agonist and RORgammat inverse agonist, in IBD models. The effects of PBT002 were assessed through in vitro and in vivo experiments. ...In DSS+IL-23 induced colitis, PBT002 mitigated disea …
This study evaluates the therapeutic potential of PBT002, a dual GPBAR1 agonist and RORgammat inverse agonist, in IBD m …
Efficacy and Safety of Histamine H3 Receptor Antagonist/Inverse Agonist Including Betahistine for Schizophrenia: A Systematic Review and Meta-Analysis.
Nishii Y, Sakuma K, Hamanaka S, Iwata N, Kishi T. Nishii Y, et al. Neuropsychopharmacol Rep. 2025 Sep;45(3):e70034. doi: 10.1002/npr2.70034. Neuropsychopharmacol Rep. 2025. PMID: 40567153 Free PMC article.
AIM: Whether histamine H3 receptor antagonists (H3R-ANTs)/inverse agonists (H3R-IAs) provides benefit for the treatment of schizophrenia remains unclear. ...Betahistine has an H1-receptor agonistic reaction and H3-receptor antagonistic reaction, while other drugs only have …
AIM: Whether histamine H3 receptor antagonists (H3R-ANTs)/inverse agonists (H3R-IAs) provides benefit for the treatment of schizophre …
An oral, liver-restricted LXR inverse agonist for dyslipidemia: preclinical development and phase 1 trial.
Li X, Benegiamo G, Vijayakumar A, Sroda N, Kimura M, Huss RS, Weng S, Murakami E, Kirby BJ, von Alvensleben GVG, Kremoser C, Gane EJ, Takebe T, Myers RP, Subramanian GM, Auwerx J. Li X, et al. Nat Med. 2026 Mar;32(3):883-893. doi: 10.1038/s41591-025-04169-6. Epub 2026 Jan 16. Nat Med. 2026. PMID: 41545590 Free PMC article.
Liver X receptor (LXR) repression can reduce plasma TG and cholesterol and improve insulin sensitivity by suppressing de novo lipogenesis and intestinal lipid absorption and enhancing clearance of TG-rich lipoproteins, but its clinical utility remains unexplored. Here we demonstr …
Liver X receptor (LXR) repression can reduce plasma TG and cholesterol and improve insulin sensitivity by suppressing de novo lipogenesis an …
Histamine H1 receptor inverse agonists improve structure and pain in an osteoarthritis mouse model.
Kurakazu I, Olmer M, Swahn H, Myers K, Kenvisay C, Akasaki Y, Nakashima Y, Lotz MK. Kurakazu I, et al. J Clin Invest. 2025 Aug 28;135(21):e183588. doi: 10.1172/JCI183588. eCollection 2025 Nov 3. J Clin Invest. 2025. PMID: 40875519 Free PMC article.
Here, we sought to discover FOXO activators and found that cyproheptadine, a histamine H1 receptor (HRH1) inverse agonist, promoted FOXO3 nuclear translocation and increased FOXO target genes while suppressing inflammation. ...Our findings suggest that HRH1 constitu …
Here, we sought to discover FOXO activators and found that cyproheptadine, a histamine H1 receptor (HRH1) inverse agonist, pro …
Cannabinoid receptors: where they are and what they do.
Mackie K. Mackie K. J Neuroendocrinol. 2008 May;20 Suppl 1:10-4. doi: 10.1111/j.1365-2826.2008.01671.x. J Neuroendocrinol. 2008. PMID: 18426493 Review.
Both CB(1) and CB(2) couple primarily to inhibitory G proteins and are subject to the same pharmacological influences as other GPCRs. Thus, partial agonism, functional selectivity and inverse agonism all play important roles in determining the cellular respon …
Both CB(1) and CB(2) couple primarily to inhibitory G proteins and are subject to the same pharmacological influences as other GPCRs. Thus, …
Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease.
Brice NL, Schiffer HH, Monenschein H, Mulligan VJ, Page K, Powell J, Xu X, Cheung T, Burley JR, Sun H, Dickson L, Murphy ST, Kaushal N, Sheardown S, Lawrence J, Chen Y, Bartkowski D, Kanta A, Russo J, Hosea N, Dawson LA, Hitchcock SH, Carlton MB. Brice NL, et al. J Pharmacol Exp Ther. 2021 Jun;377(3):407-416. doi: 10.1124/jpet.120.000438. Epub 2021 Apr 1. J Pharmacol Exp Ther. 2021. PMID: 33795395
In this study, we describe the in vitro and in vivo pharmacological characterization of (R)-1-(2-(4-(2,4-difluorophenoxy)piperidin-1-yl)-3-((tetrahydrofuran-3-yl)amino)-7,8-dihydropyrido[3,4-b]pyrazin-6(5H)-yl)ethan-1-one (CVN424), a highly potent and selective small-molecule …
In this study, we describe the in vitro and in vivo pharmacological characterization of (R)-1-(2-(4-(2,4-difluorophenoxy)piperidin-1-yl)-3-( …
5-HT 2A receptor inverse agonist attenuates morphine withdrawal syndrome and its aversiveness in rats.
Tsai PH, Morales ER, Reed YY, Qamar H, Jones EF, Saji G, Ward CP, Burstein ES, Moreno GL, Malin DH. Tsai PH, et al. Behav Pharmacol. 2025 Aug 1;36(5):234-245. doi: 10.1097/FBP.0000000000000832. Epub 2025 May 16. Behav Pharmacol. 2025. PMID: 40392225 Free PMC article.
Pimavanserin is a selective 5-HT 2A receptor inverse agonist in current medical use. A day after termination of drug infusion, rats were injected s.c. with 0.3 or 1.0 mg/kg pimavanserin or saline alone. ...
Pimavanserin is a selective 5-HT 2A receptor inverse agonist in current medical use. A day after termination of drug in …
RORgammat inverse agonist TF-S14 inhibits Th17 cytokines and prolongs skin allograft survival in sensitized mice.
Fouda A, Maallah MT, Kouyoumdjian A, Negi S, Paraskevas S, Tchervenkov J. Fouda A, et al. Commun Biol. 2024 Apr 12;7(1):454. doi: 10.1038/s42003-024-06144-2. Commun Biol. 2024. PMID: 38609465 Free PMC article.
Additionally, we investigated the therapeutic potential of novel inverse agonists of the retinoic acid receptor-related orphan receptor gamma t (RORgammat) in the treatment of skin allograft rejection in sensitized mice. Our results show that RORgammat inverse agoni …
Additionally, we investigated the therapeutic potential of novel inverse agonists of the retinoic acid receptor-related orphan recept …
A cannabinoid receptor 1 inverse agonist induces weight loss and reduces airway hyperresponsiveness in a mouse model of obese asthma.
Morris CR, Chandrasekaran R, Butzirus IM, Daphtary N, Aliyeva M, Manuel AM, Tharp WG, Bates JHT, Anathy V, Poynter ME, Duan J, Gaucher G, Crater GD, Dixon AE. Morris CR, et al. Am J Physiol Lung Cell Mol Physiol. 2025 Sep 1;329(3):L327-L340. doi: 10.1152/ajplung.00049.2025. Epub 2025 Jul 24. Am J Physiol Lung Cell Mol Physiol. 2025. PMID: 40707031 Free article.
The endocannabinoid system plays a significant role in metabolism; inhibition of cannabinoid receptor 1 (CB(1)R) induces weight loss and improves serum lipid profiles. We used a CB(1)R inverse agonist, INV-202, in a mouse model of obese asthma and investigated chang …
The endocannabinoid system plays a significant role in metabolism; inhibition of cannabinoid receptor 1 (CB(1)R) induces weight loss and imp …
Structural Basis of PPARgamma-Mediated Transcriptional Repression by the Covalent Inverse Agonist FX-909.
Laughlin ZT, Arifova L, Munoz-Tello P, Yu X, Giridhar MNK, Dong J, Harp JM, Zhu D, Kamenecka TM, Kojetin DJ. Laughlin ZT, et al. J Med Chem. 2025 Aug 28;68(16):17587-17597. doi: 10.1021/acs.jmedchem.5c01252. Epub 2025 Aug 12. J Med Chem. 2025. PMID: 40797371 Free PMC article.
Hyperactivation of peroxisome proliferator-activated receptor gamma-mediated transcription promotes tumor growth in urothelial (bladder) cancer, which can be inhibited by compounds that repress PPARgamma activity. FX-909 is a covalent PPARgamma inverse agonist in ph …
Hyperactivation of peroxisome proliferator-activated receptor gamma-mediated transcription promotes tumor growth in urothelial (bladder) can …
5,271 results