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

Year Number of Results
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1997 3
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1,119 results

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Page 1
GPR3, GPR6, and GPR12 as novel molecular targets: their biological functions and interaction with cannabidiol.
Laun AS, Shrader SH, Brown KJ, Song ZH. Laun AS, et al. Acta Pharmacol Sin. 2019 Mar;40(3):300-308. doi: 10.1038/s41401-018-0031-9. Epub 2018 Jun 25. Acta Pharmacol Sin. 2019. PMID: 29941868 Free PMC article. Review.
Using beta-arrestin2 recruitment and cAMP accumulation assays, we recently found that the nonpsychoactive phytocannabinoid cannabidiol (CBD) is an inverse agonist for GPR3, GPR6, and GPR12. This discovery highlights these orphan receptors as potential new molecular targets …
Using beta-arrestin2 recruitment and cAMP accumulation assays, we recently found that the nonpsychoactive phytocannabinoid cannabidiol (CBD) …
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, …
Evidence-based use of antihistamines for treatment of allergic conditions.
Linton S, Hossenbaccus L, Ellis AK. Linton S, et al. Ann Allergy Asthma Immunol. 2023 Oct;131(4):412-420. doi: 10.1016/j.anai.2023.07.019. Epub 2023 Jul 28. Ann Allergy Asthma Immunol. 2023. PMID: 37517656 Review.
Available since the 1940s, H(1) antihistamines are mainstay treatments for allergic conditions such as allergic rhinitis and urticaria. They function as inverse agonists that bind to the H(1) receptor to inhibit histamine-induced inflammation. ...
Available since the 1940s, H(1) antihistamines are mainstay treatments for allergic conditions such as allergic rhinitis and urticaria. They …
Antipsychotic drug action: antagonism, inverse agonism or partial agonism.
Strange PG. Strange PG. Trends Pharmacol Sci. 2008 Jun;29(6):314-21. doi: 10.1016/j.tips.2008.03.009. Epub 2008 May 28. Trends Pharmacol Sci. 2008. PMID: 18471899 Review.
Recently, the D(2)/D(3) partial agonist aripiprazole has been introduced as an antipsychotic drug. It has also been realized that, using in vitro assays, the other antipsychotic drugs are in fact inverse agonists at D(2)/D(3) dopamine receptors. ...It seems that the …
Recently, the D(2)/D(3) partial agonist aripiprazole has been introduced as an antipsychotic drug. It has also been realized that, us …
Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity.
Berg KA, Clarke WP. Berg KA, et al. Int J Neuropsychopharmacol. 2018 Oct 1;21(10):962-977. doi: 10.1093/ijnp/pyy071. Int J Neuropsychopharmacol. 2018. PMID: 30085126 Free PMC article. Review.
Constitutive receptor activity/inverse agonism and functional selectivity/biased agonism are 2 concepts in contemporary pharmacology that have major implications for the use of drugs in medicine and research as well as for the processes of new drug dev …
Constitutive receptor activity/inverse agonism and functional selectivity/biased agonism are 2 concepts in contemporary …
A Systematic Review of Inverse Agonism at Adrenoceptor Subtypes.
Michel MC, Michel-Reher MB, Hein P. Michel MC, et al. Cells. 2020 Aug 19;9(9):1923. doi: 10.3390/cells9091923. Cells. 2020. PMID: 32825009 Free PMC article.
The basal tone of endogenously expressed receptors is often low, leading to less consistent detection and a lesser extent of observed inverse agonism. Extent inverse agonism depends on specific molecular properties of a compound, but inverse …
The basal tone of endogenously expressed receptors is often low, leading to less consistent detection and a lesser extent of observed inv …
Inverse agonism: the classic concept of GPCRs revisited [Review].
Sato J, Makita N, Iiri T. Sato J, et al. Endocr J. 2016 Jun 30;63(6):507-14. doi: 10.1507/endocrj.EJ16-0084. Epub 2016 Mar 8. Endocr J. 2016. PMID: 26961122 Free article. Review.
Although many pharmacological examples of inverse agonism have been identified, its clinical importance is still unclear and debated. Thus, even though inverse agonism of angiotensin receptor blockers (ARBs) has been discussed for more than 10 years, i …
Although many pharmacological examples of inverse agonism have been identified, its clinical importance is still unclear and d …
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 constitutive ac …
Here, we sought to discover FOXO activators and found that cyproheptadine, a histamine H1 receptor (HRH1) inverse agonist, promoted F …
Structural insights into the high basal activity and inverse agonism of the orphan receptor GPR6 implicated in Parkinson's disease.
Barekatain M, Johansson LC, Lam JH, Chang H, Sadybekov AV, Han GW, Russo J, Bliesath J, Brice NL, Carlton MBL, Saikatendu KS, Sun H, Murphy ST, Monenschein H, Schiffer HH, Popov P, Lutomski CA, Robinson CV, Liu ZJ, Hua T, Katritch V, Cherezov V. Barekatain M, et al. Sci Signal. 2024 Dec 3;17(865):eado8741. doi: 10.1126/scisignal.ado8741. Epub 2024 Dec 3. Sci Signal. 2024. PMID: 39626010 Free PMC article.
Here, we solved crystal structures of GPR6 without the addition of a ligand (a pseudo-apo state) and in complex with two inverse agonists, including CVN424, which improved motor symptoms in patients with Parkinson's disease in clinical trials. ...A combination of site-dire …
Here, we solved crystal structures of GPR6 without the addition of a ligand (a pseudo-apo state) and in complex with two inverse agon …
Molecular mechanisms of inverse agonism via kappa-opioid receptor-G protein complexes.
Tyson AS, Khan S, Motiwala Z, Han GW, Zhang Z, Ranjbar M, Styrpejko D, Ramos-Gonzalez N, Woo S, Villers K, Landaker D, Kenakin T, Shenvi R, Majumdar S, Gati C. Tyson AS, et al. Nat Chem Biol. 2025 Jul;21(7):1046-1057. doi: 10.1038/s41589-024-01812-0. Epub 2025 Jan 7. Nat Chem Biol. 2025. PMID: 39775170 Free PMC article.
Here we present biochemical evidence that certain kappa-opioid receptor (KOR) inverse agonists can act via KOR-G(i) protein complexes. To investigate this phenomenon, we determined cryo-EM structures of KOR-G(i) protein complexes with three inverse agonists: JDTic, …
Here we present biochemical evidence that certain kappa-opioid receptor (KOR) inverse agonists can act via KOR-G(i) protein complexes …
1,119 results