| [1] |
Schwartz LW, Osburn BI, Frick OL. 1975. An ontogenic study of histamine and mast cells in the fetal rhesus monkey. |
| [2] |
Schwartz J. 1977. Histaminergic mechanisms in brain. |
| [3] |
Schwartz J, Dibblee M. 1975. The effect of endotoxins and enzymes in vitro on the release of gingival histamine. |
| [4] |
Schwartz JC. 1975. Histamine as a transmitter in brain. |
| [5] |
Arrang JM, Garbarg M, Schwartz JC. 1983. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. |
| [6] |
Arrang JM, Garbarg M, Lancelot JC, Lecomte JM, Pollard H, et al. 1987. Highly potent and selective ligands for histamine H3-receptors. |
| [7] |
Fujimoto K, Mizuguchi H, Fukui H, Wada H. 1991. Presynaptic localization of histamine H3-receptors in rat brain. |
| [8] |
Lovenberg TW, Roland BL, Wilson SJ, Jiang X, Pyati J, et al. 1999. Cloning and functional expression of the human histamine H3 receptor. |
| [9] |
Cogé F, Guénin SP, Audinot V, Renouard-Try A, Beauverger P, et al. 2001. Genomic organization and characterization of splice variants of the human histamine H3 receptor. |
| [10] |
Pillot C, Heron A, Cochois V, Tardivel-Lacombe J, Ligneau X, et al. 2002. A detailed mapping of the histamine H3 receptor and its gene transcripts in rat brain. |
| [11] |
Schlicker E, Kathmann M. 2017. Role of the histamine H3 receptor in the central nervous system. |
| [12] |
Ellenbroek BA. 2013. Histamine H3 receptors, the complex interaction with dopamine and its implications for addiction. |
| [13] |
Arrang JM, Morisset S, Gbahou F. 2007. Constitutive activity of the histamine H3 receptor. |
| [14] |
Schwartz JC. 2011. The histamine H3 receptor: from discovery to clinical trials with pitolisant. |
| [15] |
Schlicker E, Malinowska B, Kathmann M, Göthert M. 1994. Modulation of neurotransmitter release via histamine H3 heteroreceptors. |
| [16] |
Brioni JD, Esbenshade TA, Garrison TR, Bitner SR, Cowart MD. 2011. Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease. |
| [17] |
Ligneau X, Landais L, Perrin D, Piriou J, Uguen M, et al. 2007. Brain histamine and schizophrenia: potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649. |
| [18] |
Hancock AA, Fox GB. 2004. Perspectives on cognitive domains, H3 receptor ligands and neurological disease. |
| [19] |
Ligneau X, Perrin D, Landais L, Camelin JC, Calmels TPG, et al. 2007. BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: preclinical pharmacology. |
| [20] |
Sadek B, Saad A, Sadeq A, Jalal F, Stark H. 2016. Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases. |
| [21] |
Rahman SN, Imhaouran F, Leurs R, Christopoulos A, Valant C, et al. 2024. Ligand-directed biased agonism at human histamine H3 receptor isoforms across Gαi/o- and β-arrestin2-mediated pathways. |
| [22] |
Alhusaini M, Eissa N, Saad AK, Beiram R, Sadek B. 2022. Revisiting preclinical observations of several histamine H3 receptor antagonists/inverse agonists in cognitive impairment, anxiety, depression, and sleep-wake cycle disorder. |
| [23] |
Xu J, Pittenger C. 2023. The histamine H3 receptor modulates dopamine D2 receptor-dependent signaling pathways and mouse behaviors. |
| [24] |
Zhou Z, Zhang Y, Han F, Chen Z, Zheng Y. 2023. Umbelliferone protects against cerebral ischemic injury through selective autophagy of mitochondria. |
| [25] |
Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, et al. 2024. Structural basis of ligand recognition and activation of the histamine receptor family. |
| [26] |
Shen Q, Tang X, Wen X, Cheng S, Xiao P, et al. 2024. Molecular determinant underlying selective coupling of primary G-protein by class A GPCRs. |
| [27] |
Jin SS, Zhang H, Yan JH, Wu CR, Cai XQ, et al. 2026. Decoding ligand recognition and constitutive activation of histamine H3 and H4 receptors. |
| [28] |
Höring C, Conrad M, Söldner CA, Wang J, Sticht H, et al. 2021. Specific engineered G protein coupling to histamine receptors revealed from cellular assay experiments and accelerated molecular dynamics simulations. |
| [29] |
Conrad M, Söldner CA, Miao Y, Sticht H. 2020. Agonist binding and G protein coupling in histamine H2 receptor: a molecular dynamics study. |
| [30] |
Inoue A, Raimondi F, Kadji FMN, Singh G, Kishi T, et al. 2019. Illuminating G-protein-coupling selectivity of GPCRs. |
| [31] |
Zheng Y, Liao J, Fang Z, Tang X, Zhou Z, et al. 2026. Biased histamine signaling selectively gates fat preference. |
| [32] |
Yan H, Zhang X, Hu W, Ma J, Hou W, et al. 2014. Histamine H3 receptors aggravate cerebral ischaemic injury by histamine-independent mechanisms. |
| [33] |
Peng X, Yang L, Liu Z, Lou S, Mei S, et al. 2022. Structural basis for recognition of antihistamine drug by human histamine receptor. |
| [34] |
García-Gálvez AM, Escamilla-Sánchez J, Flores-Maldonado C, Contreras RG, Arias JM, et al. 2018. Differential homologous desensitization of the human histamine H3 receptors of 445 and 365 amino acids expressed in CHO-K1 cells. |
| [35] |
Rahman SN, McNaught-Flores DA, Huppelschoten Y, da Costa Pereira D, Christopoulos A, et al. 2023. Structural and molecular determinants for isoform bias at human histamine H3 receptor isoforms. |
| [36] |
Dehkhoda F, Xing J, Misganaw D, Mutunduwe K, Han MN, et al. 2026. GPCR crosstalk beyond obligate dimerisation: effector coincidence detection, compartmentation, and pharmacological implications. |
| [37] |
Cong Z, Liang YL, Zhou Q, Darbalaei S, Zhao F, et al. 2022. Structural perspective of class B1 GPCR signaling. |
| [38] |
Gao M, Dekker ME, Leurs R, Vischer HF. 2024. Pharmacological characterization of seven human histamine H3 receptor isoforms. |
| [39] |
Riddy DM, Cook AE, Diepenhorst NA, Bosnyak S, Brady R, et al. 2017. Isoform-specific biased agonism of histamine H3 receptor agonists. |
| [40] |
Gbahou F, Rouleau A, Arrang JM. 2012. The histamine autoreceptor is a short isoform of the H3 receptor. |
| [41] |
Gao M, Ooms JF, Leurs R, Vischer HF. 2024. Histamine H3 receptor isoforms: insights from alternative splicing to functional complexity. |
| [42] |
Bhatia S, Field MA, Hebbard L, Schmitz U. 2025. Bioinformatics frameworks for single-cell long-read sequencing: unlocking isoform-level resolution. |
| [43] |
Joglekar A, Hu W, Zhang B, Narykov O, Diekhans M, et al. 2024. Single-cell long-read sequencing-based mapping reveals specialized splicing patterns in developing and adult mouse and human brain. |
| [44] |
Huang CK, Lin WD, Wu SH. 2022. An improved repertoire of splicing variants and their potential roles in Arabidopsis photomorphogenic development. |
| [45] |
Fu Y, Kim H, Roy S, Huang S, Adams JI, et al. 2025. Single cell and spatial alternative splicing analysis with nanopore long read sequencing. |
| [46] |
Hansen MS, Hill CJ, Sussel L, Wells KL. 2026. Optimizing single-cell long-read sequencing for enhanced isoform detection in pancreatic islets. |
| [47] |
Han SW, Jewell S, Thomas-Tikhonenko A, Barash Y. 2024. Contrasting and combining transcriptome complexity captured by short and long RNA sequencing reads. |
| [48] |
Ake F, Schilling M, Fernández-Moya SM, Jaya Ganesh A, Gutiérrez-Franco A, et al. 2025. Quantification of transcript isoforms at the single-cell level using SCALPEL. |
| [49] |
Rapanelli M, Frick LR, Horn KD, Schwarcz RC, Pogorelov V, et al. 2016. The histamine H3 receptor differentially modulates mitogen-activated protein kinase (MAPK) and Akt signaling in striatonigral and striatopallidal neurons. |
| [50] |
Jiang L, Cheng L, Chen H, Dai H, An D, et al. 2021. Histamine H2 receptor negatively regulates oligodendrocyte differentiation in neonatal hypoxic-ischemic white matter injury. |
| [51] |
Pittenger C. 2020. The histidine decarboxylase model of tic pathophysiology: a new focus on the histamine H3 receptor. |
| [52] |
Rapanelli M, Frick L, Pogorelov V, Ohtsu H, Bito H, et al. 2017. Histamine H3R receptor activation in the dorsal striatum triggers stereotypies in a mouse model of tic disorders. |
| [53] |
Rapanelli M, Frick L, Jindachomthong K, Xu J, Ohtsu H, et al. 2018. Striatal signaling regulated by the H3R histamine receptor in a mouse model of tic pathophysiology. |
| [54] |
Nakajima A, Kaneko H, Oyama K, Kuchiji M, Itakura A, et al. 2026. Activity-restoring mutations in the histamine H3 receptor increase constitutive activity and reduce structural stability. |
| [55] |
Oesterhelt D, Stoeckenius W. 1971. Rhodopsin-like protein from the purple membrane of Halobacterium halobium. |
| [56] |
Nagel G, Ollig D, Fuhrmann M, Kateriya S, Musti AM, et al. 2002. Channelrhodopsin-1: a light-gated proton channel in green algae. |
| [57] |
Nagel G, Szellas T, Huhn W, Kateriya S, Adeishvili N, et al. 2003. Channelrhodopsin-2, a directly light-gated cation-selective membrane channel. |
| [58] |
Boyden ES, Zhang F, Bamberg E, Nagel G, Deisseroth K. 2005. Millisecond-timescale, genetically targeted optical control of neural activity. |
| [59] |
Deisseroth K, Feng G, Majewska AK, Miesenböck G, Ting A, et al. 2006. Next-generation optical technologies for illuminating genetically targeted brain circuits. |
| [60] |
Wijtmans M, Josimovic I, Vischer HF, Leurs R. 2022. Optical control of Class A G protein-coupled receptors with photoswitchable ligands. |
| [61] |
Raabe K, Kalaba P, Yong XLH, Crudeli G, Melzer S, et al. 2026. Photocaged oxytocin and vasopressin probes to decipher neuropeptide signalling with high spatiotemporal resolution. |
| [62] |
Maleeva G, Matera C, Roda S, Colleoni A, De Amici M, et al. 2025. Molecular tools to study and control dopaminergic neurotransmission with light. |
| [63] |
Zhou X, Du L, Li M. 2025. Recent progress in azobenzene-based in vivo photopharmacology. |
| [64] |
Hu T, Zheng G, Xue D, Zhao S, Li F, et al. 2021. Rational remodeling of atypical scaffolds for the design of photoswitchable cannabinoid receptor tools. |
| [65] |
Donthamsetti P, Konrad DB, Hetzler B, Fu Z, Trauner D, et al. 2021. Selective photoswitchable allosteric agonist of a G protein-coupled receptor. |
| [66] |
Josimovic I, Zheng Y, Wang Z, van der Meer T, Wijtmans M, et al. 2026. Optical control of H1 receptor signaling with a BODIPY-photocaged antihistamine. |
| [67] |
Hauwert NJ, Mocking TAM, Da Costa Pereira D, Kooistra AJ, Wijnen LM, et al. 2018. Synthesis and characterization of a bidirectional photoswitchable antagonist toolbox for real-time GPCR photopharmacology. |
| [68] |
Roche O, Nettekoven M, Vifian W, Sarmiento RM. 2008. Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists. |
| [69] |
Wijtmans M, Celanire S, Snip E, Gillard MR, Gelens E, et al. 2008. 4-Benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists. |
| [70] |
Ferrada C, Moreno E, Casadó V, Bongers G, Cortés A, et al. 2009. Marked changes in signal transduction upon heteromerization of dopamine D1 and histamine H3 receptors. |
| [71] |
Moreno-Delgado D, Puigdellívol M, Moreno E, Rodríguez-Ruiz M, Botta J, et al. 2020. Modulation of dopamine D1 receptors via histamine H3 receptors is a novel therapeutic target for Huntington's disease. |
| [72] |
Lin W, Zhu X, Yu X, Xia Q, Yan M, et al. 2025. BNST-projecting histaminergic circuits mediate state-dependent anxiety behavior through post-synaptic histamine H3 receptors on GABAergic neurons. |
| [73] |
Zhao X, Yan Y, Liang J, Zhang Y, Li M, et al. 2026. Histamine H3 receptors in the paraventricular thalamus link sleep loss to fat overconsumption. |
| [74] |
Ma Y, Patterson B, Zhu L. 2025. Biased signaling in GPCRs: structural insights and implications for drug development. |
| [75] |
Xu N, Legall E, Johnson RH, Zhu L, Liu W. 2025. Elucidating biased signaling in class A GPCRs. |
| [76] |
Wang T, Wang Y, Xie H, Wu Z, Yu S, et al. 2025. Tegileridine for moderate-to-severe acute pain following abdominal surgery: a randomized, double-blind, phase 3 clinical trial. |
| [77] |
Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, et al. 2022. Structure-based evolution of G protein-biased μ-opioid receptor agonists. |
| [78] |
Markham A. 2020. Oliceridine: first approval. |
| [79] |
Kelly E, Conibear A, Henderson G. 2023. Biased agonism: lessons from studies of opioid receptor agonists. |
| [80] |
Suno-Ikeda C, Nishikawa R, Suzuki R, Yokoi S, Iwata S, et al. 2025. Structural and dynamic insights into the biased signaling mechanism of the human kappa opioid receptor. |
| [81] |
Namkung Y, Le Gouill C, Lukashova V, Kobayashi H, Hogue M, et al. 2016. Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET. |
| [82] |
Kuramoto R, Ikuta T, Carino CMC, Kawakami K, Kushiro M, et al. 2025. Membrane-domain compartmentalization of active GPCRs by β-arrestins through PtdIns(4, 5)P2 binding. |
| [83] |
Wang J, Hanada K, Staus DP, Makara MA, Dahal GR, et al. 2017. Gαi is required for carvedilol-induced β1 adrenergic receptor β-arrestin biased signaling. |
| [84] |
Kumari P, Srivastava A, Banerjee R, Ghosh E, Gupta P, et al. 2016. Functional competence of a partially engaged GPCR-β-arrestin complex. |
| [85] |
Shao Z, Yin J, Chapman K, Grzemska M, Clark L, et al. 2016. High-resolution crystal structure of the human CB1 cannabinoid receptor. |
| [86] |
Yang X, Wang X, Xu Z, Wu C, Zhou Y, et al. 2022. Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1. |
| [87] |
Shen S, Wu C, Lin G, Yang X, Zhou Y, et al. 2024. Structure-based identification of a G protein-biased allosteric modulator of cannabinoid receptor CB1. |
| [88] |
Arroyo-Urea S, Nazarova AL, Carrión-Antolí Á, Bonifazi A, Battiti FO, et al. 2024. A bitopic agonist bound to the dopamine 3 receptor reveals a selectivity site. |
| [89] |
Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, et al. 2023. Structure-based design of bitopic ligands for the µ-opioid receptor. |
| [90] |
Waldhoer M, Fong J, Jones RM, Lunzer MM, Sharma SK, et al. 2005. A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. |
| [91] |
Zangrandi L, Burtscher J, MacKay JP, Colmers WF, Schwarzer C. 2016. The G-protein biased partial κ opioid receptor agonist 6'-GNTI blocks hippocampal paroxysmal discharges without inducing aversion. |
| [92] |
Liao YY, Zhang H, Shen Q, Cai C, Ding Y, et al. 2023. Snapshot of the cannabinoid receptor 1-arrestin complex unravels the biased signaling mechanism. |
| [93] |
Hishinuma S, Kosaka K, Akatsu C, Uesawa Y, Fukuiet H, et al. 2017. Asp73-dependent and -independent regulation of the affinity of ligands for human histamine H1 receptors by Na+. |
| [94] |
Nagl, M. 2024. Synthesis and pharmacological characterization of bivalent and fluorescent ligands to detect receptor dimerization for the D2-H3 heteromer. Dissertation. University of Regensburg, Regensburg, Germany doi: 10.5283/epub.53449 |
| [95] |
Mönnich, D. 2025. Characterization of monomers and heteromers of the dopamine and histamine receptor families using bioluminescence- and radioactivity-based techniques. Dissertation. University of Regensburg, Regensburg, German doi: 10.5283/epub.58594 |
| [96] |
Arora S, Layek B, Singh J. 2021. Design and validation of liposomal ApoE2 gene delivery system to evade blood-brain barrier for effective treatment of Alzheimer's disease. |
| [97] |
Xiao H, Amarsaikhan O, Zhao Y, Yu X, Hu X, et al. 2023. Astrocyte-targeted siRNA delivery by adenosine-functionalized LNP in mouse TBI model. |
| [98] |
Sharma R, Liaw K, Sharma A, Jimenez A, Chang M, et al. 2021. Glycosylation of PAMAM dendrimers significantly improves tumor macrophage targeting and specificity in glioblastoma. |
| [99] |
Fangma Y, Liu M, Liao J, Chen Z, Zheng Y. 2023. Dissecting the brain with spatially resolved multi-omics. |
| [100] |
Xia M, Liu Q, Zhang W, Ge J, Mei Z. 2025. Spatiotemporal dynamics of central nervous system diseases: advancing translational neuropathology via single-cell and spatial multiomics. |
| [101] |
Cao CK, Xu XY, Liang F, Yao M, Chen YY, et al. 2026. Nanobodies in biomedicine: from molecular characteristics to fabrication and clinical translation. |
| [102] |
Li H, Li J, Liu X, Wei X, Zeng X, et al. 2026. Nanotechnology-enhanced CAR-T therapy strategies in cancer, aging, and autoimmune diseases. |
| [103] |
Hawrylycz MJ, Lein ES, Guillozet-Bongaarts AL, Shen EH, Ng L, et al. 2012. An anatomically comprehensive atlas of the adult human brain transcriptome. |
| [104] |
Butler A, Hoffman P, Smibert P, Papalexi E, Satija R. 2018. Integrating single-cell transcriptomic data across different conditions, technologies, and species. |
| [105] |
Andreatta M, Carmona SJ. 2021. UCell: Robust and scalable single-cell gene signature scoring. |
| [106] |
DeTomaso D, Jones MG, Subramaniam M, Ashuach T, Ye CJ, et al. 2019. Functional interpretation of single cell similarity maps. |
| [107] |
Zhang XH, Anderson KM, Dong HM, Chopra S, Dhamala E, et al. 2025. The cell-type underpinnings of the human functional cortical connectome. |
| [108] |
Zhang H, Liu Y, Jiang S, Fang Z, Jiang M, et al. 2026. Transcriptomic and neuroimaging decoding of brain-immune crosstalk in thyroid eye disease. |
| [109] |
Lin W, Xu L, Zheng Y, An S, Zhao M, et al. 2023. Whole-brain mapping of histaminergic projections in mouse brain. |