- Home
- Knowledge Base
- References
References
Discovery and development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A novel, potent, selective, and orally active histamine H3 receptor inverse agonist with robust wake-promoting activity.
Nirogi R, Shinde A, Mohammed AR, Badange RK, Reballi V, Bandyala TR, Saraf SK, Bojja K, Manchineella S, Achanta PK, Kandukuri KK, Subramanian R, Benade V, Palacharla RC, Jayarajan P, Pandey S, Jasti V (2019) Discovery and development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A novel, potent, selective, and orally active histamine H3 receptor inverse agonist with robust wake-promoting activity. J Med Chem 62(3):1203-1217. doi: 10.1021/acs.jmedchem.8b01280
Objective: To discover and develop a therapeutic for human sleep disorders.
Summary: Histamine H3 Receptor Inverse Agonist demonstrated high receptor occupancy and marked wake promoting effects with decreased REM sleep in Orexin-B-SAP lesioned rats. This study supports its potential therapeutic utility in treating human sleep disorders.
Usage: Injections (490 ng/0.8 μl) were made bilaterally to the lateral hypothalamus.
Related Products: Orexin-B-SAP (Cat. #IT-20)
Selective hematopoietic stem cell ablation using CD117-antibody-drug-conjugates enables safe and effective transplantation with immunity preservation.
Czechowicz A, Palchaudhuri R, Scheck A, Hu Y, Hoggatt J, Saez B, Pang WW, Mansour MK, Tate TA, Chan YY, Walck E, Wernig G, Shizuru JA, Winau F, Scadden DT, Rossi DJ (2019) Selective hematopoietic stem cell ablation using CD117-antibody-drug-conjugates enables safe and effective transplantation with immunity preservation. Nat Commun 10:617. doi: 10.1038/s41467-018-08201-x
Objective: To investigate a safe and effective method for hematopoietic stem cell transplantation.
Summary: CD117-ADC selectively targets hematopoietic stem cells yet does not cause clinically significant side-effects.
Usage: The CD117-ADC was prepared by combining biotinylated anti-CD117 (clone 2B8) with Streptavidin–ZAP. A dose of 1.5 mg/kg of CD117-ADC (~12 µg Streptavidin-ZAP) optimally resulted in depletion of >99% of immunophenotypic and functional HSCs.
Related Products: Streptavidin-ZAP (Cat. #IT-27), Anti-CD117-SAP (Cat. #IT-83)
Hematopoietic chimerism and donor-specific skin allograft tolerance after non-genotoxic CD117 antibody-drug-conjugate conditioning in MHC-mismatched allotransplantation.
Li Z, Czechowicz A, Scheck A, Rossi DJ, Murphy PM (2019) Hematopoietic chimerism and donor-specific skin allograft tolerance after non-genotoxic CD117 antibody-drug-conjugate conditioning in MHC-mismatched allotransplantation. Nat Commun 10:616. doi: 10.1038/s41467-018-08202-w
Objective: To develop a conditioning protocol for fully MHC-mismatched bone marrow allotransplantation in mice involving transient immunosuppression and selective depletion of recipient hematopoietic stem cells.
Summary: CD117-ADC conditioning promotes skin allograft tolerance.
Usage: Biotinylated monoclonal antibodies directed against mouse CD117 were coupled to Streptavidin-ZAP. Each mouse was injected with 1.5 mg/kg of ADC in a total volume of 300 mcl PBS.
Related Products: Streptavidin-ZAP (Cat. #IT-27)
Basal forebrain chemogenetic inhibition disrupts the superior complex movement control of goal-tracking rats.
Kucinski A, Kim Y, Sarter M (2019) Basal forebrain chemogenetic inhibition disrupts the superior complex movement control of goal-tracking rats. Behav Neurosci 133:121-134. doi: 10.1037/bne0000290
Usage: Basal forebrain cholinergic neurons situated in the nucleus basalis and substantia innominata were targeted with 192-IgG-SAP in aCSF infused bilaterally (200 ng/μL; 0.8 μL/hemisphere).
Related Products: 192-IgG-SAP (Cat. #IT-01)
Ablation of brainstem C1 neurons improves cardiac function in volume overload heart failure.
Andrade DC, Toledo C, Díaz HS, Lucero C, Arce-Álvarez A, Oliveira LM, Takakura AC, Moreira TS, Schultz HD, Marcus NJ, Alcayaga J, Del Rio R (2019) Ablation of brainstem C1 neurons improves cardiac function in volume overload heart failure. Clin Sci (Lond) 133(3):393-405. doi: 10.1042/CS20180589
Objective: To determine the role played by RVLM-C1 neurons in cardiac autonomic imbalance, arrhythmogenesis and cardiac dysfunction in volume overload-induced heart failure.
Summary: RVLM-C1 neurons were selectively ablated using Anti-DBH-SAP and measures of cardiacautonomictone, function, and arrhythmia incidence were evaluated. Cardiac autonomic imbalance, arrhythmogenesis and cardiac dysfunction were present in HF rats and improved after Anti-DBH-SAP treatment.
Usage: 7.5ng/100nl of sterile saline solution was injected bilaterally into the RVLM.
Related Products: Anti-DBH-SAP (Cat. #IT-03)
Ro41-5253, a selective antagonist of retinoic acid receptor α, ameliorates chronic unpredictable mild stress-induced depressive-like behaviors in rats: Involvement of regulating HPA axis and improving hippocampal neuronal deficits.
Ke Q, Li R, Cai L, Wu SD, Li CM (2019) Ro41-5253, a selective antagonist of retinoic acid receptor α, ameliorates chronic unpredictable mild stress-induced depressive-like behaviors in rats: Involvement of regulating HPA axis and improving hippocampal neuronal deficits. Brain Res Bull 146:302-309. doi: 10.1016/j.brainresbull.2019.01.022 PMID: 30711623
Usage: histology
Related Products: Corticotropin Releasing Hormone Rabbit Polyclonal (Cat. #AB-02)
Brain-derived neurotrophic factor precursor in the hippocampus regulates both depressive and anxiety-like behaviors in rats.
Zhong F, Liu L, Wei J-L, Hu Z-L, Li L, Wang S, Xu J-M, Zhou X-F, Li C-Q, Yang Z-Y, Dai R-P (2019) Brain-derived neurotrophic factor precursor in the hippocampus regulates both depressive and anxiety-like behaviors in rats. Front Psychiatry 9:776. doi: 10.3389/fpsyt.2018.00776 PMID: 30740068
Objective: To investigate the role of proBDNF in the hippocampus in the development of depression and anxiety.
Summary: Despite some behavioral and morphological differences between depression and anxiety, hippocampal proBDNF is a common mediator to regulate these two mental disorders.
Usage: Western Blot
Related Products: NGFr (mu p75) Rabbit Polyclonal, affinity-purified (Cat. #AB-N01AP)
Non-peptidergic nociceptive neurons are essential for mechanical inflammatory hypersensitivity in mice.
Pinto LG, Souza GR, Kusuda R, Lopes AH, Sant’Anna MB, Cunha FQ, Ferreira SH, Cunha TM (2019) Non-peptidergic nociceptive neurons are essential for mechanical inflammatory hypersensitivity in mice. Mol Neurobiol 56(8):5715-5728. doi: 10.1007/s12035-019-1494-5
Objective: To determine the role of non-peptidergic nociceptors in mediating mechanical inflammatory hypersensitivity in mice.
Summary: rIB4-SAP oblates non-peptidergic neurons as displayed by the decrease of purinoceptor 3. The depletion of these neurons inhibited the mechanical inflammatory sensitivity induced by GDMF and carrageenan, but not by other expected factors such as nerve growth factor implying the role of this subset of neurons to be one of mediation as opposed to direct nociception.
Usage: IB4-SAP (0.16–3.2 μg/5 μl, i.t.), unconjugated Saporin (as control, 1.8 μg/5 μl, i.t.), or saline (vehicle, 5 μl/i.t.) were injected into the subarachnoid space on the midline between the L5 and L6 vertebrae.
Related Products: IB4-SAP (Cat. #IT-10), Saporin (Cat. #PR-01)
Targeting the niche: Depleting haemopoietic stem cells with targeted therapy.
Abadir E, Bryant C, Larsen S, Clark GJ (2019) Targeting the niche: Depleting haemopoietic stem cells with targeted therapy. Bone Marrow Transplant 54:961–968. doi: 10.1038/s41409-019-0445-0
Summary: Anti-mouse CD45 ADC (clone 104-Saporin) Depletes mature lymphoid cells and HSPC, conditioning allows for high level sustained multilineage engraftment of congenic mice. Anti-mouse ADC (CD117-saporin) Combined with T cell depleting agents allowed for significant and durable engraftment in an immunocompetent mouse allo-HSCT model.
Related Products: Streptavidin-ZAP (Cat. #IT-27), Anti-CD45.2-SAP (Cat. #IT-91)
Infrared fluorescence imaging of infarcted hearts with Ag2S nanodots.
Ortgies DH, García-Villalón ÁL, Granado M, Amor S, Rodríguez EM, Santos HDA, Yao J, Rubio-Retama J, Jaque D (2019) Infrared fluorescence imaging of infarcted hearts with Ag2S nanodots. Nano Res 12:749–757. doi: 10.1007/s12274-019-2280-4 PMID: 0
Objective: To investigate the potential application of functionalized Ag2S nanodots for accurate imaging of damaged myocardium tissues after a myocardial infarction induced by either partial or global ischemia.
Summary: NIR-II images generated by ATII-functionalized Ag2S nanodots contain valuable information about the location and extension of damaged tissue in the myocardium allowing for a proper identification of the occluded artery as well as an indirect evaluation of the damage level.
Usage: Assessment of AT1R protein content in ischemic and non-ischemic hearts by Western blot (1:1000).
Related Products: Angiotensin II receptor (AT-1R) Rabbit Polyclonal, affinity-purified (Cat. #AB-N27AP)