5‐HT7 Receptor Antagonists with an Unprecedented Selectivity Profile
Sign Up to like & getrecommendations! Published in 2018 at "ChemMedChem"
DOI: 10.1002/cmdc.201800026
Abstract: Selective leads: In this study, we generated a new series of serotonin 5-HT7 receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT7 antagonists with unprecedented high selectivity for the… read more here.
Keywords: antagonists unprecedented; ht7 receptor; unprecedented selectivity; receptor antagonists ... See more keywords
Serotonin 5‐HT7 receptor overexpression in the raphe nuclei area produces antidepressive effect and affects brain serotonin system in male mice
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Neuroscience Research"
DOI: 10.1002/jnr.25055
Abstract: Heterodimerization between 5‐HT7 and 5‐HT1A receptors seems to play an important role in the mechanism of depression and antidepressant drug action. It was suggested that the shift of the ratio between 5‐HT1A/5‐HT7 hetero‐ and 5‐HT1A/5‐HT1A… read more here.
Keywords: ht7 receptor; ht1a; receptor; receptor overexpression ... See more keywords
Design and discovery of a high affinity, selective and β-arrestin biased 5-HT7 receptor agonist
Sign Up to like & getrecommendations! Published in 2021 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-021-02797-4
Abstract: Compound 1c, 5-chloro-2-(2-(3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-2,3-dihydro-1H-inden-1-one was previously reported from our laboratory showing high affinity binding to the 5-HT7 receptor (Ki = 0.5 nM). However, compound 1c racemizes readily upon enantiomeric separation. To prevent racemization, we have redesigned and synthesized methyl… read more here.
Keywords: ht7 receptor; high affinity; arrestin biased;
5‐HT7 receptor antagonism (SB‐269970) attenuates bleomycin‐induced pulmonary fibrosis in rats via downregulating oxidative burden and inflammatory cascades and ameliorating collagen deposition: Comparison to terguride
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2017.08.014
Abstract: ABSTRACT The neurotransmitter 5‐hydroxytryptamine (5‐HT) is involved in regulation of local tissue inflammation and repair through a set of receptors (5‐HT1‐7 receptors), which are expressed in the lung. Considering the protective importance of 5‐HT receptor… read more here.
Keywords: receptor; ht7 receptor; pulmonary fibrosis; receptor antagonist ... See more keywords
Effect of a 5-HT7 Receptor Antagonist on Reversal Learning in the Rat Attentional Set-Shifting Test.
Sign Up to like & getrecommendations! Published in 2020 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.0c00554
Abstract: 5-HT7 receptor antagonism has been shown to ameliorate ketamine-induced schizophrenia-like deficits in extradimensional set-shifting using the attentional set-shifting task (ASST). However, this rodent paradigm distinguishes between several types of cognitive rigidity associated with neuropsychiatric conditions.… read more here.
Keywords: receptor; set shifting; ht7 receptor; reversal ... See more keywords
In Vitro and In Silico Analysis of the Residence Time of Serotonin 5-HT7 Receptor Ligands with Arylpiperazine Structure: A Structure-Kinetics Relationship Study.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.1c00710
Abstract: During the last decade, the kinetics of drug-target interaction has received increasing attention as an important pharmacological parameter in the drug development process. Several studies have suggested that the lipophilicity of a molecule can play… read more here.
Keywords: ht7 receptor; structure kinetics; structure; ht7r ... See more keywords
Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of [18F]ENL30: A Potential PET Radiotracer for the 5-HT7 Receptor
Sign Up to like & getrecommendations! Published in 2019 at "ACS Omega"
DOI: 10.1021/acsomega.9b00394
Abstract: The 5-HT7 receptor (5-HT7R) is involved in a broad range of physiological conditions and disorders. Currently, there is no validated clinical positron emission tomography (PET) tracer available; however, we have recently developed a promising 11C-labeled… read more here.
Keywords: evaluation; pet; 18f enl30; ht7 receptor ... See more keywords
The 5-HT7 receptor antagonist SB-269970 alleviates seizure activity and downregulates hippocampal c-Fos expression in pentylenetetrazole-induced kindled rats
Sign Up to like & getrecommendations! Published in 2022 at "Neurological Research"
DOI: 10.1080/01616412.2022.2064700
Abstract: ABSTRACT Objectives Recently, studies have demonstrated that serotonin type 7 receptors (5-HT7) have conflincting effects on neuronal excitability in different brain regions. However, the effect of 5-HT7 on seizures has not been exactly elucidated yet.… read more here.
Keywords: ptz; antagonist 269970; seizure; ht7 receptor ... See more keywords
Is the 5-hydroxytryptamine 7 Receptor Constitutively Active in the Vasculature? A Study in Veins/Vein
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Cardiovascular Pharmacology"
DOI: 10.1097/fjc.0000000000001296
Abstract: Abstract: The 5-hydroxytryptamine 7 (5-HT7) receptor is reported to have considerable constitutive activity when transfected into cells. Constitutive activity—receptor activity in the absence of known agonist—is important for understanding the contributions of a receptor to… read more here.
Keywords: ht7 receptor; constitutive activity; contraction; vena cava ... See more keywords
Electroacupuncture exerts an anti-migraine effect via modulation of the 5-HT7 receptor in the conscious rat
Sign Up to like & getrecommendations! Published in 2019 at "Acupuncture in Medicine"
DOI: 10.1136/acupmed-2017-011410
Abstract: Background: Acupuncture has been recommended as an alternative therapy for migraine. Emerging evidence suggests that the 5-HT7 receptor (5-HT7R) plays a significant facilitatory role in descending modulation in migraine pathophysiology, and that activation of 5-HT7R… read more here.
Keywords: modulation; ht7 receptor; migraine; via modulation ... See more keywords
T Lymphocyte Serotonin 5-HT7 Receptor Is Dysregulated in Natalizumab-Treated Multiple Sclerosis Patients
Sign Up to like & getrecommendations! Published in 2022 at "Biomedicines"
DOI: 10.3390/biomedicines10102418
Abstract: Serotonin (5-HT) is known as a potent immune cell modulator in autoimmune diseases and should be protective in the pathogenesis of multiple sclerosis (MS). Nevertheless, there is limited knowledge about receptors involved in 5-HT effects… read more here.
Keywords: natalizumab treated; ht7 receptor; multiple sclerosis; ht7 ... See more keywords