α2A- and α2C-Adrenoceptors as Potential Targets for Dopamine and Dopamine Receptor Ligands
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Neurobiology"
DOI: 10.1007/s12035-018-1004-1
Abstract: The poor norepinephrine innervation and high density of Gi/o-coupled α2A- and α2C-adrenoceptors in the striatum and the dense striatal dopamine innervation have prompted the possibility that dopamine could be an effective adrenoceptor ligand. Nevertheless, the… read more here.
Keywords: adrenoceptors potential; potential targets; dopamine receptor; receptor ligands ... See more keywords
An insight into the multifunctional role of ghrelin and structure activity relationship studies of ghrelin receptor ligands with clinical trials.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114308
Abstract: Ghrelin is a multifunctional gastrointestinal acylated peptide, primarily synthesized in the stomach and regulates the secretion of growth hormone and energy homeostasis. It plays a central role in modulating the diverse biological, physiological and pathological… read more here.
Keywords: ghrelin receptor; receptor ligands; ghrelin structure; ligands clinical ... See more keywords
Influence of the CB1 and CB2 cannabinoid receptor ligands on the activity of atypical antidepressant drugs in the behavioural tests in mice
Sign Up to like & getrecommendations! Published in 2020 at "Pharmacology Biochemistry and Behavior"
DOI: 10.1016/j.pbb.2019.172833
Abstract: Available data support the notion that cannabinoids, whose therapeutic value is limited due to severe adverse reactions, could be beneficial as adjunctive agents in the management of mood disorders. Polytherapy, which is superior to monotherapy… read more here.
Keywords: antidepressant; cannabinoid receptor; receptor ligands; receptor ... See more keywords
Exposure to Cannabinoid Receptor 1 ligands induces miswiring of GnRH axons in the brain of zebrafish embryos
Sign Up to like & getrecommendations! Published in 2017 at "Reproductive Toxicology"
DOI: 10.1016/j.reprotox.2017.06.144
Abstract: Importantly, GABAA receptors act differently during development compared to adulthood; the early exposure leads to excitation rather than inhibition of GABAA receptors. This excitation, together with NMDA receptor activation, may potentially trigger excess apoptosis affecting… read more here.
Keywords: exposure; exposure cannabinoid; cannabinoid receptor; receptor ligands ... See more keywords
Synthesis, Characterization, and Application of Muscarinergic M3 Receptor Ligands Linked to Fluorescent Dyes.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01376
Abstract: Through the linkage of two muscarinergic M3 receptor ligands to fluorescent tetramethylrhodamine- and cyanine-5-type dyes, two novel tool compounds, OFH5503 and OFH611, have been developed. Based on the suitable binding properties and kinetics related to… read more here.
Keywords: characterization application; muscarinergic receptor; application muscarinergic; receptor ligands ... See more keywords
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01584
Abstract: Methoxycarbonyl-1-phenyl-2-cyclopropylmethyl based derivatives cis-(+)-1a [cis-(+)-MR200], cis-(-)-1a [cis-(-)-MR201], and trans-(±)-1a [trans-(±)-MR204], have been identified as new potent sigma (σ) receptor ligands. In the present paper, novel enantiomerically pure analogues were synthesized and optimized for their σ… read more here.
Keywords: methyl; receptor ligands; sigma receptor; receptor ... See more keywords
Tetrahydroquinoline Ring as a Versatile Bioisostere of Tetralin for Melatonin Receptor Ligands.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00359
Abstract: A new family of melatonin receptor ligands, characterized by a tetrahydroquinoline (THQ) scaffold carrying an amide chain in position 3, was devised as conformationally constrained analogs of flexible N-anilinoethylamides previously developed. Molecular superposition models allowed… read more here.
Keywords: tetrahydroquinoline ring; ring versatile; receptor ligands; receptor ... See more keywords
Zebrafish behavioural profiling identifies GABA and serotonin receptor ligands related to sedation and paradoxical excitation
Sign Up to like & getrecommendations! Published in 2019 at "Nature Communications"
DOI: 10.1038/s41467-019-11936-w
Abstract: Anesthetics are generally associated with sedation, but some anesthetics can also increase brain and motor activity—a phenomenon known as paradoxical excitation. Previous studies have identified GABAA receptors as the primary targets of most anesthetic drugs,… read more here.
Keywords: paradoxical excitation; sedation; receptor ligands; serotonin receptor ... See more keywords
Identification of Histamine H3 Receptor Ligands Using a New Crystal Structure Fragment-based Method
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-05058-w
Abstract: Virtual screening offers an efficient alternative to high-throughput screening in the identification of pharmacological tools and lead compounds. Virtual screening is typically based on the matching of target structures or ligand pharmacophores to commercial or… read more here.
Keywords: receptor; receptor ligands; histamine receptor; identification histamine ... See more keywords
Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 1: 4-acylamino derivatives.
Sign Up to like & getrecommendations! Published in 2017 at "MedChemComm"
DOI: 10.1039/c7md00077d
Abstract: The synthesis of a new series of 4-acylaminopyrazolo[3,4-d]pyrimidines active on the sigma-1 receptor (σ1R) is reported. Compounds were efficiently prepared using a two to three step process starting from commercially available 1H-pyrazolo[3,4-d]pyrimidin-4-amine. A SAR study… read more here.
Keywords: pyrimidines sigma; pyrazolo pyrimidines; ligands treatment; treatment pain ... See more keywords
5-HT1A receptor ligands and their therapeutic applications: review of new patents
Sign Up to like & getrecommendations! Published in 2018 at "Expert Opinion on Therapeutic Patents"
DOI: 10.1080/13543776.2018.1514011
Abstract: ABSTRACT Introduction: 5-HT1AR was one of the first discovered serotonin receptors and is one of the most thoroughly studied. Dysfunctions associated with 5-HT1AR neurotransmission are linked to several psychiatric disorders, including anxiety, depression, and movement… read more here.
Keywords: applications review; ligands therapeutic; ht1a receptor; therapeutic applications ... See more keywords