• Publications
  • Influence
Update on melatonin receptors: IUPHAR Review 20
Melatonin receptors are seven transmembrane‐spanning proteins belonging to the GPCR superfamily. In mammals, two melatonin receptor subtypes exist ‐ MT1 and MT2 ‐ encoded by the MTNR1A and MTNR1BExpand
  • 131
  • 10
Recent Advances in Melatonin Receptor Ligands
  • D. Zlotos
  • Medicine, Chemistry
  • Archiv der Pharmazie
  • 1 June 2005
Melatonin is a hormone exerting its multiple actions mainly through two G‐protein‐coupled receptors MT1 and MT2. Exploring the physiological role of each of these subtypes requires subtype selectiveExpand
  • 95
  • 5
Discovery of Nanomolar Dengue and West Nile Virus Protease Inhibitors Containing a 4-Benzyloxyphenylglycine Residue.
The dengue virus (DENV) and West Nile Virus (WNV) NS2B-NS3 proteases are attractive targets for the development of dual-acting therapeutics against these arboviral pathogens. We present the synthesisExpand
  • 39
  • 4
Allosteric site on muscarinic acetylcholine receptors: a single amino acid in transmembrane region 7 is critical to the subtype selectivities of caracurine V derivatives and alkane-bisammonium
Diverse muscarinic allosteric ligands exhibit greatest affinity toward the M2 receptor subtype and lowest affinity toward M5. In this study, we evaluated the potencies with which two groups of highlyExpand
  • 52
  • 3
  • PDF
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
Numerous physiological functions of the pineal gland hormone melatonin are mediated via activation of two G-protein-coupled receptors, MT1 and MT2. The melatonergic drugs on the market, ramelteon andExpand
  • 123
  • 2
Bisquaternary ligands of the common allosteric site of M2 acetylcholine receptors: search for the minimum essential distances between the pharmacophoric elements.
Structurally diverse molecules, such as alcuronium, gallamine, and tubocurarine as well as W84 and WDUO, are known to interact allosterically with ligand binding to muscarinic M2 acetylcholineExpand
  • 18
  • 1
Pharmacological characterisation of strychnine and brucine analogues at glycine and alpha7 nicotinic acetylcholine receptors.
Strychnine and brucine from the plant Strychnos nux vomica have been shown to have interesting pharmacological effects on several neurotransmitter receptors, including some members of the superfamilyExpand
  • 30
  • 1
Probing the pharmacophore for allosteric ligands of muscarinic M2 receptors: SAR and QSAR studies in a series of bisquaternary salts of caracurine V and related ring systems.
Allosteric effects on muscarinic acetylcholine M(2) receptors were examined in a series of bisquaternary salts of the Strychnos alkaloid caracurine V (6) and related iso-caracurine V,Expand
  • 18
  • 1
N1-linked melatonin dimers as bivalent ligands targeting dimeric melatonin receptors
A novel series of dimeric melatonin analogues obtained by connecting two melatonin molecules through N1 with spacers of 15–24 atoms was synthesized and characterized in 2-[125-I]-iodomelatoninExpand
  • 10
  • 1
  • PDF
Muscarinic receptor agonists and antagonists
Although four different subtypes of the muscarinic acetylcholine (ACh) receptor with functional correlates are known to exist (function for M5 is still unclear), all muscarinic agonists and antagon...
  • 17