5-HT receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on [198] and subsequently revised [180]) are, with exception of ionotropic 5-HT3 class, GPCRs where endogenous agonist is 5-hydroxytryptamine. The diversity metabotropic increased alternative splicing that produces isoforms 5-HT2A (non-functional), 5-HT2C 5-HT4, 5-HT6 (non-functional) 5-HT7 receptors. Unique amongst GPCRs, RNA...

EFFECTS OF THE NITRIC OXIDE SYNTHASE INHIBITOR L-NAME ON RECOGNITION AND SPATIAL MEMORY DEFICITS PRODUCED BY DIFFERENT NMDA RECEPTOR ANTAGONIST IN THE RAT Antonios Boultadakis and Nikolaos Pitsikas* Department of Pharmacology, School of Medicine, University of Thessaly, Larissa, Greece *Correspondence to: N. Pitsikas. Department of Pharmacology, School of Medicine, University of Thessaly, Biopo...

MICROTUBULES-ASSOCIATED PROTEINS, ON KAPPA OPIOID RECEPTOR EXPRESSION Chongguang Chen, Yulin Wang, Peng Huang and Lee-Yuan Liu-Chen Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA, USA Running head: GEC1-KOPR interaction Address correspondence to: Dr. Lee-Yuan Liu-Chen, Department of Pharmacology, Temple University School of Medicine, 3420 North Broad Street, ...

Bradykinin (or kinin) receptors (nomenclature as agreed by the NC-IUPHAR subcommittee on (kinin) Receptors [92]) are activated endogenous peptides bradykinin (BK), [des-Arg9]bradykinin, Lys-BK (kallidin), [des-Arg10]kallidin, [Phospho-Ser6]-Bradykinin, T-kinin (Ile-Ser-BK), [Hyp3]bradykinin and Lys-[Hyp3]-bradykinin. Variation in pharmacology activity of B1 B2 receptor antagonists at species or...

G protein-coupled receptors (GPCRs) are historically the most successful family of drug targets. In recent times it has become clear that the pharmacology of these receptors is far more complex than previously imagined. Understanding of the pharmacological regulation of GPCRs now extends beyond simple competitive agonism or antagonism by ligands interacting with the orthosteric binding site of ...

Nuclear receptors are ligand-activated transcription factors and include the receptors for steroid hormones, lipophilic vitamins, sterols, and bile acids. These receptors serve as targets for development of myriad drugs that target a range of disorders. Classically defined ligands that bind to the ligand-binding domain of nuclear receptors, whether they are endogenous or synthetic, either activ...

Pharmacology is an integrative discipline that originated from activities, now nearly 7000 years old, to identify therapeutics from natural product sources. Research in the 19th Century that focused on the Law of Mass Action (LMA) demonstrated that compound effects were dose-/concentration-dependent eventually leading to the receptor concept, now a century old, that remains the key to understan...