Molecular Pharmacology of Neurotransmitter Receptors

Understanding neurotransmitter receptors: molecular biology-based strategies.

Neurotransmitter receptor proteins can be divided into GPCRs and ligand-gated ion channels. Members within each family utilize a similar signalling mechanism and are structurally related. Multiple receptor subtypes are expressed for individual neurotransmitters, generating orders of complexity that have been exploited for therapeutic intervention. GPCRs have been cloned and extensively studied ...

Vesicular neurotransmitter transporters: Pharmacology, Biochemistry and Molecular Analysis

Molecular Pharmacology of the Incretin Receptors

The incretin hormones glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) are important regulators of insulin and glucagon secretion as well as lipid metabolism and appetite. These biological functions make their respective receptors (GIPR and GLP-1R) attractive targets in the treatment of both type 2 diabetes mellitus (T2DM) and obesity. The use of these nati...

Molecular Pharmacology of δ-Opioid Receptors.

Opioids are among the most effective analgesics available and are the first choice in the treatment of acute severe pain. However, partial efficacy, a tendency to produce tolerance, and a host of ill-tolerated side effects make clinically available opioids less effective in the management of chronic pain syndromes. Given that most therapeutic opioids produce their actions via µ-opioid receptors...

Alternative Radioligands for Investigating the Molecular Pharmacology of Melatonin Receptors.

Melatonin exerts a variety of physiologic activities that are mainly relayed through the melatonin receptors MT1 and MT2 Low expressions of these receptors in tissues have led to widespread experimental use of the agonist 2-[(125)I]-iodomelatonin as a substitute for melatonin. We describe three iodinated ligands: 2-(2-[(2-iodo-4,5-dimethoxyphenyl)methyl]-4,5-dimethoxy phenyl) (DIV880) and (2-io...