Related Experiment Video
Updated: Jun 21, 2026

06:00
Assessment of Spatial Lingual Tactile Sensitivity using a Gratings Orientation Test
Published on: September 17, 2021
Interrogating 7TM receptors: does texture in the question yield greater texture in the answer?
1GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina 27709, USA. Terry.P.Kenakin@gsk.com
Journal of Receptor and Signal Transduction Research
|July 8, 2009
Summary
Pharmacological assays are crucial for drug discovery at seven transmembrane (7TM) receptors. Modern label-free live-cell assays offer superior ligand detection and efficacy characterization compared to older methods.
Area of Science:
- Pharmacology
- Biochemistry
- Drug Discovery
Background:
- Traditional drug discovery relied on animal tissue testing.
- High-throughput screening advanced molecule testing but was limited to radioligand interactions.
- Early functional assays focused on specific signaling pathways like cyclic AMP and calcium.
Purpose of the Study:
- To highlight the evolution of pharmacological assays for seven transmembrane (7TM) receptors.
- To discuss the advantages of modern label-free live-cell assays.
- To explore harnessing functional selectivity for therapeutic benefit.
Main Methods:
- Review of historical pharmacological assay techniques.
- Comparison of radioligand binding assays with functional assays.
- Emphasis on advancements in label-free live-cell assay technology.
Main Results:
- Label-free assays in live cells enable detection of more ligands.
- These assays provide a more comprehensive characterization of drug efficacy.
- Functional selectivity offers a pathway for therapeutic advantage.
Conclusions:
- Pharmacological assays are essential for understanding drug effects on 7TM receptors.
- Label-free live-cell assays represent a significant advancement in drug discovery.
- Exploiting functional selectivity holds promise for developing targeted therapeutics.
Related Concept Videos
Shape and Texture of Coarse Aggregate
Aggregate shape is classified based on the relative sharpness or roundness of the edges and corners. This classification includes categories like rounded, angular, elongated, and flaky, each with specific characteristics. Rounded aggregates, fully shaped by attrition, are typical of river or seashore gravel, while angular aggregates, such as crushed rock, have well-defined edges. Aggregates that are elongated and flaky are less desirable, as they can reduce the workability and strength of...
Somatosensation
The somatosensory system relays sensory information from the skin, mucous membranes, limbs, and joints. Somatosensation is more familiarly known as the sense of touch. A typical somatosensory pathway includes three types of long neurons: primary, secondary, and tertiary. Primary neurons have cell bodies located near the spinal cord in groups of neurons called dorsal root ganglia. The sensory neurons of ganglia innervate designated areas of skin called dermatomes.
Gustation
Gustation is a chemical sense that, along with olfaction (smell), contributes to our perception of taste. It starts with the activation of receptors by chemical compounds (tastants) dissolved in the saliva. The saliva and filiform papillae on the tongue distribute the tastants and increase their exposure to the taste receptors.
Sensory Functions of the Skin
The skin is the largest organ of the human body and plays a crucial role in our sensory perception. It contains a vast network of sensory receptors that contribute to the skin's protective function by perceiving physical, biological, and environmental cues and generating relevant responses.
There are two main categories of receptors on the skin: capsulated and non-capsulated. The non-capsulated ones are mainly the pain receptors. The capsulated ones can be further categorized based on the...
There are two main categories of receptors on the skin: capsulated and non-capsulated. The non-capsulated ones are mainly the pain receptors. The capsulated ones can be further categorized based on the...
The Physiology of Taste
The perception of a salty flavor is facilitated by sodium ions within the oral salivary fluid. Upon consumption of a salty substance, salt crystals disassemble, leading to the liberation of its constituents—Na+ and Cl- ions. These ions subsequently dissolve into the salivary fluid present in the oral cavity. The external environment of the gustatory cells experiences an elevation in Na+ concentration, thereby establishing a potent concentration gradient. This gradient propels the diffusion of...
