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Overview

Tags

Nervous System Diseases

Endocrinology and Metabolic Disease

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Endocrinology and Metabolic Disease	1
Nervous System Diseases	1

Top 5 Drug Type	Count

Small molecule drug	2

Top 5 Target	Count

GABAA receptor(Gamma-aminobutyric acid A receptor)	1
α-glucosidase(Acidic alpha-glucosidase)	1

AbstractThe dielectric response of four batches of lactose has been measured over a frequency range of 104 to 10−2 Hz. The spectra corresponding to three of the batches were identical, while the fourth showed a marked reduction in response. This particular batch has also been reported to exhibit longer disintegration times than the other three when formulated as a tablet. The potential use of dielectric spectroscopy as a means of screening batches of pharmaceutical materials is discussed.

01 Feb 1991·European Journal of Pharmacology: Molecular PharmacologyQ3 · MEDICINE

[3H]5,7-Dichlorokynurenic acid, a novel radioligand labels NMDA receptor-associated glycine binding sites

Q3 · MEDICINE

Article

Author: Harrison, Boyd L. ; Hurt, Stephen D. ; Slone, Amy L. ; Palfreyman, Michael G. ; Siegel, Barry W. ; Baron, Bruce M.

A strychnine-insensitive glycine binding site is located on the N-methyl-D-aspartate (NMDA)-preferring glutamate receptor complex. Kynurenic acid analogs are antagonists at this binding site. A derivative of kynurenic acid, 5,7-dichlorokynurenic acid (5,7-DCKA) was radiolabeled with 3H and used to study antagonist binding to the glycine recognition site. This ligand ( [3H]5,7-DCKA) showed high affinity (Kd = 69 nM), saturable (Bmax = 14.5 pmol/mg protein) binding to rat brain membranes. A variety of agonists and antagonists inhibited the binding of [3H]5,7-DCKA and [3H]glycine in a similar fashion (r = 0.93). In addition, glutamate site agonists and antagonists exerted opposite allosteric effects on [3H]5,7-DCKA binding suggesting that [3H]5,7-DCKA preferentially binds to the agonist-activated conformation of the receptor.

01 Jan 1991·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

The role of the disulphide bonds in endothelin-1

Q3 · MEDICINE

Article

Author: Miller, Robert C ; Pelton, John T

AbstractThe smooth muscle contracting peptide endothelin-1 is characterized by the presence of two disulphide bonds and their importance for maintaining the agonist activity of the peptide was examined by synthesizing analogues of endothelin-1 lacking one or the other, or both, of these bonds. The circular dichroic spectra of these analogues (in which alanine residues replaced the appropriate cystines), [Ala1,15]-, [Ala3,11]- and [Ala1,3,11,15]-endothelin-l had features in common with that of endothelin-1. All three analogues exhibited at least some agonist activity in guinea-pig isolated trachea, but surprisingly endothelin-1 was a partial agonist in comparison with the analogue [Ala3,11]endothelin-1. The disulphide bonds are therefore not absolutely essential for maintaining the tertiary structure necessary for agonist activity at endothelin-1 receptors in all tissues.

100 Deals associated with Merrell Dow Research Institutes

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100 Translational Medicine associated with Merrell Dow Research Institutes

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Pipeline

Pipeline Snapshot as of 23 Jan 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Preclinical

2

1

Other

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Suritozole ( GABAA receptor )	Depressive Disorder More	Preclinical
Camiglibose ( α-glucosidase )	Diabetes Mellitus More	Preclinical
MDL-28050	Thrombosis More	Discontinued