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Neuromedin U Family Related Drug Discovery Products

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The neuromedin U (NmU) refers to a new multifunctional neuropeptide that was initially isolated from pig spinal cord and has a potent uterine contraction-inducing activity. It is a gut and brain peptide that is highly conserved across a variety of animals, from mammals to amphibians. At NmU receptors, it is regarded as an endogenous agonist. The first biological activity connected to NmU was the contraction of the uterine smooth muscle, however it has now been found that it also has a variety of peripheral and central activities.

Creative Biolabs can offer neuromedin U family related tools to contribute to the success of drug discovery and development:

Overview of Neuromedin U Family

NmU receptors come in two different varieties: NMUR1 and NMUR2. The location of human NmU receptors has been the subject of numerous investigations, although a precise picture has not yet materialized. According to several methods used to analyze the pattern of receptor expression, human NMUR1 is predominately expressed in the peripheral, particularly the GIT, while human NMUR2 is predominately expressed in the central nervous system (CNS). The predicted molecular mass of the NMUR1 is 44,979 Da and it has 403 amino acids. The predicted molecular mass of the NMUR2 is 47,450 Da and it has 412 amino acids. The two receptors share 45 to 50% of their amino acid sequences, and they both share about 30% identity with the human growth hormone secretagogue receptor, the human motilin receptor, and the human neurotensin receptor. When NMUR1 or NMUR2 are both activated, G𝜶q/11 and G𝜶i are also activated but not G𝜶s, which leads to an increase in intracellular Ca2+ and an inhibition of forskolin-stimulated cAMP synthesis, respectively. Arachidonic acid can also be released by receptor activation, most likely via Ca2+-dependent phospholipase A2 activation.

Schematic representation of human NMUR1 and NMUR2. Fig.1 Schematic representation of human NMUR1 and NMUR2. (Brighton, 2004)

Neuromedin U Family Drug Discovery

The broad distribution of NmU and its receptors throughout the body and the conservation of NmU structural components across species suggest that these molecules play a basic role in important physiological processes. According to current research, NmU may play a function in controlling blood flow, blood pressure, nutrition and energy homeostasis, stress reactions, cancer, pain, the immune system, and smooth-muscle contraction in the gastrointestinal and genitourinary tracts. This might enable the development of small molecule agonists and antagonists, ideally with receptor subtype selectivity, that could help to further describe the roles of NmU and the receptor subtypes through which various effects are mediated in addition to enabling the identification of the cellular signaling pathways and cellular functions mediated by NmU.

Reference

  1. Brighton, P.J.; et al. Neuromedin U and its receptors: structure, function, and physiological roles. Pharmacological reviews. 2004, 56(2): 231-248.

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