VUF-8430

Last updated
VUF-8430
VUF-8430 structure.png
Names
Preferred IUPAC name
2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester[ citation needed ]
Identifiers
3D model (JSmol)
AbbreviationsVUF-8430
ChEMBL
ChemSpider
PubChem CID
UNII
  • InChI=1S/C4H11N5S/c5-3(6)9-1-2-10-4(7)8/h1-2H2,(H3,7,8)(H4,5,6,9) Yes check.svgY
    Key: GSYGTVNTZHFQQH-UHFFFAOYSA-N Yes check.svgY
  • NC(=N)NCCSC(N)=N
Properties
C4H11N5S
Molar mass 161.23 g·mol−1
log P -1.367
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
X mark.svgN  verify  (what is  Yes check.svgYX mark.svgN ?)

VUF-8430 is a histamine agonist [1] selective for the H4 subtype. [2]

Related Research Articles

Histamine H<sub>3</sub> receptor Mammalian protein found in Homo sapiens

Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act as autoreceptors in presynaptic histaminergic neurons and control histamine turnover by feedback inhibition of histamine synthesis and release. The H3 receptor has also been shown to presynaptically inhibit the release of a number of other neurotransmitters (i.e. it acts as an inhibitory heteroreceptor) including, but probably not limited to dopamine, GABA, acetylcholine, noradrenaline, histamine and serotonin.

Histamine H<sub>4</sub> receptor Mammalian protein found in Homo sapiens

The histamine H4 receptor, like the other three histamine receptors, is a member of the G protein-coupled receptor superfamily that in humans is encoded by the HRH4 gene.

Histamine H<sub>1</sub> receptor Histamine receptor

The H1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is activated by the biogenic amine histamine. It is expressed in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. The H1 receptor is linked to an intracellular G-protein (Gq) that activates phospholipase C and the inositol triphosphate (IP3) signalling pathway. Antihistamines, which act on this receptor, are used as anti-allergy drugs. The crystal structure of the receptor has been determined (shown on the right/below) and used to discover new histamine H1 receptor ligands in structure-based virtual screening studies.

Histamine H<sub>2</sub> receptor Mammalian protein found in Homo sapiens

H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of protein kinase A. PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine H2 receptor agonist.

Lisuride Chemical compound

Lisuride, sold under the brand name Dopergin among others, is a monoaminergic medication of the ergoline class which is used in the treatment of Parkinson's disease, migraine, and high prolactin levels. It is taken by mouth.

ABT-239 Chemical compound

ABT-239 is an H3-receptor inverse agonist developed by Abbott. It has stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia. ABT-239 is more active at the human H3 receptor than comparable agents such as thioperamide, ciproxifan, and cipralisant. It was ultimately dropped from human trials after showing the dangerous cardiac side effect of QT prolongation, but is still widely used in animal research into H3 antagonists / inverse agonists.

Impromidine

Impromidine (INN) is a highly potent and specific histamine H2 receptor agonist.

Ciproxifan

Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.

Antihistamine Drug that blocks histamine or histamine agonists

Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic drug that can be bought without a prescription and provides relief from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use.

An H3 receptor antagonist is a classification of drugs used to block the action of histamine at the H3 receptor.

A-349821

A-349,821 is a potent and selective histamine H3 receptor antagonist (or possibly an inverse agonist). It has nootropic effects in animal studies, although there do not appear to be any plans for clinical development at present and it is currently only used in laboratory research.

4-Methylhistamine Chemical compound

4-Methylhistamine is a histamine agonist selective for the H4 subtype.

VUF-5681 Chemical compound

VUF-5681 is a potent and selective histamine antagonist which binds selectively to the H3 subtype. However while VUF-5681 blocks the activity of more potent H3 agonists, recent studies suggest that it may have some weak partial agonist activity when administered by itself.

VUF-6002

VUF-6002 (JNJ-10191584) is a drug which acts as a potent and selective antagonist at the histamine H4 receptor. It has anti-inflammatory and analgesic effects in animal studies of inflammatory diseases.

Amthamine Chemical compound

Amthamine is a histamine agonist selective for the H2 subtype. It has been used in vitro and in vivo to study gastric secretion, as well as other functions of the H2 receptor.

Proxyfan Chemical compound

Proxyfan is a histamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from full agonist, to antagonist, to inverse agonist in different tissues, depending on the level of constitutive activity of the histamine H3 receptor. This gives it a complex activity profile in vivo which has proven useful for scientific research.

Immethridine Chemical compound

Immethridine is a histamine agonist selective for the H3 subtype.

UR-AK49 is a drug used in scientific research which acts as a potent antagonist for the Neuropeptide Y / Pancreatic polypeptide receptor Y4, and also as a partial agonist at the histamine receptors H1 and H2. UR-AK49 is a pure antagonist at Y4 with no partial agonist effects, and although it is only slightly selective for Y4 over the related Y1 and Y5 receptors, as the first non-peptide Y4 antagonist developed UR-AK49 is expected to be useful in the study of this receptor and its role in the body.

Clorotepine Chemical compound

Clorotepine, also known as octoclothepin or octoclothepine, is an antipsychotic of the tricyclic group which was derived from perathiepin in 1965 and marketed in the Czech Republic by Spofa in or around 1971 for the treatment of schizophrenic psychosis.

OUP-16 Chemical compound

OUP-16 is a histamine agonist selective for the H4 subtype.

References

  1. ↑ Smith FM, Haskelberg H, Tracey DJ, Moalem-Taylor G (2007). "Role of histamine H3 and H4 receptors in mechanical hyperalgesia following peripheral nerve injury". Neuroimmunomodulation. 14 (6): 317–25. doi:10.1159/000125048. PMID   18401194. S2CID   23020760.
  2. ↑ Lim, HD; Smits, RA; Bakker, RA; Van Dam, CM; De Esch, IJ; Leurs, R (2006). "Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist". Journal of Medicinal Chemistry. 49 (23): 6650–1. doi:10.1021/jm060880d. PMID   17154494.


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