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Characterization of the human cysteinyl leukotriene CysLT1 receptor
The molecular and pharmacological characterization of the cloned human CysLT1 receptor is reported and the functional activation (calcium mobilization) of this receptor is described by LTD4 and LTC4, and competition for radiolabelled LTD4 binding to this receptor by the cysteinyl leukotrienes and three structurally distinct classes of Cys LT1-receptor antagonists.
Characterization of the Human Cysteinyl Leukotriene 2 Receptor*
- C. Heise, B. O'dowd, Jilly F. Evans
- Biology, MedicineThe Journal of Biological Chemistry
- 29 September 2000
The cloning and characterization of the second cysteinyl leukotriene receptor, CysLT2, a 346-amino acid protein with 38% amino acid identity to the Cys LT1 receptor is described and demonstrated high affinity binding and a rank order of potency for competition of LTC4 = LTD4 ≫ LTE4.
Identification of receptors for neuromedin U and its role in feeding
It is shown that the previously described orphan G-protein-coupled receptor FM-3 and a newly discovered one (FM-4) are cognate receptors for NMU, which provides a molecular basis for the biochemical activities of NMU and may indicate that NMU is involved in the central control of feeding.
A Novel Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Has in Vivo Activity and Antipsychotic-Like Effects in Rat Behavioral Models
It is demonstrated that positive allosteric modulation of mGluR5 produces behavioral effects, suggesting that such modulation serves as a viable approach to increasing mGLUR5 activity in vivo.
Identification and Characterization of Novel Mammalian Neuropeptide FF-like Peptides That Attenuate Morphine-induced Antinociception*
The results indicate that the endogenous ligands for FF1 and FF2 are NPVF- and NPFF-derived peptides, respectively, and suggest that theNPVF/FF1 system may be an important part of endogenous anti-opioid mechanism.
Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment
- M. Marino, David Williams, P. Conn
- BiologyProceedings of the National Academy of Sciences…
- 30 October 2003
Evidence for in vivo behavioral effects of an allosteric potentiator of mGluRs is reported and it is suggested that potentiation ofmGluR4 may be a useful therapeutic approach to the treatment of PD.
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.
Evidence that allosteric sites on GPCRs can respond to closely related ligands with a range of pharmacological activities from positive to negative modulation as well as to neutral competition of this modulation is provided.
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Compound 8q demonstrated in vivo proof of concept in an animal behavior model where known antipsychotics are active, supporting the development of new antipsychotic based on the NMDA hypofunction model for schizophrenia.
A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain
- J. O'brien, Wei Lemaire, David Williams
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 May 2004
It is found that allosteric potentiation of mGluR5 increases the effect of threshold agonist concentrations in native systems and potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself.
Pharmacological Properties of MK-3207, a Potent and Orally Active Calcitonin Gene-Related Peptide Receptor Antagonist
In vitro autoradiography studies on rhesus monkey brain slices identified the highest level of binding in the cerebellum, brainstem, and meninges, and the in vivo cerebrospinal fluid/plasma ratio was determined to be 2 to 3% in cisterna magna-ported rhesUS monkeys.