PROCEEDINGS OF THE British Pharmacological Society 10th‐12th September, 1980

doi:10.1111/j.1476-5381.1981.tb11001.x

British J Pharmacology

1981

DOI: 10.1111/j.1476-5381.1981.tb11001.x

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PROCEEDINGS OF THE British Pharmacological Society 10th‐12th September, 1980

Abstract: * Imipramine was added to the homogenate otherwise the animals were identical to the control group. ** Uptake is expressed per 10 mg cortical protein. References COPPEN, A., RAMA RAO, V.A.. SWADE, C. & WOOD, K. (1979). Inhibition of 5-hydroxytryptamine reuptake by amitriptyline and zimelidine and its relationship to their therapeutic action. Psychopharmacology, 63, 125-129. DICKISON, S.E., DIGGORY, G.L., WOOD, M.D. & WYLLIE, M.G. (1980). The effects of a selective uptake blocker on 5-HT turnover in the CNS. Br… Show more

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Cited by 3 publications

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[³H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H₂ Receptor Antagonist

et al. 2014

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A series of new piperidinomethylphenoxypropylamine-type histamine H2 receptor (H2 R) antagonists with different substituted "urea equivalents" was synthesized and characterized in functional in vitro assays. Based on these data as selection criteria, radiosynthesis of N-[6-(3,4-dioxo-2-{3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino}cyclobut-1-enylamino)hexyl]-(2,3-(3) H2 )propionic amide ([(3) H]UR-DE257) was performed. The radioligand (specific activity: 63 Ci mmol(-1) ) had high affinity for human, rat, and guinea pig H2 R (hH2 R, Sf9 cells: Kd , saturation binding: 31 nM, kinetic studies: 20 nM). UR-DE257 revealed high H2 R selectivity on membranes of Sf9 cells, expressing the respective hHx R subtype (Ki values: hH1 R: >10000 nM, hH2 R: 28 nM, hH3 R: 3800 nM, hH4 R: >10000 nM). In spite of insurmountable antagonism, probably due to rebinding of [(3) H]UR-DE257 to the H2 R (extended residence time), the title compound proved to be a valuable pharmacological tool for the determination of H2 R affinities in competition binding assays.

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[³H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H₂ Receptor Antagonist

et al. 2014

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Enantiomers of 2-methylglutamate and 2-methylglutamine selectively impact mouse brain metabolism and behavior

Wawro

Gajera

Baker

et al. 2021

Sci Rep

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Imbalance of excitatory and inhibitory neurotransmission is implicated in a wide range of psychiatric and neurologic disorders. Here we tested the hypothesis that insertion of a methyl group on the stereogenic alpha carbon of l-Glu or l-Gln would impact the γ-aminobutyric acid (GABA) shunt and the glutamate-glutamine cycle. (S)-2-methylglutamate, or (S)-2MeGlu, was efficiently transported into brain and synaptosomes where it was released by membrane depolarization in a manner equivalent to endogenous l-Glu. (R)-2MeGlu was transported less efficiently into brain and synaptosomes but was not released by membrane depolarization. Each enantiomer of 2MeGlu had limited activity across a panel of over 30 glutamate and GABA receptors. While neither enantiomer of 2MeGlu was metabolized along the GABA shunt, (S)-2MeGlu was selectively converted to (S)-2-methylglutamine, or (S)-2MeGln, which was subsequently slowly hydrolyzed back to (S)-2MeGlu in brain. rac-2MeGln was also transported into brain, with similar efficiency as (S)-2MeGlu. A battery of behavioral tests in young adult wild type mice showed safety with up to single 900 mg/kg dose of (R)-2MeGlu, (S)-2MeGlu, or rac-2MeGln, suppressed locomotor activity with single ≥ 100 mg/kg dose of (R)-2MeGlu or (S)-2MeGlu. No effect on anxiety or hippocampus-dependent learning was evident. Enantiomers of 2MeGlu and 2MeGln show promise as potential pharmacologic agents and imaging probes for cells that produce or transport l-Gln.

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Identification of adrenoceptors and dopamine receptors mediating vascular responses in the superior mesenteric arterial bed of the rat

Nichols,

Hiley

1985

Journal of Pharmacy and Pharmacology

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The nature of the adrenoceptors and dopamine receptors mediating vascular responses in the in-situ blood perfused superior mesenteric arterial bed of the rat have been studied. alpha 1-Adrenoceptor agonists produced vasoconstriction but alpha 2-agonists had no significant effect on vascular resistance. The vasoconstrictor effects of noradrenaline were antagonized by low doses of prazosin (26 nmol kg-1 i.v.). Isoprenaline and salbutamol produced vasodilation when the vasculature was preconstricted with arginine vasopressin. The responses to isoprenaline were potently antagonized by propranolol (1.69 mumol kg-1 i.v.) and weakly but significantly reduced by practolol (3.75 mumol kg-1 i.v.) whereas the responses to salbutamol were unaffected by the same dose of practolol. After preconstriction of the vasculature and alpha-adrenoceptor blockade, dopamine and apomorphine produced dilator responses with both compounds producing the same maximal response and apomorphine being 1.8 times more potent than dopamine. The dopamine responses were present after the animals had been pithed and were resistant to spiperone (506 nmol kg-1 i.v.) but were antagonized by cis-alpha-flupenthixol (460 nmol kg-1 i.v.). These results suggest that this vascular bed possesses vasoconstrictor alpha 1- but not alpha 2-adrenoceptors, vasodilator beta 1- and beta 2-adrenoceptors and vasodilator dopamine receptors which appear similar to the D1-type found centrally.

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PROCEEDINGS OF THE British Pharmacological Society 10th‐12th September, 1980

Cited by 3 publications

References 296 publications

[³H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H₂ Receptor Antagonist

[³H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H₂ Receptor Antagonist

Enantiomers of 2-methylglutamate and 2-methylglutamine selectively impact mouse brain metabolism and behavior

Identification of adrenoceptors and dopamine receptors mediating vascular responses in the superior mesenteric arterial bed of the rat

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PROCEEDINGS OF THE British Pharmacological Society 10th‐12th September, 1980

Cited by 3 publications

References 296 publications

[3H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H2 Receptor Antagonist

[3H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H2 Receptor Antagonist

Enantiomers of 2-methylglutamate and 2-methylglutamine selectively impact mouse brain metabolism and behavior

Identification of adrenoceptors and dopamine receptors mediating vascular responses in the superior mesenteric arterial bed of the rat

Contact Info

Product

Resources

About

[³H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H₂ Receptor Antagonist

[³H]UR‐DE257: Development of a Tritium‐Labeled Squaramide‐Type Selective Histamine H₂ Receptor Antagonist