Characterization and inhibition of a cholecystokinin-inactivating serine peptidase

Article Abstract:

The human tripeptidyl peptidase II (TPPII) is a neuropeptidase that inactivates cholecystokinin (CCK). TPPII is a serine peptidase with a molecular mass of 135,000 and is irreversibly labeled on sodium dodecy sulphate-polyacrylamide gel electrophoresis. TPPII is present in the brain, liver, testis, kidney and spleen. It is both cytosolic and linked to the synaptonemal membranes. The enzyme is specific for CCK-8 which it breaks up into biologically inactive parts. Blockade of TPPII by butabindide prevents the inactivation of neuronal CCK-8. CCK-responsive neurons express TPPII.

Author: Ganellin, C. Robin, Schwartz, Jean-Charles, Rose, Christiane, Vargas, Froylan, Facchinetti, Patricia, Bourgeat, Pierre, Bambal, Ramesh B., Bishop, Paul B., Chan, Suzanne M.T., Moore, Andrew N.J.
Observations, Proteases, cholecystokinin

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Selective inhibition of cocaine-seeking behavior by a partial dopamine D(sub3) receptor agonist

Article Abstract:

Environmental stimuli associated with the effects of abused drugs, particularly cocaine, may produce craving in abstinent human substance abusers. The first D(sub3)-receptor-selective agonist, BP897 was designed and assessed in vitro and in vivo with mice having disrupted D(sub3)-receptor genes. BP 897 was found to inhibit cocaine-seeking behaviour.

Author: Schwartz, Jean-Charles, Everitt, Barry J., Pilla, Maria, Perachon, Sylvie, Sautel, Francois, Garrido, Fabrice, Mann, Andre, Wermuth, Camille G., Sokloff, Pierre
Prevention, Cocaine abuse, Drug abuse, Dopamine receptors

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High constitutive activity of native H3 receptors regulates histamine neurons in brain

Article Abstract:

Research carried out concludes that H3 receptors are present in rat brains and control histaminergic neuron activity.

Author: Stark, Holger, Morisset, Severine, Rouleau, Agnes, Ligneau, Xavier, Gbahou, Florence, Tardivel-Lacombe, Joel, Schunack, Walter, Ganellin, C. Robin, Schwartz, Jean-Charles, Arrang, Jean-Michael
Analysis, Brain research

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Subjects list: Research
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