Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P08908 (5-HT1A)
 5,574 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

1. In order to investigate the functional interaction between adenosine receptors and G-proteins in native brain membranes, stimulation of high-affinity GTPase activity by adenosine receptor agonists was characterized in rat hippocampal membranes. 2. Addition of 1 microM R-N6-phenylisopropyladenosine (R-PIA), a selective A1 adenosine receptor agonist, augmented the Vmax of the low-KM GTPase by 51%, with a slight increase in the KM value. 3. Several adenosine receptor agonists stimulated the high-affinity GTPase activity in a concentration-dependent manner, with a rank order of potency indicative of the involvement of A1 adenosine receptor subtype as follows: R-PIA > N6-cyclohexyladenosine > 5'-N-ethylcarboxamidoadenosine > or = 2-chloroadenosine > S-PIA > CGS 21680, 2-phenylaminoadenosine. 4. The selective A1 adenosine receptor antagonist, 8-cyclopentyl-1,3-dipropylxanthine, inhibited R-PIA-stimulated high-affinity GTPase activity in a competitive manner, with a KB value of 2.5 nM. 5. The activating effects on high-affinity GTPase of R-PIA (via A1 adenosine receptors) and of 5-HT (via 5-HT1A receptors) were completely additive, indicating that A1 adenosine and 5-HT1A receptors were coupled to distinct pools of G-proteins in hippocampus. 6. Stimulation of high-affinity GTPase activity by adenosine receptor agonists can be used as a valuable measure for the investigation of the functional coupling between A1 adenosine receptors and G-proteins associated with adenylyl cyclase inhibition.
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PMID:Functional coupling between A1 adenosine receptors and G-proteins in rat hippocampal membranes assessed by high-affinity GTPase activity. 859 Sep 91

The basal ganglia in the brain contains glutamate, dopamine, serotonin, noradrenaline, CCK, adenosine, opioid, cannabinoid, etc. These agents contribute to keep motor control and modulation of the agent may be a cue to the treatment of movement disorders. D1 or D2 dopamine receptor agonists increase locomotor activity in MPTP-treated common marmosets which showed decreased locomotor activity and decreased number of dopamine neurons in the substantia nigra. Using this model of parkinsonism, NMDA receptor antag-onists, antimuscarinic receptor antagonists, 5-HT1A receptor agonists, adenosine receptor antagonists were showed to reverse the impaired movement of the model animals. The results may contribute to the development of new drugs for the treatment of Parkinson's disease.
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PMID:[The pharmacological and rational theory for the drug development of Parkinson's disease]. 1546 80