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

A series of 17 long-chain arylpiperazines containing bulky, complex imide systems (5,8-dimethyl-3b,9-epoxy-(3a,4,5,6,7,8,9,9a)-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione or 4,9-diphenyl-4,9-epoxy-3a,4,9,9a-tetra-hydro-1H-benzo[f]isoindole-1,3(2H)-dione) was synthesized and evaluated for their affinity for serotonin 5-HT1A, 5-HT2A and dopamine D2 receptors. Most of the new compounds showed moderate activity at 5-HT1A binding sites (Ki = 100-492 nM), and two derivatives were found to have marked affinity for the 5-HT2A receptor subtype. None of the tested compounds displayed appreciable binding to dopamine D2 receptors Structure-activity relationships were discussed in respect to an arylpiperazine fragment, whereas the comparison of different imide terminals enabled determination of the size of a hydrophobic pocket (approximately 300 A3) within the 5-HT1A receptor.
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PMID:Introduction of a new complex imide system into the structure of LCAPs. The synthesis and a 5-HT1A, 5-HT2A and D2 receptor binding study. 1566 99

Pindolol and propranolol are used in the treatment of cardiovascular diseases, including hypotension or hypertension and antiarrythmic. Moreover, in the light of current 5-HT receptors classification it is known the mentioned drugs possess high 5-HT1A/5-HT1B affinity. It allows to establish two ways of researches. Department of Medicinal Chemistry of Medical University of Warsaw reports on synthesis of new compounds, analogues of Propranolol and Pindolol. A series of 5,8-dimethyl-3b,9-epoxy-3a,4,5,6,7,8,9,9a-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione and 6,7-dimethyl-4,9-epoxy-3a,4,5,8,9,9a-hexahydro-1H-benzo[f]isoindole-1,3(2H)-dione have been designed with oxygen bridged rings. This property provides pharmacological activity increasing and toxicity decreasing.
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PMID:Synthesis of some N-substituted aminoalkanol derivatives of 5,8-dimethyl-3b,9-epoxy-3a,4,5,6,7,8,9,9a-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione and 6,7-dimethyl-4,9-epoxy-3a,4,5,8,9,9a-hexahydro-1H-benzo[f]isoindole-1,3(2H)-dione with an expected b-adrenolytic activity. 1590 37