canadine--(r)-isomer and stepholidine

canadine--(r)-isomer has been researched along with stepholidine* in 1 studies

Other Studies

1 other study(ies) available for canadine--(r)-isomer and stepholidine

Article	Year
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile. Bioorganic & medicinal chemistry, 2013, Feb-15, Volume: 21, Issue:4 An effective and rapid method for the microwave-assisted preparation of the key intermediate for the total synthesis of tetrahydroprotoberberines (THPBs) including l-stepholidine (l-SPD) was developed. Thirty-one THPB derivatives with diverse substituents on A and D ring were synthesized, and their binding affinity to dopamine D(1), D(2) and serotonin 5-HT(1A) and 5-HT(2A) receptors were determined. Compounds 18k and 18m were identified as partial agonists at the D(1) receptor with K(i) values of 50 and 6.3nM, while both compounds act as D(2) receptor antagonists (K(i)=305 and 145nM, respectively) and 5-HT(1A) receptor full agonists (K(i)=149 and 908nM, respectively). These two THPBs compounds exerted antipsychotic actions in animal models. Further electrophysiological studies employing single-unit recording in intact animals demonstrated that 18k-excited dopaminergic (DA) neurons are associated with its 5-HT(1A) receptor agonistic activity. These results suggest that these two compounds targeted to multiple neurotransmitter receptors may present novel lead drugs with new pharmacological profiles for the treatment of schizophrenia. Topics: Animals; Antipsychotic Agents; Berberine; Berberine Alkaloids; CHO Cells; Cricetinae; Cricetulus; Dopamine D2 Receptor Antagonists; HEK293 Cells; Humans; Microwaves; Motor Activity; Protein Binding; Rats; Receptor, Serotonin, 5-HT1A; Receptor, Serotonin, 5-HT2A; Receptors, Dopamine D1; Receptors, Dopamine D2; Schizophrenia; Serotonin 5-HT1 Receptor Agonists; Structure-Activity Relationship	2013

Article

Year

Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.

Bioorganic & medicinal chemistry, 2013, Feb-15, Volume: 21, Issue:4

An effective and rapid method for the microwave-assisted preparation of the key intermediate for the total synthesis of tetrahydroprotoberberines (THPBs) including l-stepholidine (l-SPD) was developed. Thirty-one THPB derivatives with diverse substituents on A and D ring were synthesized, and their binding affinity to dopamine D(1), D(2) and serotonin 5-HT(1A) and 5-HT(2A) receptors were determined. Compounds 18k and 18m were identified as partial agonists at the D(1) receptor with K(i) values of 50 and 6.3nM, while both compounds act as D(2) receptor antagonists (K(i)=305 and 145nM, respectively) and 5-HT(1A) receptor full agonists (K(i)=149 and 908nM, respectively). These two THPBs compounds exerted antipsychotic actions in animal models. Further electrophysiological studies employing single-unit recording in intact animals demonstrated that 18k-excited dopaminergic (DA) neurons are associated with its 5-HT(1A) receptor agonistic activity. These results suggest that these two compounds targeted to multiple neurotransmitter receptors may present novel lead drugs with new pharmacological profiles for the treatment of schizophrenia.

Topics: Animals; Antipsychotic Agents; Berberine; Berberine Alkaloids; CHO Cells; Cricetinae; Cricetulus; Dopamine D2 Receptor Antagonists; HEK293 Cells; Humans; Microwaves; Motor Activity; Protein Binding; Rats; Receptor, Serotonin, 5-HT1A; Receptor, Serotonin, 5-HT2A; Receptors, Dopamine D1; Receptors, Dopamine D2; Schizophrenia; Serotonin 5-HT1 Receptor Agonists; Structure-Activity Relationship

2013