化学性质

资料参考

Benocyclidine is an inhibitor of dopamine reuptake [1, 2].

Dopamine plays important roles in the brain and body. In the brain, dopamine functions as a neurotransmitter involved in reward-motivated behavior, motor control and controlling the release of various hormones. Dysfunctions of the dopamine system have been associated several important diseases including Parkinson's disease, attention deficit hyperactivity disorder, schizophrenia, and addiction [3]. Dopamine also functions in blood vessels, kidneys, pancreas, the digestive system, the immune system, and the blood vessels.

Benocyclidine (BTCP) was a derivative of phencyclidine (PCP) with a benzothiophenyl group instead of a phenyl ring. BTCP potently inhibited dopamine (DA) uptake with the IC50 of 7-8 nM. BTCP showed low affinity for the PCP receptor with the IC50 of 6 μM [1, 2]. In the striatum, BTCP binding was dose-dependently inhibited by unlabeled BTCP and nomifensine with the ID50 of 6.34 mg/kg and 11.06 mg/kg, respectively. BTCP bound to the dopamine uptake complex in the mouse brain in vivo [4].

References:
[1] Vignon J, Pinet V, Cerruti C, et al.  [3H] N-[1-(2-Benzo (b) thiophenyl) cycohexyl] piperidine ([3H] BTCP): a new phencyclidine analog selective for the dopamine uptake complex[J]. European journal of pharmacology, 1988, 148(3): 427-436.
[2] Chaudieu I, Vignon J, Chicheportiche M, et al.  Role of the aromatic group in the inhibition of phencyclidine binding and dopamine uptake by PCP analogs[J]. Pharmacology Biochemistry and Behavior, 1989, 32(3): 699-705.
[3] Seeman P.  Brain dopamine receptors[J]. Pharmacological Reviews, 1980, 32(3): 229-313.
[4] Maurice T, Vignon J, Kamenka J M, et al.  In vivo labelling of the mouse dopamine uptake complex with the phencyclidine derivative [3 H] BTCP[J]. Neuroscience letters, 1989, 101(2): 234-238.