An active metabolite of carbamazepine, carbamazepine-10,11-epoxide, inhibits ion channel-mediated catecholamine secretion in cultured bovine adrenal medullary cells.

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Title:	An active metabolite of carbamazepine, carbamazepine-10,11-epoxide, inhibits ion channel-mediated catecholamine secretion in cultured bovine adrenal medullary cells.
Authors:	Yoshimura, Reiji, Yanagihara, N., Terao, Takeshi, Minami, Kouichiro, Toyohira, Yumiko, Ueno, Susumu, Uezono, Yasuhito, Abe, Kazuhiko, Izumi, Futoshi
Source:	Psychopharmacology. 1998, Vol. 135 Issue 4, p368. 6p.
Subjects:	Carbamazepine, Ion channels, Catecholamines, Cholinergic receptors, Physiology
Abstract:	Abstract We have recently reported inhibitory effects of carbamazepine (CBZ) on ion channel-mediated secretion of catecholamines in bovine adrenal medullary cells. Here, we report the effects of carbamazepine 10,11-epoxide (CBZ-E), an active metabolite of CBZ, and carbamazepine-10,11-diol (CBZ-D), a non-active metabolite, on [sup 22]Na[sup +] influx, [sup 45]Ca[sup 2+] influx and catecholamine secretion in cultured adrenal medullary cells. CBZ-E, but not CBZ-D inhibited [sup 22]Na[sub +] influx, [sup 45]Ca[sup 2+] influx and catecholamine secretion induced by carbachol or veratridine with a half-maximal inhibitory concentration (IC[sub 50]) of 0.26 or 0.68 mug/ml, respectively. CBZ-E also inhibited high K[sup +]-evoked [sup 45]Ca[sub 2+] influx and catecholamine secretion (IC[sub 50] = 0.3 mug/ml), but CBZ-D did not. These findings suggest that CBZ-E, but not CBZ-D, attenuates catecholamine secretion by inhibiting nicotinic acetylcholine receptor-associated ion channels, voltage-dependent Na[sup +] channels and voltage-dependent Ca[sup 2+] channels in the cells. This inhibition... [ABSTRACT FROM AUTHOR]
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Database:	Psychology and Behavioral Sciences Collection

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Abstract:	Abstract We have recently reported inhibitory effects of carbamazepine (CBZ) on ion channel-mediated secretion of catecholamines in bovine adrenal medullary cells. Here, we report the effects of carbamazepine 10,11-epoxide (CBZ-E), an active metabolite of CBZ, and carbamazepine-10,11-diol (CBZ-D), a non-active metabolite, on [sup 22]Na[sup +] influx, [sup 45]Ca[sup 2+] influx and catecholamine secretion in cultured adrenal medullary cells. CBZ-E, but not CBZ-D inhibited [sup 22]Na[sub +] influx, [sup 45]Ca[sup 2+] influx and catecholamine secretion induced by carbachol or veratridine with a half-maximal inhibitory concentration (IC[sub 50]) of 0.26 or 0.68 mug/ml, respectively. CBZ-E also inhibited high K[sup +]-evoked [sup 45]Ca[sub 2+] influx and catecholamine secretion (IC[sub 50] = 0.3 mug/ml), but CBZ-D did not. These findings suggest that CBZ-E, but not CBZ-D, attenuates catecholamine secretion by inhibiting nicotinic acetylcholine receptor-associated ion channels, voltage-dependent Na[sup +] channels and voltage-dependent Ca[sup 2+] channels in the cells. This inhibition... [ABSTRACT FROM AUTHOR]
ISSN:	00333158
DOI:	10.1007/s002130050524