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Cyclothiazide (Anhydron, Acquirel, Doburil, Fluidil, Renazide, Tensodiural, Valmiran) is a benzothiadiazide (thiazide) diuretic and antihypertensive that was originally introduced in the United States in 1963 by Eli Lilly and was subsequently also marketed in Europe and Japan.^[1]^[2] Related drugs include diazoxide, hydrochlorothiazide, and chlorothiazide.^[3]

In 1993, it was discovered that cyclothiazide is a positive allosteric modulator of the AMPA and kainate receptors, capable of reducing or essentially eliminating rapid desensitization of the former receptor, and potentiating AMPA-mediated glutamate currents by as much as 18-fold at the highest concentration tested (100 μM).^[3]^[4]^[5]^[6] Additionally, in 2003, cyclothiazide was also found to act as a GABA_A receptor negative allosteric modulator, potently inhibiting GABA_A-mediated currents.^[7] In animals it is a powerful convulsant, robustly enhancing epileptiform activity and inducing seizures, but without producing any apparent neuronal death.^[8]^[9]

References

^ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. p. 1932. ISBN 3-88763-075-0.
^ Sittig, Marshall (1988). Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. p. 1756. ISBN 0-8155-1144-2.
^ ^a ^b Skolnick, Phil; Palfreyman, Michael G.; Reynolds, Ian J. (1994). Direct and allosteric control of glutamate receptors. Boca Raton: CRC Press. p. 174. ISBN 0-8493-8307-2.
^ Yamada KA, Tang CM (September 1993). "Benzothiadiazides inhibit rapid glutamate receptor desensitization and enhance glutamatergic synaptic currents". Journal of Neuroscience 13 (9): 3904–15. PMID 8103555.
^ Bertolino M, Baraldi M, Parenti C et al. (1993). "Modulation of AMPA/kainate receptors by analogues of diazoxide and cyclothiazide in thin slices of rat hippocampus". Receptors & Channels 1 (4): 267–78. PMID 7915948.
^ Ströhle, Andreas; Bilkei-Gorzo, A.; Holsboer, Florian (2005). Anxiety and anxiolytic drugs. Berlin: Springer. p. 566. ISBN 3-540-22568-4.
^ Deng L, Chen G (October 2003). "Cyclothiazide potently inhibits gamma-aminobutyric acid type A receptors in addition to enhancing glutamate responses". Proceedings of the National Academy of Sciences of the United States of America 100 (22): 13025–9. doi:10.1073/pnas.2133370100. PMC 240738. PMID 14534329.
^ Qi J, Wang Y, Jiang M, Warren P, Chen G (March 2006). "Cyclothiazide induces robust epileptiform activity in rat hippocampal neurons both in vitro and in vivo". The Journal of Physiology 571 (Pt 3): 605–18. doi:10.1113/jphysiol.2005.103812. PMC 1805799. PMID 16423850.
^ Kong S, Qian B, Liu J, Fan M, Chen G, Wang Y (July 2010). "Cyclothiazide induces seizure behavior in freely moving rats". Brain Research 1355: 207–213. doi:10.1016/j.brainres.2010.07.088. PMC 2947190. PMID 20678492.

English Journal

Nicotinic receptors modulate the function of presynaptic AMPA receptors on glutamatergic nerve terminals in the trigeminal caudal nucleus.

Samengo IA1, Currò D1, Martire M2.
Neurochemistry international.Neurochem Int.2015 Aug 12. pii: S0197-0186(15)30036-X. doi: 10.1016/j.neuint.2015.08.008. [Epub ahead of print]
In this study, we demonstrate the existence on trigeminal caudal nucleus (TCN) glutamatergic terminals of α4β2 nicotinic receptors (nAChRs) capable of enhancing the terminals' spontaneous release of [3H]D-aspartate ([3H]D-Asp). In rat TCN synaptosomes, spontaneous [3H]D-Asp release was increased b
PMID 26277383

Quantification of bursting and synchrony in cultured hippocampal neurons.

Eisenman LN1, Emnett CM2, Mohan J2, Zorumski CF3, Mennerick S3.
Journal of neurophysiology.J Neurophysiol.2015 Aug;114(2):1059-71. doi: 10.1152/jn.00079.2015. Epub 2015 Jun 3.
It is widely appreciated that neuronal networks exhibit patterns of bursting and synchrony that are not captured by simple measures such as average spike rate. These patterns can encode information or represent pathological behavior such as seizures. However, methods for quantifying bursting and syn
PMID 26041823

Prenatal nicotine is associated with reduced AMPA and NMDA receptor-mediated rises in calcium within the laterodorsal tegmentum: a pontine nucleus involved in addiction processes.

McNair LF1, Kohlmeier KA1.
Journal of developmental origins of health and disease.J Dev Orig Health Dis.2015 Jun;6(3):225-41. doi: 10.1017/S2040174414000439. Epub 2014 Nov 3.
Despite huge efforts from public sectors to educate society as to the deleterious physiological consequences of smoking while pregnant, 12-25% of all babies worldwide are born to mothers who smoked during their pregnancies. Chief among the negative legacies bestowed to the exposed individual is an e
PMID 25362989

Japanese Journal

Blocking AMPA receptor desensitization prolongs spontaneous EPSC decay times and depolarizes H1 horizontal cells in carp retinal slices

Neuroscience research : the official journal of the Japan Neuroscience Society 40(3), 217-225, 2001-07-01
NAID 50000904861

Synaptic and Non-synaptic AMPA Receptors Permeable to Calcium

The Japanese journal of pharmacology 86(1), 1-17, 2001-05-01
NAID 10007121159

Modulation of desensitization at glutamate receptors in isolated crucian carp horizontal cells by concanavalin A, cyclothiazide, aniracetam and PETA

Neuroscience 89, 979-990, 1999
NAID 30008317693

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リンク元	「シクロチアジド」「チクロチアジド」

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Cyclothiazide
Systematic (IUPAC) name
	3-(bicyclo[2.2.1]hept-5-en-2-yl)-6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
Clinical data
Legal status	℞ (Prescription only);
Identifiers
CAS Registry Number	2259-96-3
ATC code	C03AA09
PubChem	CID 2910
DrugBank	DB00606
ChemSpider	4535011
UNII	P71U09G5BW
KEGG	D01256
ChEMBL	CHEMBL61593
Chemical data
Formula	C14H16ClN3O4S2
Molecular mass	389.88 g/mol
	SMILES O=S(=O)(c1c(Cl)cc2c(c1)S(=O)(=O)NC(N2)C4[C@@H]3\C=C/[C@@H](C3)C4)N;
	InChI InChI=1S/C14H16ClN3O4S2/c15-10-5-11-13(6-12(10)23(16,19)20)24(21,22)18-14(17-11)9-4-7-1-2-8(9)3-7/h1-2,5-9,14,17-18H,3-4H2,(H2,16,19,20)/t7-,8+,9?,14?/m0/s1 ; Key:BOCUKUHCLICSIY-QJWLJZLASA-N ;
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