関: taltirelin hydrate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/07/18 16:41:51」(JST)

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Taltirelin (marketed under the tradename Ceredist) is a thyrotropin-releasing hormone (TRH) analog, which mimics the physiological actions of TRH, but with a much longer half-life and duration of effects,^[1] and little development of tolerance following prolonged dosing.^[2] It has nootropic,^[3] neuroprotective^[4] and analgesic effects.^[5]

Taltirelin is primarily being researched for the treatment of spinocerebellar ataxia; limited research has also been carried out with regard to other neurodegenerative disorders, e.g., spinal muscular atrophy.^[6]^[7]^[8]

References

^ Fukuchi, I.; Asahi, T.; Kawashima, K.; Kawashima, Y.; Yamamura, M.; Matsuoka, Y.; Kinoshita, K. (1998). "Effects of taltirelin hydrate (TA-0910), a novel thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in rat brain". Arzneimittel-Forschung 48 (4): 353–359. PMID 9608876.
^ Asai, H.; Asahi, T.; Yamamura, M.; Yamauchi-Kohno, R.; Saito, A. (2005). "Lack of behavioral tolerance by repeated treatment with taltirelin hydrate, a thyrotropin-releasing hormone analog, in rats". Pharmacology Biochemistry and Behavior 82 (4): 646–651. doi:10.1016/j.pbb.2005.11.004. PMID 16368129.
^ Yamamura, M.; Suzuki, M.; Matsumoto, K. (1997). "Synthesis and pharmacological action of TRH analog peptide (Taltirelin)". Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 110 Suppl 1: 33P–38P. PMID 9503402.
^ Urayama, A.; Yamada, S.; Kimura, R.; Zhang, J.; Watanabe, Y. (2002). "Neuroprotective effect and brain receptor binding of taltirelin, a novel thyrotropin-releasing hormone (TRH) analogue, in transient forebrain ischemia of C57BL/6J mice". Life Sciences 72 (4–5): 601–607. doi:10.1016/S0024-3205(02)02268-3. PMID 12467901.
^ Tanabe, M.; Tokuda, Y.; Takasu, K.; Ono, K.; Honda, M.; Ono, H. (2009). "The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems". British Journal of Pharmacology 150 (4): 403–414. doi:10.1038/sj.bjp.0707125. PMC 2189720. PMID 17220907.
^ Takeuchi, Y.; Miyanomae, Y.; Komatsu, H.; Oomizono, Y.; Nishimura, A.; Okano, S.; Nishiki, T.; Sawada, T. (1994). "Efficacy of Thyrotropin-Releasing Hormone in the Treatment of Spinal Muscular Atrophy". Journal of Child Neurology 9 (3): 287–289. doi:10.1177/088307389400900313. PMID 7930408.
^ Tzeng, A. C.; Cheng, J.; Fryczynski, H.; Niranjan, V.; Stitik, T.; Sial, A.; Takeuchi, Y.; Foye, P.; Deprince, M.; Bach, J. R. (2000). "A study of thyrotropin-releasing hormone for the treatment of spinal muscular atrophy: A preliminary report". American Journal of Physical Medicine & Rehabilitation 79 (5): 435–440. doi:10.1097/00002060-200009000-00005. PMID 10994885.
^ Kato, Z.; Okuda, M.; Okumura, Y.; Arai, T.; Teramoto, T.; Nishimura, M.; Kaneko, H.; Kondo, N. (2009). "Oral Administration of the Thyrotropin-Releasing Hormone (TRH) Analogue, Taltireline Hydrate, in Spinal Muscular Atrophy". Journal of Child Neurology 24 (8): 1010–1012. doi:10.1177/0883073809333535. PMID 19666885.

External links

(Japanese) Ceredist セレジスト錠 (PDF) Mitsubishi Tanabe Pharma. October 2007.

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English Journal

Thyrotropin-releasing hormone and its analogs accelerate wound healing.

Nie C1, Yang D2, Liu N1, Dong D3, Xu J4, Zhang J5.Author information 1Department of Head and Neck Surgery, The Third Affiliated Hospital of Harbin Medical University, Harbin, China.2Department of Plastic Surgery, The Second Affiliated Hospital of Harbin Medical University, Harbin, China.3Department of Pharmacology, Harbin Medical University, Harbin, China.4Department of Cell Biology, Harbin Medical University, Harbin, China.5Department of Head and Neck Surgery, The Third Affiliated Hospital of Harbin Medical University, Harbin, China. Electronic address: Jiewu_zhang@126.com.AbstractBACKGROUND: Thyrotropin-releasing hormone (TRH) is a classical hormone that controls thyroid hormone production in the anterior pituitary gland. However, recent evidence suggested that TRH is expressed in nonhypothalamic tissues such as epidermal keratinocytes and dermal fibroblasts, but its function is not clear. This study aimed to investigate the effects of TRH and its analogs on wound healing and explore the underlying mechanisms.
The Journal of surgical research.J Surg Res.2014 Mar 11. pii: S0022-4804(14)00238-8. doi: 10.1016/j.jss.2014.03.004. [Epub ahead of print]
BACKGROUND: Thyrotropin-releasing hormone (TRH) is a classical hormone that controls thyroid hormone production in the anterior pituitary gland. However, recent evidence suggested that TRH is expressed in nonhypothalamic tissues such as epidermal keratinocytes and dermal fibroblasts, but its functio
PMID 24713470

Thyrotropin-releasing hormone receptor type 1 (TRH-R1), not TRH-R2, primarily mediates taltirelin actions in the CNS of mice.

Thirunarayanan N1, Nir EA, Raaka BM, Gershengorn MC.Author information 1Laboratory of Endocrinology and Receptor Biology, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), National Institutes of Health (NIH), Bethesda, MD, USA.AbstractThyrotropin-releasing hormone receptor type 2 (TRH-R2), not TRH-R1, has been proposed to mediate the CNS effects of TRH and its more effective analog taltirelin (TAL). Consistent with this idea, TAL exhibited higher binding affinity and signaling potency at mouse TRH-R2 than TRH-R1 in a model cell system. We used TRH-R1 knockout (R1ko), R2ko and R1/R2ko mice to determine which receptor mediates the CNS effects of TAL. There was no TRH-R1 mRNA in R1ko and R1/R2ko mice and no TRH-R2 mRNA in R2ko and R1/R2ko mice. Specific [(3)H]MeTRH binding to whole brain membranes was 5% of wild type (WT) for R1ko mice, 100% for R2ko mice and 0% for R1/R2ko mice, indicating TRH-R1 is the predominant receptor expressed in the brain. In arousal assays, TAL shortened sleep time with pentobarbital sedation in WT and R2ko mice by 44 and 49% and with ketamine/xylazine sedation by 66 and 55%, but had no effect in R1ko and R1/R2ko mice. In a tail flick assay of nociception, TAL increased response latency by 65 and 70% in WT and R2ko mice, but had no effect in R1ko and R1/R2ko mice. In a tail suspension test of depression-like behavior, TAL increased mobility time by 49 and 37% in WT and R2ko mice, but had no effect in R1ko and R1/R2ko mice. Thus, in contrast to the generally accepted view that the CNS effects of TAL are mediated by TRH-R2, these effects are mediated primarily if not exclusively by TRH-R1 in mice.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology.Neuropsychopharmacology.2013 May;38(6):950-6. doi: 10.1038/npp.2012.256. Epub 2012 Dec 11.
Thyrotropin-releasing hormone receptor type 2 (TRH-R2), not TRH-R1, has been proposed to mediate the CNS effects of TRH and its more effective analog taltirelin (TAL). Consistent with this idea, TAL exhibited higher binding affinity and signaling potency at mouse TRH-R2 than TRH-R1 in a model cell s
PMID 23303050

Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor.

Thirunarayanan N1, Raaka BM, Gershengorn MC.Author information 1Laboratory of Endocrinology and Receptor Biology, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health Bethesda, MD, USA.AbstractTaltirelin (TAL) is a thyrotropin-releasing hormone (TRH) analog that is approved for use in humans in Japan. In this study, we characterized TAL binding to and signaling by the human TRH receptor (TRH-R) in a model cell system. We found that TAL exhibited lower binding affinities than TRH and lower signaling potency via the inositol-1,4,5-trisphosphate/calcium pathway than TRH. However, TAL exhibited higher intrinsic efficacy than TRH in stimulating inositol-1,4,5-trisphosphate second messenger generation. This is the first study that elucidates the pharmacology of TAL at TRH-R and shows that TAL is a superagonist at TRH-R. We suggest the superagonism exhibited by TAL may in part explain its higher activity in mediating central nervous system effects in humans compared to TRH.
Frontiers in endocrinology.Front Endocrinol (Lausanne).2012 Oct 9;3:120. doi: 10.3389/fendo.2012.00120. eCollection 2012.
Taltirelin (TAL) is a thyrotropin-releasing hormone (TRH) analog that is approved for use in humans in Japan. In this study, we characterized TAL binding to and signaling by the human TRH receptor (TRH-R) in a model cell system. We found that TAL exhibited lower binding affinities than TRH and lower
PMID 23087672

Japanese Journal

TRH誘導体タルチレリンの熱侵害受容に対する鎮痛作用は下行性セロトニン神経を介する

徳田泰士,田辺光男,本多基子,小野秀樹
日本神経精神薬理学雑誌 = Japanese journal of psychopharmacology 25(6), 331, 2005-12-25
NAID 10016943032

Taltirelin Improves Motor Ataxia Independently of Monoamine Levels in Rolling Mouse Nagoya, a Model of Spinocerebellar Atrophy(Pharmacology)

Nakamura Tomoka,Honda Motoko,Kimura Satoko [他],TANABE Mitsuo,ODA Senichi,ONO Hideki
Biological & pharmaceutical bulletin 28(12), 2244-2247, 2005-12-01
To examine the relationship between motor ataxia and monoamine levels in the central nervous system, the contents and concentrations of noradrenaline (NA), dopamine (DA) and serotonin (5-HT) in the ce …
NAID 110004049124

Blood-Brain Permeability of [^3H]-(3-methyl-His^2) Thyrotropin-releasing Hormone (MeTRH) in Mice : Effects of TRH and its Analogues

URAYAMA Akihiko,YAMADA Shizuo,OHMORI Yuki,DEGUCHI Yoshiharu,UCHIDA Shinya,KIMURA Ryohei
Drug metabolism and pharmacokinetics 18(5), 310-318, 2003-11-26
NAID 10012554183

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★リンクテーブル★

リンク元	「タルチレリン」
拡張検索	「taltirelin hydrate」

「タルチレリン」

Taltirelin
Systematic (IUPAC) name
	N-{[(4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-L-histidyl-L-prolinamide
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
Identifiers
CAS Number	103300-74-9 ; 201677-75-0
ATC code	none
PubChem	CID 656609
IUPHAR/BPS	2143
ChemSpider	102734
UNII	DOZ62MV6A5
Synonyms	(4S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(3H-imidazol-4-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
Chemical data
Formula	C17H31N7O9
Molar mass	477.46 g/mol
	SMILES CN1C(=O)C[C@H](NC1=O)C(=O)N[C@@H](CC2=CN=CN2)C(=O)N3CCC[C@H]3C(=O)N ;
	InChI InChI=1S/C17H23N7O5/c1-23-13(25)6-10(22-17(23)29)15(27)21-11(5-9-7-19-8-20-9)16(28)24-4-2-3-12(24)14(18)26/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29)/t10-,11-,12-/m0/s1 ; Key:LQZAIAZUDWIVPM-SRVKXCTJSA-N ;
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　　[★]

英: taltirelin
化: タルチレリン水和物 taltirelin hydrate
商: セレジスト
関: 脊髄小脳変性症。その他の中枢神経系用薬

「taltirelin hydrate」

　　[★] タルチレリン。タルチレリン水和物

[pmid9608876-1] Fukuchi, I.; Asahi, T.; Kawashima, K.; Kawashima, Y.; Yamamura, M.; Matsuoka, Y.; Kinoshita, K. (1998). "Effects of taltirelin hydrate (TA-0910), a novel thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in rat brain". Arzneimittel-Forschung 48 (4): 353–359. PMID 9608876.

[2] Asai, H.; Asahi, T.; Yamamura, M.; Yamauchi-Kohno, R.; Saito, A. (2005). "Lack of behavioral tolerance by repeated treatment with taltirelin hydrate, a thyrotropin-releasing hormone analog, in rats". Pharmacology Biochemistry and Behavior 82 (4): 646–651. doi:10.1016/j.pbb.2005.11.004. PMID 16368129.

[3] Yamamura, M.; Suzuki, M.; Matsumoto, K. (1997). "Synthesis and pharmacological action of TRH analog peptide (Taltirelin)". Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 110 Suppl 1: 33P–38P. PMID 9503402.

[4] Urayama, A.; Yamada, S.; Kimura, R.; Zhang, J.; Watanabe, Y. (2002). "Neuroprotective effect and brain receptor binding of taltirelin, a novel thyrotropin-releasing hormone (TRH) analogue, in transient forebrain ischemia of C57BL/6J mice". Life Sciences 72 (4–5): 601–607. doi:10.1016/S0024-3205(02)02268-3. PMID 12467901.

[5] Tanabe, M.; Tokuda, Y.; Takasu, K.; Ono, K.; Honda, M.; Ono, H. (2009). "The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems". British Journal of Pharmacology 150 (4): 403–414. doi:10.1038/sj.bjp.0707125. PMC 2189720. PMID 17220907.

[6] Takeuchi, Y.; Miyanomae, Y.; Komatsu, H.; Oomizono, Y.; Nishimura, A.; Okano, S.; Nishiki, T.; Sawada, T. (1994). "Efficacy of Thyrotropin-Releasing Hormone in the Treatment of Spinal Muscular Atrophy". Journal of Child Neurology 9 (3): 287–289. doi:10.1177/088307389400900313. PMID 7930408.

[7] Tzeng, A. C.; Cheng, J.; Fryczynski, H.; Niranjan, V.; Stitik, T.; Sial, A.; Takeuchi, Y.; Foye, P.; Deprince, M.; Bach, J. R. (2000). "A study of thyrotropin-releasing hormone for the treatment of spinal muscular atrophy: A preliminary report". American Journal of Physical Medicine & Rehabilitation 79 (5): 435–440. doi:10.1097/00002060-200009000-00005. PMID 10994885.

[8] Kato, Z.; Okuda, M.; Okumura, Y.; Arai, T.; Teramoto, T.; Nishimura, M.; Kaneko, H.; Kondo, N. (2009). "Oral Administration of the Thyrotropin-Releasing Hormone (TRH) Analogue, Taltireline Hydrate, in Spinal Muscular Atrophy". Journal of Child Neurology 24 (8): 1010–1012. doi:10.1177/0883073809333535. PMID 19666885.

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