Last update 01 Nov 2024

TRHR

Last update 01 Nov 2024

Basic Info

Synonyms

Thyroliberin receptor, thyrotropin releasing hormone receptor, Thyrotropin-releasing hormone receptor

+ [3]

Introduction

Receptor for thyrotropin-releasing hormone (TRH). Upon ligand binding, this G-protein-coupled receptor triggers activation of the phosphatidylinositol (IP3)-calcium-protein kinase C (PKC) pathway.

Drugs associated with TRHR

Taltirelin Hydrate

Target

TRHR

Mechanism

TRHR agonists

Active Org.

Mitsubishi Tanabe Pharma Corp. [+1]

Originator Org.

Mitsubishi Tanabe Pharma Corp.

Active Indication

Spinocerebellar Degenerations [+1]

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date26 Oct 2009

Protirelin

Target

TRHR

Mechanism

TRHR agonists

Active Org.

Livzon Group Livzon Pharmaceutical Factory [+1]

Originator Org.

Abbott Laboratories

Active Indication

Hypothyroidism [+2]

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date05 Nov 1976

DN-1417

Target

TRHR

Mechanism

TRHR agonists

Active Org.

Takeda Pharmaceuticals LLC

Originator Org.

Takeda Pharmaceutical Co., Ltd.

Active Indication

Central Nervous System Diseases

Inactive Indication

Epilepsy

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with TRHR

CTR20233554 / CompletedNot Applicable

评价他替瑞林片在中国成年健康受试者中的一项单中心、随机、开放、空腹/餐后单次给药、两制剂、两周期、双交叉的生物等效性研究

[Translation] A single-center, randomized, open-label, single-dose, fasting/fed, two-dose, two-period, double-crossover bioequivalence study to evaluate the efficacy of talactirelin tablets in healthy adult Chinese subjects

主要目的：评价空腹/餐后状态下受试制剂和参比制剂在中国成年健康受试者中的生物等效性。次要目的：评价空腹/餐后状态下受试制剂和参比制剂在中国健康成年受试者中的安全性。

[Translation]

Primary objective: Evaluate the bioequivalence of the test formulation and the reference formulation in Chinese healthy adult subjects in the fasting/fed state. Secondary objective: Evaluate the safety of the test formulation and the reference formulation in Chinese healthy adult subjects in the fasting/fed state.

Start Date01 Nov 2023

Sponsor / Collaborator

Jiangsu Durui Pharmaceutical Co. Ltd.

CTR20232774 / CompletedNot Applicable

他替瑞林片随机、开放、两制剂、两周期、双交叉在健康人体餐后条件下生物等效性试验

[Translation] A randomized, open-label, two-dose, two-period, double-crossover bioequivalence study of talatirelin tablets in healthy volunteers under postprandial conditions

主要目的：评价在餐后给药条件下，受试制剂他替瑞林片（四川科伦药业股份有限公司生产）5mg和参比制剂他替瑞林片（商品名：Ceredist®，田辺三菱製薬株式会社生产）5mg在中国健康受试者中的生物等效性。次要目的：评价中国健康成人受试者餐后口服试验药物他替瑞林片的安全性。

[Translation]

Main purpose: To evaluate the test preparation Tatirelin Tablets (manufactured by Sichuan Kelun Pharmaceutical Co., Ltd.) 5 mg and the reference preparation Tatirelin Tablets (trade name: Ceredist®, Mitsubishi Tabei) under postprandial administration conditions. Bioequivalence of 5 mg (manufactured by Seiko Co., Ltd.) in Chinese healthy subjects. Secondary objective: To evaluate the safety of oral administration of the experimental drug tartirelin tablets to healthy adult subjects in China after meals.

Start Date04 Sep 2023

Sponsor / Collaborator

Chengdu Jianze Pharmaceutical Technology Co., Ltd.

CTR20232775 / CompletedNot Applicable

他替瑞林片随机、开放、两制剂、两周期、双交叉在健康人体空腹条件下生物等效性试验

[Translation] A randomized, open-label, two-dose, two-period, double-crossover bioequivalence study of talatirelin tablets in healthy volunteers under fasting conditions

主要目的：评价在空腹给药条件下，受试制剂他替瑞林片（四川科伦药业股份有限公司生产）5mg和参比制剂他替瑞林片（商品名：Ceredist®，田辺三菱製薬株式会社生产）5mg在中国健康受试者中的生物等效性。次要目的：评价中国健康成人受试者空腹口服试验药物他替瑞林片的安全性。

[Translation]

Main purpose: To evaluate the efficacy of the test preparation Tatirelin Tablets (manufactured by Sichuan Kelun Pharmaceutical Co., Ltd.) 5 mg and the reference preparation Tatirelin Tablets (trade name: Ceredist®, manufactured by Mitsubishi Tabae) under fasting administration conditions. Bioequivalence of 5 mg (produced by 薬有限公司) in Chinese healthy subjects. Secondary objective: To evaluate the safety of oral administration of the investigational drug tartirelin tablets to healthy Chinese adult subjects on an empty stomach.

Start Date23 Jul 2023

Sponsor / Collaborator

Chengdu Jianze Pharmaceutical Technology Co., Ltd.

100 Clinical Results associated with TRHR

100 Translational Medicine associated with TRHR

0 Patents (Medical) associated with TRHR

3,410

Literatures (Medical) associated with TRHR

01 Nov 2024·Colloids and Surfaces B: Biointerfaces

Contribution of chemical permeation enhancers to the process of transdermal drug delivery: Adsorption, microscopic interactions, and mechanism

Article

Author: Li, Ying ; Zhang, Heng ; Yuan, Shiling ; Liu, Shasha ; Jiang, Zhaoli

Transdermal drug delivery (TDD) has attracted widespread attention because of the advantage of its non-invasive nature, easy self-administration, and low side effects. The key to this pathway of drug delivery is how to overcome the barrier of the lipid matrix in the stratum corneum (SC). In this work, molecular dynamics (MD) were employed to investigate the adsorption of thyrotropin-releasing hormone (TRH) on the SC, and the effects of three different chemical permeation enhancers (ethanol (ETOH), carveol (CAV), and borneol (BOR)) on the SC were analyzed. The results showed that ETOH hardly altered the order of lipids in the SC, while CAV and BOR disrupted the morphology of the SC. The primary target of CAV was the CHOL in SC, which not only disrupted the ordered arrangement of CHOL, but also "extracted" CHOL from SC. The thickness distribution of SC became more inhomogeneous in the presence of CAV and BOR, which facilitated the penetration of drug molecules. Compared to no chemical permeation enhancers, the free energy of permeation in the presence of chemical permeation enhancers was less than 4-10 kcal mol^-1, which suggested that chemical permeation enhancers were more favorable for the permeation of drugs from viewpoints of thermodynamics. All the results provided theoretical insights into the effect of chemical permeation enhancers on the transdermal permeation of drugs.

01 Nov 2024·The Lancet Diabetes & Endocrinology

Aberrant hormone receptors regulate a wide spectrum of endocrine tumors

Review

Author: Louiset, Estelle ; Lefebvre, Hervé ; Kamenický, Peter ; Bourdeau, Isabelle ; Chasseloup, Fanny ; Lacroix, André ; Lopez, Antoine-Guy

Aberrant G-protein coupled receptor (GPCR) expression is highly prevalent in cortisol-secreting primary bilateral macronodular adrenal hyperplasia (PBMAH) and unilateral adenomas. The aberrant expression of diverse GPCRs and their ligands play an important role in the over-function of various endocrine tumours. Examples include aberrant expression of MC2R, 5-HT4R, AVPR1A, LHCGR, and GnRHR in primary aldosteronism; GCGR, LHCGR, and 5-HT4R in phaeochromocytomas and paragangliomas; TRHR, GnRHR, GIPR, and GRP101 in pituitary somatotroph tumours; AVPR2, D2DR, and SSTR5 in pituitary corticotroph tumours; GLP1R, GIPR, and somatostatin receptors in medullary thyroid carcinoma; and SSTRs, GLP1R, and GIPR in other neuroendocrine tumours. The genetic mechanisms causing the ectopic expression of GIPR in cortisol-secreting PBMAHs and unilateral adenomas have been identified, but distinct mechanisms are implicated in other endocrine tumours. Development of functional imaging targeting aberrant GPCRs should be useful for identification and for specific therapies of this wide spectrum of tumours. The aim of this review is to show that the regulation of endocrine tumours by aberrant GPCR is not restricted to cortisol-secreting adrenal lesions, but also occurs in tumours of several other organs.

29 Oct 2024·Environmental Science & Technology

Thyroid Endocrine Disruption and Mechanism of the Marine Antifouling Pollutant 4,5-Dichloro-2-n-octyl-4-isothiazolin-3-one

Article

Author: Liu, Mengyuan ; Li, Jiali ; Chen, Lianguo ; Hu, Chenyan ; Lam, Paul K.S. ; Zhou, Bingsheng

The antifoulant 4,5-dichloro-2-n-octyl-4-isothiazolin-3-one (DCOIT) is an emerging pollutant in the marine environment, which may disrupt the thyroid endocrine system. However, DCOIT toxicity in relation to thyroid endocrine disruption and the underlying mechanisms remains largely unclear. In this study, in vivo, in silico, in vitro, and ex vivo assays were performed to clarify DCOIT's thyroid toxicity. First, marine medaka (Oryzias melastigma) were exposed to environmentally realistic concentrations of DCOIT for an entire life cycle. The results demonstrated that DCOIT exposure potently stimulated the hypothalamic-pituitary-thyroid axis, characterized by hyperthyroidism symptom induction and prevalent key gene and protein upregulation in the brain. Moreover, the in silico and in vitro results evidenced that DCOIT could bind to thyroid hormone receptor β (TRβ) and interact synergistically with triiodothyronine, thus promoting GH3 cell proliferation. The CUT&Tag experiment found that DCOIT interfered with the affinity fingerprint of TRβ to target genes implicated in thyroid hormone signaling cascade regulation. Furthermore, ex vivo, Chem-seq revealed that DCOIT directly bound to the genomic sequences of thyrotropin-releasing hormone receptor b and thyroid-stimulating hormone receptor in marine medaka brain tissues. In conclusion, the current multifaceted evidence confirmed that DCOIT has a strong potency for thyroid endocrine system disruption and provided comprehensive insights into its toxicity mechanisms.

Analysis

Perform a panoramic analysis of this field.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis

TRHR

Basic Info

Related

Analysis