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HTR1B Membrane Protein Introduction

Introduction of HTR1B

5-hydroxytryptamine receptor 1B, also known as 5-HT-1B or 5-HT1B, is encoded by HTR1B gene in human. It is a subtype of serotonin receptor (5-HT receptor) that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT), and belongs to the G protein-coupled receptor (GPCR) family. HTR1B is widely expressed throughout the CNS central nervous system with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus. The function of the HTR1B differs relying on its location.

Basic Information of HTR1B
Protein Name 5-hydroxytryptamine receptor 1B
Gene Name HTR1B
Aliases S12, 5-HT1B, HTR1D2, HTR1DB, 5-HT-1B
Organism Homo sapiens (Human)
UniProt ID P28222
Transmembrane Times 7
Length (aa) 390
Sequence MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALITLATTLSNAFV
IATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQVVCDFWLSSDITCCTASILHL
CVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISISLPPFFWRQAKAEEEVSECVVNTDHILYTV
YSTVGAFYFPTLLLIALYGRIYVEARSRILKQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSE
SGSPVYVNQVKVRVSDALLEKKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAI
FDFFTWLGYLNSLINPIIYTMSNEDFKQAFHKLIRFKCTS

Function of HTR1B Membrane Protein

The binding of HTR1B and its ligand activates second messengers that causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and regulates the activity of downstream effectors, such as adenylate cyclase. In the frontal cortex, HTR1B is supposed to act as a postsynaptic receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, several studies suggest HTR1B signaling functions on an autoreceptor, inhibiting the release of serotonin and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency. And in the hippocampus, it has demonstrated that activation of postsynaptic HTR1B heteroreceptors induces a facilitation in excitatory synaptic transmission which is altered in depression. HTR1B is also involved in vasoconstriction of cerebral arteries. Besides, HTR1B can function as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD).

Structure of 5-HT1B membrane protein. Fig.1 Structure of 5-HT1B membrane protein.

Application of HTR1B Membrane Protein in Literature

  1. Bräunig J., et al. The trace amine-associated receptor 1 agonist 3-iodothyronamine induces biased signaling at the serotonin 1b receptor. Front Pharmacol. 2018, 9:222. PubMed ID: 29593543

    The results of this article provided evidence for 5-HT1b as a new receptor target for 3-T1AM, albeit with a different signaling effect than the endogenous ligand. And this indicated a complex interrelation of signaling effects between the investigated GPCRs and respective ligands.

  2. Tiger M., et al. The 5-HT1B receptor-a potential target for antidepressant treatment. Psychopharmacology (Berl). 2018, 235(5):1317-1334. PubMed ID: 29546551

    This study found that 5-HT1BR agonists most consistently displayed antidepressant-like properties when 5-HT1BR ligands were administered to animals.

  3. Deen M., et al. Low 5-HT1B receptor binding in the migraine brain: A PET study. Cephalalgia. 2018, 38(3):519-527. PubMed ID: 28730894

    Authors of this article reported here for the first time that migraine patients had low 5-HT1B receptor binding in pain-modulating regions reflecting decreased receptor density. This was either a primary constitutive trait of the migraine brain or secondary to repeated exposure to migraine attacks.

  4. P da Cunha-Bang S., et al. Anterior cingulate serotonin 1B receptor binding is associated with emotional response inhibition. J Psychiatr Res. 2017, 92:199-204. PubMed ID: 28502766

    The findings indicated that 5-HT1BRs in the anterior cingulate were involved in a prepotent response in the context of angry faces. Our findings suggested that serotonin modulated response inhibition in the context of certain emotional stimuli.

  5. Veldman E. R., et al. Distribution and levels of 5-HT1B receptors in anterior cingulate cortex of patients with bipolar disorder, major depressive disorder and schizophrenia-An autoradiography study. Eur Neuropsychopharmacol. 2017, 27(5):504-514. PubMed ID: 28318898

    The binding distribution of the serotonin 1B receptor found in this study supported a role in glutamate transmission in the ACC and was not shown to be significantly altered in BD (bipolar disorder), MDD (major depressive disorder) or SZ (schizophrenia).

HTR1B Preparation Options

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