5-HT2 receptor subtypes: a family re-united?

Abstract:

:The current classification for 5-HT2 receptors accommodates three subtypes. In addition to the originally defined 5-HT2 receptor, sanctuary is now provided for the structurally related 5-HT1c receptor (now 5-HT2c) and at least one atypical 5-HT receptor subtype. The strong functional union of this family is reflected in the paucity of ligands that will discriminate between its subtypes and prompts some re-evaluation of the activities of compounds which may now be regarded as nonselective for the receptor subtypes in this class. In this article, Gordon Baxter and colleagues examine the pharmacology of both officially recognized and atypical 5-HT2 receptor subtypes. A number of novel selective agents are highlighted, some of which may prove useful for 5-HT2 receptor classification and, ultimately, clarify the mechanistic basis for current and future therapeutic strategies which target this receptor family.

journal_name

Trends Pharmacol Sci

authors

Baxter G,Kennett G,Blaney F,Blackburn T

doi

10.1016/s0165-6147(00)88991-9

subject

Has Abstract

pub_date

1995-03-01 00:00:00

pages

105-10

issue

3

eissn

0165-6147

issn

1873-3735

pii

S0165-6147(00)88991-9

journal_volume

16

pub_type

杂志文章,评审
  • Intracellular 5-HT 2C-receptor dephosphorylation: a new target for treating drug addiction.

    abstract::The 5-hydroxytryptamine (5-HT)(2C) receptor has received considerable attention as a target for treating drug addiction. 5-HT(2C)-receptor agonism, however, also induces side-effects. In this article, we review recent findings regarding the involvement of 5-HT(2C) receptors in behaviours related to drug addiction in a...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2006.07.003

    authors: Müller CP,Carey RJ

    更新日期:2006-09-01 00:00:00

  • Pharmacological tools for the development of traditional Chinese medicine.

    abstract::Pharmacology as a modern science was introduced in China approximately 150 years ago, and has been used since then to study traditional Chinese medicine (TCM). Pharmacology has experienced its own development over this time and continues to provide new tools for the study of TCM. In the present review, three models fo...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2013.09.004

    authors: Liu X,Wu WY,Jiang BH,Yang M,Guo DA

    更新日期:2013-11-01 00:00:00

  • Rho-Rho-kinase pathway in smooth muscle contraction and cytoskeletal reorganization of non-muscle cells.

    abstract::Hypercontraction or abnormal contraction of vascular smooth muscle is a major cause of diseases such as hypertension and vasospasm of the coronary and cerebral arteries. A better understanding of the mechanism of regulation of smooth muscle contraction should lead to improved treatments for such diseases. Recent studi...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01596-0

    authors: Fukata Y,Amano M,Kaibuchi K

    更新日期:2001-01-01 00:00:00

  • A novel way to spread drug resistance in tumor cells: functional intercellular transfer of P-glycoprotein (ABCB1).

    abstract::Intercellular transfer of proteins is a mode of communication between cells that is crucial for certain physiological processes. Chemotherapy is the treatment of choice for approximately 50% of all cancers. However, multidrug resistance mediated by drug-efflux pumps such as P-glycoprotein (Pgp) minimizes the effective...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2005.06.001

    authors: Ambudkar SV,Sauna ZE,Gottesman MM,Szakacs G

    更新日期:2005-08-01 00:00:00

  • Regulation of drug-induced liver injury by signal transduction pathways: critical role of mitochondria.

    abstract::Drugs that cause liver injury often 'stress' mitochondria and activate signal transduction pathways important in determining cell survival or death. In most cases, hepatocytes adapt to the drug-induced stress by activating adaptive signaling pathways, such as mitochondrial adaptive responses and nuclear factor erythro...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2013.01.009

    authors: Han D,Dara L,Win S,Than TA,Yuan L,Abbasi SQ,Liu ZX,Kaplowitz N

    更新日期:2013-04-01 00:00:00

  • Annexin A1 in the brain--undiscovered roles?

    abstract::Annexin A1 (ANXA1) is an endogenous protein known to have potent anti-inflammatory properties in the peripheral system. It has also been detected in the brain, but its function there is still ambiguous. In this review, we have, for the first time, collated the evidence currently available on the function of ANXA1 in t...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2007.12.003

    authors: Solito E,McArthur S,Christian H,Gavins F,Buckingham JC,Gillies GE

    更新日期:2008-03-01 00:00:00

  • Identifying Missing Biosynthesis Enzymes of Plant Natural Products.

    abstract::Elucidating plant-specialized biosynthetic pathways has always constituted a laborious task, notably for natural products with high pharmaceutical values. Here, we discuss emerging omics-based strategies that facilitate the identification of genes from these complex metabolic pathways, paving the way to engineered sup...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.tips.2019.12.006

    authors: Dugé de Bernonville T,Papon N,Clastre M,O'Connor SE,Courdavault V

    更新日期:2020-03-01 00:00:00

  • Lithium therapy and signal transduction.

    abstract::Lithium is the simplest therapeutic agent available for the treatment of depression and has been used for over 100 years, yet no definitive mechanism for its effect has been established. Among the proposed mechanisms, two lithium-sensitive signal transduction pathways are active in the brain; these are mediated by gly...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/s0165-6147(99)01428-5

    authors: Williams RS,Harwood AJ

    更新日期:2000-02-01 00:00:00

  • Drugs of abuse: anatomy, pharmacology and function of reward pathways.

    abstract::Drugs of abuse are very powerful reinforcers, and even in conditions of limited access (where the organism is not dependent) these drugs will motivate high rates of operant responding. This presumed hedonic property and the drugs' neuropharmacological specificity provide a means of studying the neuropharmacology and n...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(92)90060-j

    authors: Koob GF

    更新日期:1992-05-01 00:00:00

  • Involvement of biogenic amines and amino acids in the central regulation of cardiovascular homeostasis.

    abstract::Biogenic amines and amino acids have been implicated in central cardiovascular homeostasis. Initially, drugs were injected into the brain and their effects on blood pressure were investigated. Other approaches allowed endogenous neurotransmitters released in the extracellular space of brain structures involved in card...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:

    authors: Singewald N,Philippu A

    更新日期:1996-10-01 00:00:00

  • Inflammation and neurodegeneration: the story 'retolled'.

    abstract::Toll-like receptors (TLRs) play a crucial role in innate immunity by recognizing conserved motifs predominantly found in microorganisms. Increasing evidence supports a role for TLRs in sterile inflammation as observed in neurodegenerative disorders. This includes work suggesting a contribution for these receptors to t...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2012.07.002

    authors: Drouin-Ouellet J,Cicchetti F

    更新日期:2012-10-01 00:00:00

  • GPCR deorphanizations: the novel, the known and the unexpected transmitters.

    abstract::Pairing orphan G-protein-coupled receptors (GPCRs) to potential ligands found in tissue extracts or in libraries of synthetic compounds has identified an ever-increasing number of transmitters, some of which are novel, some of which were previously known and, more recently, some of which are unexpected. These discover...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2004.11.005

    authors: Civelli O

    更新日期:2005-01-01 00:00:00

  • Receptors coupled to heterotrimeric G proteins of the G12 family.

    abstract::Much regarding the engagement of the G(12) family of heterotrimeric G proteins (G(12) and G(13)) by agonist-activated receptors remains unclear. For example, the identity of receptors that couple unequivocally to G(12) and G(13) and how signals are allocated among these and other G proteins remain open questions. Part...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2005.01.007

    authors: Riobo NA,Manning DR

    更新日期:2005-03-01 00:00:00

  • Novel GPCRs and their endogenous ligands: expanding the boundaries of physiology and pharmacology.

    abstract::Nearly all molecules known to signal cells via G proteins have been assigned a cloned G-protein-coupled-receptor (GPCR) gene. This has been the result of a decade-long genetic search that has also identified some receptors for which ligands are unknown; these receptors are described as orphans (oGPCRs). More than 80 o...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(99)01366-8

    authors: Marchese A,George SR,Kolakowski LF Jr,Lynch KR,O'Dowd BF

    更新日期:1999-09-01 00:00:00

  • The minor binding pocket: a major player in 7TM receptor activation.

    abstract::From the deep part of the main ligand-binding crevice, a minor, often shallower pocket extends between the extracellular ends of transmembrane domains (TM)-I, II, III and VII of 7TM receptors. This minor binding pocket is defined by a highly conserved kink in TM-II that is induced by a proline residue located in one o...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.tips.2010.08.006

    authors: Rosenkilde MM,Benned-Jensen T,Frimurer TM,Schwartz TW

    更新日期:2010-12-01 00:00:00

  • Selective and mixed endothelin receptor antagonism in cardiovascular disease.

    abstract::Within five years of discovering endothelin (ET-1) in 1988, the first report of an orally available ET receptor antagonist was published. Within twelve years, bosentan, the first ET receptor antagonist to gain marketing authorization, was made available for the treatment of pulmonary artery hypertension (PAH). Since t...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2007.10.002

    authors: Dhaun N,Pollock DM,Goddard J,Webb DJ

    更新日期:2007-11-01 00:00:00

  • Protein kinase Calpha: disease regulator and therapeutic target.

    abstract::Protein kinase Calpha (PKCalpha) is a member of the AGC (which includes PKD, PKG and PKC) family of serine/threonine protein kinases that is widely expressed in mammalian tissues. It is closely related in structure, function and regulation to other members of the protein kinase C family, but has specific functions wit...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2009.10.006

    authors: Konopatskaya O,Poole AW

    更新日期:2010-01-01 00:00:00

  • Non-genomic and genomic effects of steroids on neural activity.

    abstract::Steroid hormones are recognized as producing their major long-term effects on cell structure and function via intracellular receptors acting on the expression of genes. There is now increasing evidence that steroids also affect the surface of cells and alter ion permeability, as well as release of neurohormones and ne...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(91)90531-v

    authors: McEwen BS

    更新日期:1991-04-01 00:00:00

  • Do computer simulations of laboratory practicals meet learning needs?

    abstract::There is a variety of pressures on pharmacology teachers to replace real laboratory practicals with simulations but do they help students achieve the required learning objectives? In this article, the marks obtained by students in a variety of assessments using 'wet' or simulated practicals are analysed. Poorer perfor...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01605-9

    authors: Hughes IE

    更新日期:2001-02-01 00:00:00

  • Turning on cGMP-dependent pathways to treat cardiac dysfunctions: boom, bust, and beyond.

    abstract::cGMP inhibits hypertrophy, decreases fibrosis, and protects against cardiac ischemia-reperfusion (I/R) injury. Gene-targeting studies have not defined a clear role for its major downstream effector, cGMP-dependent protein kinase I (cGKI), in cardiac hypertrophy, but do implicate cGMP-cGKI signaling in fibrosis and I/R...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2014.05.003

    authors: Lukowski R,Krieg T,Rybalkin SD,Beavo J,Hofmann F

    更新日期:2014-08-01 00:00:00

  • Prostaglandins and chronic inflammation.

    abstract::Chronic inflammation is the basis of various chronic illnesses including cancer and vascular diseases. However, much has yet to be learned how inflammation becomes chronic. Prostaglandins (PGs) are well established as mediators of acute inflammation, and recent studies in experimental animals have provided evidence th...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2012.02.004

    authors: Aoki T,Narumiya S

    更新日期:2012-06-01 00:00:00

  • Control of transmitter release from the motor nerve by presynaptic nicotinic and muscarinic autoreceptors.

    abstract::Until recently, release studies have failed to indicate the existence of autoreceptors on motor nerves. Ignaz Wessler now reports on a refinement of the technique - the measurement of newly synthesized [3H]acetylcholine released from the phrenic nerve - which provides clear evidence in support of release-modulating au...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(89)90208-3

    authors: Wessler I

    更新日期:1989-03-01 00:00:00

  • Therapeutic approaches to spinal and bulbar muscular atrophy.

    abstract::Spinal and bulbar muscular atrophy is a hereditary motor neuron disease caused by trinucleotide repeat expansion in the androgen receptor gene. The disease mechanism probably involves a toxic gain of function in the mutant protein, because other mutations that cause a loss of androgen receptor function result in a dif...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2010.08.005

    authors: Ranganathan S,Fischbeck KH

    更新日期:2010-11-01 00:00:00

  • Regulation of free calmodulin levels by neuromodulin: neuron growth and regeneration.

    abstract::Neuromodulin is a neurospecific calmodulin binding protein that is implicated in neurite extension, axonal elongation and long-term potentiation. Yuechueng Liu and Daniel Storm propose that neuromodulin binds and concentrates calmodulin on growth cone membranes and that stimulation of protein kinase C releases high lo...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(90)90195-e

    authors: Liu YC,Storm DR

    更新日期:1990-03-01 00:00:00

  • Nicotine addiction: the possible role of functional upregulation.

    abstract::Upregulation of binding to nicotinic acetylcholine receptors (nAChRs) is observed in the brains of both smokers and animals chronically exposed to nicotine, although whether this in vivo change is accompanied by an increase in receptor function is unknown. In vitro recordings indicate that alpha4beta2- and alpha7-subt...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/S0165-6147(00)01979-9

    authors: Buisson B,Bertrand D

    更新日期:2002-03-01 00:00:00

  • A Coordinated Attack: Rett Syndrome Therapeutic Development.

    abstract::Rett syndrome (RTT) is a neurodevelopmental disorder caused by mutations in the Methyl CpG binding protein 2 (MeCP2) gene. This Science & Society article focuses on pharmacological strategies that attack RTT treatment from multiple angles, including drug repurposing and de novo discovery efforts, and discusses the imp...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2019.02.007

    authors: Gogliotti RG,Niswender CM

    更新日期:2019-04-01 00:00:00

  • Sniffing out pharmacology: interactions of drugs with human olfaction.

    abstract::Advances in the understanding of the sense of smell have increased awareness of the role of olfaction in human life. Odors are perceived via specific G protein-coupled receptors (GPCRs) with cAMP as the second messenger. Drugs that interact with this signaling cascade, such as opioids, cannabinoids and sildenafil, are...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2012.01.004

    authors: Lötsch J,Geisslinger G,Hummel T

    更新日期:2012-04-01 00:00:00

  • GABA and its receptors in the spinal cord.

    abstract::The importance of the inhibitory neurotransmitter, GABA, within higher centres of the mammalian brain is unquestionable. However, its role within the spinal cord is of equal significance. There have been numerous studies over the past two decades that have established GABA as a neurotransmitter at both post- and presy...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(96)01013-9

    authors: Malcangio M,Bowery NG

    更新日期:1996-12-01 00:00:00

  • Regulation of mglu(7) receptors by proteins that interact with the intracellular C-terminus.

    abstract::The metabotropic glutamate type 7 (mglu(7)) receptor is a widely distributed, mainly presynaptic Group III mglu receptor that can regulate glutamate release. Recently, largely as a result of the identification of specific proteins that interact with the C-terminal domain of this receptor, considerable progress has bee...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01684-9

    authors: Dev KK,Nakanishi S,Henley JM

    更新日期:2001-07-01 00:00:00

  • Clodronate: A Vesicular ATP Release Blocker.

    abstract::Clodronate is a first-generation bisphosphonate used worldwide for antiresorptive therapy for osteoporosis. Although clodronate is analgesic in nature, its mechanism and efficacy were unknown for some time. Recently, clodronate was identified as a selective and potent inhibitor for vesicular nucleotide transporter (VN...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2017.10.007

    authors: Moriyama Y,Nomura M

    更新日期:2018-01-01 00:00:00