药物化学词汇表.docx
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药物化学词汇表.docx
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药物化学词汇表
药物化学词汇表
GlossaryofTermsUsedinMedicinalChemistry
(IUPACRecommendations1998)
Activetransport*
Activetransportisthecarriageofasoluteacrossabiologicalmembranefromlowtohighconcentrationthatrequirestheexpenditureof(metabolic)energy.
Address-messageconcept
Address-messageconceptreferstocompoundsinwhichpartofthemoleculeisrequiredforbinding(address)andpartforthebiologicalaction(message).
ADME
AbbreviationforAbsorption,Distribution,Metabolism,Excretion.(SeealsoPharmacokinetics;Drugdisposition).
Affinity
Affinityisthetendencyofamoleculetoassociatewithanother.Theaffinityofadrugisitsabilitytobindtoitsbiologicaltarget(receptor,enzyme,transportsystem,etc.)Forpharmacologicalreceptorsitcanbethoughtofasthefrequencywithwhichthedrug,whenbroughtintotheproximityofareceptorbydiffusion,willresideatapositionofminimumfreeenergywithintheforcefieldofthatreceptor.
Foranagonist(orforanantagonist)thenumericalrepresentationofaffinityisthereciprocaloftheequilibriumdissociationconstantoftheligand-receptorcomplexdenotedKA,calculatedastherateconstantforoffset(k-1)dividedbytherateconstantforonset(k1).
Agonist***
Anagonistisanendogenoussubstanceoradrugthatcaninteractwithareceptorandinitiateaphysiologicalorapharmacologicalresponsecharacteristicofthatreceptor(contraction,relaxation,secretion,enzymeactivation,etc.).
Allostericbindingsites
Allostericbindingsitesarecontainedinmanyenzymesandreceptors.AsaconsequenceofthebindingtoAllostericbindingsites,theinteractionwiththenormalligandmaybeeitherenhancedorreduced.
Allostericenzyme*
Anallostericenzymeisanenzymethatcontainsaregiontowhichsmall,regulatorymolecules("effectors")maybindinadditiontoandseparatefromthesubstratebindingsiteandtherebyaffectthecatalyticactivity.
Onbindingtheeffector,thecatalyticactivityoftheenzymetowardsthesubstratemaybeenhanced,inwhichcasetheeffectorisanactivator,orreduced,inwhichcaseitisade-activatororinhibitor.
Allostericregulation
Allostericregulationistheregulationoftheactivityofallostericenzymes.(SeealsoAllostericbindingsites;Allostericenzymes).
Analog
Ananalogisadrugwhosestructureisrelatedtothatofanotherdrugbutwhosechemicalandbiologicalpropertiesmaybequitedifferent.(SeealsoCongener).
Antagonist***
Anantagonistisadrugoracompoundthatopposesthephysiologicaleffectsofanother.Atthereceptorlevel,itisachemicalentitythatopposesthereceptor-associatedresponsesnormallyinducedbyanotherbioactiveagent.
Antimetabolite***
Anantimetaboliteisastructuralanalogofanintermediate(substrateorcoenzyme)inaphysiologicallyoccurringmetabolicpathwaythatactsbyreplacingthenaturalsubstratethusblockingordivertingthebiosynthesisofphysiologicallyimportantsubstances.
Antisensemolecule
AnantisensemoleculeisanoligonucleotideoranalogthereofthatiscomplementarytoasegmentofRNA(ribonucleicacid)orDNA(deoxyribonucleicacid)andthatbindstoitandinhibitsitsnormalfunction.
Autacoid
Anautacoidisabiologicalsubstancesecretedbyvariouscellswhosephysiologicalactivityisrestrictedtothevicinityofitsrelease;itisoftenreferredtoaslocalhormone.
Autoreceptor
Anautoreceptor,presentatanerveending,isareceptorthatregulates,viapositiveornegativefeedbackprocesses,thesynthesisand/orreleaseofitsownphysiologicalligand.(SeealsoHeteroreceptor).
Bioassay***
Abioassayisaprocedurefordeterminingtheconcentration,purity,and/orbiologicalactivityofasubstance(e.g.,vitamin,hormone,plantgrowthfactor,antibiotic,enzyme)bymeasuringitseffectonanorganism,tissue,cell,enzymeorreceptorpreparationcomparedtoastandardpreparation.
Bioisostere
Abioisostereisacompoundresultingfromtheexchangeofanatomorofagroupofatomswithanother,broadlysimilar,atomorgroupofatoms.Theobjectiveofabioisostericreplacementistocreateanewcompoundwithsimilarbiologicalpropertiestotheparentcompound.Thebioisostericreplacementmaybephysicochemicallyortopologicallybased.(SeealsoIsostere)
Bioprecursorprodrug
Abioprecursorprodrugisaprodrugthatdoesnotimplythelinkagetoacarriergroup,butresultsfromamolecularmodificationoftheactiveprincipleitself.Thismodificationgeneratesanewcompound,abletobetransformedmetabolicallyorchemically,theresultingcompoundbeingtheactiveprinciple.
Biotransformation
Biotransformationisthechemicalconversionofsubstancesbylivingorganismsorenzymepreparations.
CADD
SeeComputer-assisteddrugdesign.
Carrier-linkedprodrug(Carrierprodrug)
Acarrier-linkedprodrugisaprodrugthatcontainsatemporarylinkageofagivenactivesubstancewithatransientcarriergroupthatproducesimprovedphysicochemicalorpharmacokineticpropertiesandthatcanbeeasilyremovedinvivo,usuallybyahydrolyticcleavage.
Cascadeprodrug
Acascadeprodrugisaprodrugforwhichthecleavageofthecarriergroupbecomeseffectiveonlyafterunmaskinganactivatinggroup.
Catabolism***
Catabolismconsistsofreactionsinvolvingendogenousorganicsubstratestoprovidechemicallyavailableenergy(e.g.,ATP)and/ortogeneratemetabolicintermediatesusedinsubsequentanabolicreactions.
Catabolite
Acataboliteisanaturallyoccurringmetabolite.
Clone*
Acloneisapopulationofgeneticallyidenticalcellsproducedfromacommonancestor.Sometimes,"clone"isalsousedforanumberofrecombinantDNA(deoxyribonucleicacid)moleculesallcarryingthesameinsertedsequence.
Codon*
AcodonisthesequenceofthreeconsecutivenucleotidesthatoccursinmRNAwhichdirectstheincorporationofaspecificaminoacidintoaproteinorrepresentsthestartingorterminationsignalsofproteinsynthesis.
Coenzyme
Acoenzymeisadissociable,low-molecularweight,non-proteinaceousorganiccompound(oftennucleotide)participatinginenzymaticreactionsasacceptorordonorofchemicalgroupsorelectrons.
Combinatorialsynthesis
Combinatorialsynthesisisaprocesstopreparelargesetsoforganiccompoundsbycombiningsetsofbuildingblocks.
Combinatoriallibrary
Acombinatoriallibraryisasetofcompoundspreparedbycombinatorialsynthesis.
CoMFA
SeeComparativeMolecularFieldAnalysis.
ComparativeMolecularFieldAnalysis(CoMFA)**
Comparativemolecularfieldanalysis(CoMFA)isa3D-QSARmethodthatusesstatisticalcorrelationtechniquesfortheanalysisofthequantitativerelationshipbetweenthebiologicalactivityofasetofcompoundswithaspecifiedalignment,andtheirthree-dimensionalelectronicandstericproperties.Otherpropertiessuchashydrophobicityandhydrogenbondingcanalsobeincorporatedintotheanalysis.(SeealsoThree-dimensionalQuantitativeStructure-ActivityRelationship[3D-QSAR]).
Computationalchemistry**
Computationalchemistryisadisciplineusingmathematicalmethodsforthecalculationofmolecularpropertiesorforthesimulationofmolecularbehaviour.
Computer-assisteddrugdesign(CADD)**
Computer-assisteddrugdesigninvolvesallcomputer-assistedtechniquesusedtodiscover,designandoptimizebiologicallyactivecompoundswithaputativeuseasdrugs.
Congener***
Acongenerisasubstanceliterallycon-(with)generatedorsynthesizedbyessentiallythesamesyntheticchemicalreactionsandthesameprocedures.Analogsaresubstancesthatareanalogousinsomerespecttotheprototypeagentinchemicalstructure.
Clearlycongenersmaybeanalogsorviceversabutnotnecessarily.Thetermcongener,whilemostoftenasynonymforhomologue,hasbecomesomewhatmorediffuseinmeaningsothatthetermscongenerandanalogarefrequentlyusedinterchangeablyintheliterature.
Cooperativity
Cooperativityistheinteractionprocessbywhichbindingofaligandtoonesiteonamacromolecule(enzyme,receptor,etc.)influencesbindingatasecondsite,e.g.betweenthesubstratebindingsitesofanallostericenzyme.Cooperativeenzymestypicallydisplayasigmoid(S-shaped)plotofthereactionrateagainstsubstrateconcentration.(SeealsoAllostericbindingsites).
3D-QSAR
SeeThree-dimensionalQuantitativeStructure-ActivityRelationship.
Denovodesign**
Denovodesignisthedesignofbioactivecompoundsbyincrementalconstructionofaligandmodelwithinamodelofthereceptororenzymeactivesite,thestructureofwhichisknownfromX-rayornuclearmagneticresonance(NMR)data.
Disposition
SeeDrugdisposition.
Distomer
Adistomeristheenantiomerofachiralcompoundthatisthelesspotentforaparticularaction.Thisdefinitiondoesnotexcudethepossibilityofothereffectorsideeffectofthedistomer(SeealsoEutomer).
Dockingstudies
Dockingstudiesaremolecularmodelingstudiesaimingatfindingaproperfitbetweenaligandanditsbindingsite.
Double-blindstudy
Adouble-blindstudyisaclinicalstudyofpotentialandmarketeddrugs,whereneithertheinvestigatorsnorthesubjectsknowwhichsubjectswillbetreatedwiththeactiveprincipleandwhichoneswillreceiveaplacebo.
Doubleprodrug(orpro-prodrug)
Adoubleprodrugisabiologicallyinactivemoleculewhichistransformedinvivointwosteps(enzymaticallyand/orchemically)totheactivespecies.
Drug***
Adrugisanysubstancepresentedfortreating,curingorpreventingdiseaseinhumanbeingsorinanimals.Adrugmayalsobeusedformakingamedicaldiagnosisorforrestoring,correcting,ormodifyingphysiologicalfunctions
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