Actions

::RTI-55

::concepts



{{#invoke:Infobox|infobox}}{{#invoke:TemplatePar |check |template=Template:Infobox_drug |all= |opt= pronounce= ATC_prefix= ATC_suffix= ATC_supplemental= ATCvet= CAS_number_Ref= CAS_number= CAS_supplemental= ChEBI= ChEBI_Ref= ChEMBL_Ref= ChEMBL= ChemSpiderID= ChemSpiderID_Ref= ChemSpiderID= DailyMedID= data_page= DrugBank_Ref= DrugBank= Drugs.com= duration_of_action= IUPAC_name= IUPHAR_ligand= KEGG_Ref= KEGG= MedlinePlus= NIAID_ChemDB= PDB_ligand= PubChemSubstance= PubChem= StdInChIKey_Ref= StdInChIKey_comment= StdInChIKey= StdInChI_Ref= StdInChI_comment= StdInChI= UNII_Ref= UNII= Verifiedfields= Watchedfields= addiction_liability= alt2= altL= altR= alt= bioavailability= boiling_high= boiling_notes= boiling_point= captionLR= caption= charge= chemical_formula= chemical_formula_ref= chemical_formula_comment= class1= class2= class3= class4= component1= component2= component3= component4= density= dependency_liability= drug_name= elimination_half-life= excretion= InChI= InChIKey= image2= imageL= imageR= imagename= image= legal_AU= legal_CA= legal_DE= legal_EU= legal_NZ= legal_UK= legal_UN= legal_US= legal_AU_comment= legal_CA_comment= legal_DE_comment= legal_UK_comment= legal_NZ_comment= legal_US_comment= legal_UN_comment= legal_EU_comment= legal_status= licence_EU= licence_US= mab_type= melting_high= melting_notes= melting_point= metabolism= metabolites= molecular_weight= molecular_weight_round= molecular_weight_unit= molecular_weight_ref= molecular_weight_comment= onset= pregnancy_AU= pregnancy_US= pregnancy_AU_comment= pregnancy_US_comment= pregnancy_category= protein_bound= routes_of_administration= sec_combustion= SMILES= smiles= solubility= source= specific_rotation= synonyms= target= tradename= type= vaccine_type= verifiedrevid= width2= widthL= widthR= width= Ac=Ag=Al=Am=Ar=As=At=Au=B=Ba=Be=Bh=Bi=Bk=Br=C=Ca=Cd=Ce=Cf=Cl=Cm=Cn=Co=Cr=Cs=Cu= Db=Ds=Dy=Er=Es=Eu=F=Fe=Fl=Fm=Fr=Ga=Gd=Ge=H=He=Hf=Hg=Ho=Hs=I=In=Ir=K=Kr=La=Li=Lr=Lu=Lv= Md=Mg=Mn=Mo=Mt=N=Na=Nb=Nd=Ne=Ni=No=Np=O=Os=P=Pa=Pb=Pd=Pm=Po=Pr=Pt=Pu=Ra=Rb=Re=Rf=Rg=Rh=Rn=Ru= S=Sb=Sc=Se=Sg=Si=Sm=Sn=Sr=Ta=Tb=Tc=Te=Th=Ti=Tl=Tm=U=Uuo=Uup=Uus=Uut=V=W=Xe=Y=Yb=Zn=Zr |cat=Chemical articles with unknown parameter in Infobox drug |format=0|preview=1|errNS=0 }}

RTI-55 (iometopane) is a phenyltropane-based psychostimulant used in scientific research and with some medical application/s. This drug was first cited in 1991.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> RTI-55 is a non-selective dopamine reuptake inhibitor derived from methylecgonidine. However, more selective analogs are derived by conversion to "pyrrolidinoamido" RTI-229, for instance. Due to the large bulbous nature of the weakly electron withdrawing iodo halogen atom, RTI-55 is the most strongly serotonergic of the simple para-substituted troparil based analogs.<ref name=FIC/> In rodents RTI-55 actually caused death at a dosage of 100 mg/kg, whereas RTI-51 and RTI-31 did not.<ref name=FIC>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> Another notable observation is the strong propensity of RTI-55 to cause locomotor activity enhancements,<ref name=FIC/> although in an earlier study, RTI-51 was actually even stronger than RTI-55 in shifting baseline LMA.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> This observation serves to highlight the disparities that can arise between studies.

RTI-55 is one of the most potent phenyltropane stimulants commercially available, which limits its use in humans, as it might have significant abuse potential if used outside a strictly controlled medical setting.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> However, it is definitely worthy of mentioning that increasing the size of the halogen atom attached to troparil serves to reduce the number of lever responses in a session when these analogs were compared in a study.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> Although RTI-55 wasn't specifically examined in this study the number of lever responses in a given session was of the order cocaine > WIN35428 > RTI-31 > RTI-51.

In contrast to RTI-31 which is predominantly dopaminergic, increasing the size of the covalently bonded halogen from a chlorine to an iodine markedly increases the affinity for the SERT, while retaining mostly all of its DAT blocking activity.

If desired, a radioactive source of iodine can be utilized.

I123 and I125 in particular because these are very high energy γ-ray emitters.

Compared to the "WIN" compounds, extremely low Ki values are attainable.


RTI-55 sections
Intro   Uses   Chemistry  See also   References   

PREVIOUS: IntroNEXT: Uses
<<>>

First::journal    Pages::title    Volume::issue    Dopamine::category    Carroll::legal    Number::reuptake

{{#invoke:Infobox|infobox}}{{#invoke:TemplatePar |check |template=Template:Infobox_drug |all= |opt= pronounce= ATC_prefix= ATC_suffix= ATC_supplemental= ATCvet= CAS_number_Ref= CAS_number= CAS_supplemental= ChEBI= ChEBI_Ref= ChEMBL_Ref= ChEMBL= ChemSpiderID= ChemSpiderID_Ref= ChemSpiderID= DailyMedID= data_page= DrugBank_Ref= DrugBank= Drugs.com= duration_of_action= IUPAC_name= IUPHAR_ligand= KEGG_Ref= KEGG= MedlinePlus= NIAID_ChemDB= PDB_ligand= PubChemSubstance= PubChem= StdInChIKey_Ref= StdInChIKey_comment= StdInChIKey= StdInChI_Ref= StdInChI_comment= StdInChI= UNII_Ref= UNII= Verifiedfields= Watchedfields= addiction_liability= alt2= altL= altR= alt= bioavailability= boiling_high= boiling_notes= boiling_point= captionLR= caption= charge= chemical_formula= chemical_formula_ref= chemical_formula_comment= class1= class2= class3= class4= component1= component2= component3= component4= density= dependency_liability= drug_name= elimination_half-life= excretion= InChI= InChIKey= image2= imageL= imageR= imagename= image= legal_AU= legal_CA= legal_DE= legal_EU= legal_NZ= legal_UK= legal_UN= legal_US= legal_AU_comment= legal_CA_comment= legal_DE_comment= legal_UK_comment= legal_NZ_comment= legal_US_comment= legal_UN_comment= legal_EU_comment= legal_status= licence_EU= licence_US= mab_type= melting_high= melting_notes= melting_point= metabolism= metabolites= molecular_weight= molecular_weight_round= molecular_weight_unit= molecular_weight_ref= molecular_weight_comment= onset= pregnancy_AU= pregnancy_US= pregnancy_AU_comment= pregnancy_US_comment= pregnancy_category= protein_bound= routes_of_administration= sec_combustion= SMILES= smiles= solubility= source= specific_rotation= synonyms= target= tradename= type= vaccine_type= verifiedrevid= width2= widthL= widthR= width= Ac=Ag=Al=Am=Ar=As=At=Au=B=Ba=Be=Bh=Bi=Bk=Br=C=Ca=Cd=Ce=Cf=Cl=Cm=Cn=Co=Cr=Cs=Cu= Db=Ds=Dy=Er=Es=Eu=F=Fe=Fl=Fm=Fr=Ga=Gd=Ge=H=He=Hf=Hg=Ho=Hs=I=In=Ir=K=Kr=La=Li=Lr=Lu=Lv= Md=Mg=Mn=Mo=Mt=N=Na=Nb=Nd=Ne=Ni=No=Np=O=Os=P=Pa=Pb=Pd=Pm=Po=Pr=Pt=Pu=Ra=Rb=Re=Rf=Rg=Rh=Rn=Ru= S=Sb=Sc=Se=Sg=Si=Sm=Sn=Sr=Ta=Tb=Tc=Te=Th=Ti=Tl=Tm=U=Uuo=Uup=Uus=Uut=V=W=Xe=Y=Yb=Zn=Zr |cat=Chemical articles with unknown parameter in Infobox drug |format=0|preview=1|errNS=0 }}

RTI-55 (iometopane) is a phenyltropane-based psychostimulant used in scientific research and with some medical application/s. This drug was first cited in 1991.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> RTI-55 is a non-selective dopamine reuptake inhibitor derived from methylecgonidine. However, more selective analogs are derived by conversion to "pyrrolidinoamido" RTI-229, for instance. Due to the large bulbous nature of the weakly electron withdrawing iodo halogen atom, RTI-55 is the most strongly serotonergic of the simple para-substituted troparil based analogs.<ref name=FIC/> In rodents RTI-55 actually caused death at a dosage of 100 mg/kg, whereas RTI-51 and RTI-31 did not.<ref name=FIC>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> Another notable observation is the strong propensity of RTI-55 to cause locomotor activity enhancements,<ref name=FIC/> although in an earlier study, RTI-51 was actually even stronger than RTI-55 in shifting baseline LMA.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> This observation serves to highlight the disparities that can arise between studies.

RTI-55 is one of the most potent phenyltropane stimulants commercially available, which limits its use in humans, as it might have significant abuse potential if used outside a strictly controlled medical setting.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> However, it is definitely worthy of mentioning that increasing the size of the halogen atom attached to troparil serves to reduce the number of lever responses in a session when these analogs were compared in a study.<ref>{{#invoke:Citation/CS1|citation |CitationClass=journal }}</ref> Although RTI-55 wasn't specifically examined in this study the number of lever responses in a given session was of the order cocaine > WIN35428 > RTI-31 > RTI-51.

In contrast to RTI-31 which is predominantly dopaminergic, increasing the size of the covalently bonded halogen from a chlorine to an iodine markedly increases the affinity for the SERT, while retaining mostly all of its DAT blocking activity.

If desired, a radioactive source of iodine can be utilized.

I123 and I125 in particular because these are very high energy γ-ray emitters.

Compared to the "WIN" compounds, extremely low Ki values are attainable.


RTI-55 sections
Intro   Uses   Chemistry  See also   References   

PREVIOUS: IntroNEXT: Uses
<<>>