Functional assays are available for the following receptors:

Not available ***;     h:human, m:mouse, r:rat, rab:rabbit
RECEPTOR/
TRANSPORTER
RECEPTOR/
TRANSPORTER
RECEPTOR/
TRANSPORTER
h 5-HT1A h D1* h m1-muscarinic
h 5-HT1B h D2 h m2-muscarinic
h 5-HT1D r D3 h m3-muscarinic
h 5-HT1E* r D4 h m4-muscarinic
h 5-HT1F* h D5* h m5-muscarinic
h 5-HT2A h EDG02 h NK-1
r 5-HT2A h EDG03 h NK-2*
h 5-HT2B h Endothelial differentiation,lysophosphatidic acid,EDG4 h NK-3*
h 5-HT2C-INI h EDG05 h neuropeptide Y receptor Y1*
h 5-HT2C-VGI h EDG06 h neuropeptide Y receptor Y2*
h 5-HT3 h EDG07 h NPYR4
h 5-HT4* h EDG08 h NPYR5
h 5-HT5A h EDNRA h NMUR1
h 5-HT6 h EDNRB h NMUR2
h 5-HT7A h EDNRBL h NTII neurotensin receptor
h 5-HT7B h EMR1 h orexin 2 receptor
a1A-adrenergic h EMR2 m d-opiate
a1B-adrenergic h EMR3 h d-opiate
a1D-adrenergic h FPR01 h k-opiate*
a2A-adrenergic h FPRL1 m m-opiate
a2B-adrenergic h FPRL2 h P2RY1
a2C-adrenergic h FSK80 h P2RY11
h b1-adrenergic* h GCGR h P2RY12
h b2-adrenergic* h GHRHR h P2RY2
h b3-adrenergic* h GIPR h P2RY4
h ADCYAP1R h GLP1R h P2RY6
h Adenosine A2B h GLP2R h PNR
h ADORA1 h GLUH1 rab Prostaglandin E receptor 2, (subtype EP2)
h ADORA2A h glutamate Receptor NR1 rab Prostaglandin E receptor 4, (subtype EP4)
h ADORA2B h glutamate receptor NR2B h PTGIR Prostaglandin I2 (prostacyclin) receptor
h ADORA3 h GPR115 h Oxytocin
h BDKRB1 bradykinin h GPR123 h PTHR1
h BDKRB2 bradykinin h GPR125 h PTHR2
h BPZP h GPR128 h SALPR
h C3AR1 complement component 3A h GPR133 h SCTR
h C5L2 h GPR157 h SSTR1
h C5R01 h GPR21 h SSTR2
h CALCR h GPR26 h SSTR3
h CB2 cannabinoid h GPR40 h SSTR4
h CCBP2 h GPR41 h SSTR5
h CCR01 h GPR43 h TA1 trace amine receptor
h CCR02 h GPR45 h TA3 - trace amine
h CCR03 h GPR58 h TA4 trace amine receptor
h CCR04 h GPR61 h TA5 trace amine receptor
h CCR05 h GPR62 h TM7SF1
h CCR06 h HAMEP1 h UROII urotensin receptor
h CCR07 h H1 Histamine r vanilloid receptor
h CCR08 h H2 Histamine V1-vasopressin
h CCR09 h HTR3 V2-vasopressin
h CCR10 h H4 histamine V3-vasopressin
h CCRL1 h LTB4R h VIPR2
h CCRL2 h LTB4R2 h VMAT1 ***
h CLR01 Cysteinyl leukotriene receptor 1 h MASS1 h VMAT2 ***
h CLR02 h MC1 melanocortin receptor h XCR01
h CMKL1 h MC2 melanocortin receptor  
h CMKL2 h MC3 melanocortin receptor 5-HT transporter
h CRHR1 h MC4 melanocortin receptor DA transporter
h CRHR2 h MC5 melanocortin receptor NE transporter
h CX3R1 h melanin concentrating hormone receptor 1  
h CXCR1 h melanin concentrating hormone receptor 2 HERG
h CXCR2 h mGluR4 metabotropic glutamate receptor MDR-1
h CXCR3 r mGluR4 metabotropic glutamate receptor  
h CXCR4 h mGluR5 metabotropic glutamate receptor  
h CXCR5 r mGluR5 metabotropic glutamate receptor  
h CXCR6 r mGluR7 metabotropic glutamate receptor  
  h motilin receptor/GPR38/ghrelin receptor  
  • We will offer primary functional assays (Ca++ flux, GTPgS, cAMP formation. ERK phosphorylation). Ca++ flux assays are performed using a FLIPRTETRA while other assays are performed using scintillation proximity or fluorescent-based assays.
  • We will soon have the capacity to determine arrestin-translocation, receptor internalization and signal transduction pathways in the 384- and 96-well formats using a BD Platform 855 HCS system.
  • We will offer secondary functional assays to assess agonist potencies and efficacies. Assay characteristics: assays are done in 348- or 96-well formats.
  • For some Gi- and Gs-linked receptors, Gq-i5/Gs-i5 chimeric G proteins may be co-transfected and [3H]-IP release and/or Ca++ release quantified.
  • For Gq-linked receptors, [3H]-IP release and Ca++ release can be quantified. Kact (Kactivation) and %Vmax relative to a full agonist values are calculated
  • For compounds which do not demonstrate activation, antagonist properties can be determined using Schild analysis.

How to request a functional assay?

  • To request services from the PDSP you must submit an assay request. Requests are processed by the PDSP Online Database. To create an assay request you first need to be registered as an Investigator. Please use the following tutorial which will help you create an account and submit an assay request: PDSP Assay Request Tutorial. If you already have a PDSP account simply login and initiate a new request.