Comparative binding of μ and δ selective ligands in whole brain and pons/medulla homogenates from rat: Affinity profiles of fentanyl derivatives

Yeadon, Michael; Kitchen, Ian

doi:10.1016/0028-3908(88)90141-4

Cited by 52 publications

(20 citation statements)

References 14 publications

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“…Alfentanil is a p-opioid agonist with a p/! selectivity ratio of over 600 in binding studies (Yeadon & Kitchen, 1988) and exhibits a profile in nociceptive tests consistent with p-receptor activation (Niemegeers & Janssen, 1981;Williams et al, 1982). Antinociception induced by alfentanil was blocked by naloxone and only slightly antagonized by naltrindole in doses up to 1 mgkg-' suggesting that naltrindole at these doses, in vivo, has negligible activity at "-receptors.…”

Section: Discussionmentioning

confidence: 84%

Antagonism of swim‐stress‐induced antinociception by the δ‐opioid receptor antagonist naltrindole in adult and young rats

Kitchen

Pinker

1990

British J Pharmacology

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1 The availability of the non-peptide 6-opioid receptor antagonist naltrindole has provided the possibility for in vivo studies on the function of 6-opioid receptors. We have studied the effects of naltrindole on swim-stress-induced antinociception in adult and neonatal rats. 2 Adult, 25 and 20 day old rats were stressed by warm water (20°C) swimming for 3min periods and antinociception was assessed by the tail immersion test (50°C). 3 Naltrindole (0.5 and 1 mgkg 1) antagonized swim-stress-induced antinociception in adult and 25 day old rats but in 20 day old rats naltrindole (1 mg kg-1) was without effect. 4 Antinociception induced by the highly p-opioid receptor selective agonist alfentanil was completely antagonized by naloxone (1 mg kg-1) but virtually unaffected by naltrindole (1 mg kg-'). 5 Neither naloxone nor naltrindole (1 mg kg-1) antagonized swim-stress-induced rises in plasma corticosterone in adult rats at the time of peak antinociception. 6 In conclusion, naltrindole shows in vivo antagonism of opioid-mediated responses. Swim-stressinduced antinociception is mediated through the b-opioid receptor in 25 day old and adult rats and through the p-opioid site in 20 day old animals.

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Section: Discussionmentioning

confidence: 84%

Antagonism of swim‐stress‐induced antinociception by the δ‐opioid receptor antagonist naltrindole in adult and young rats

Kitchen

Pinker

1990

British J Pharmacology

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“…]deltorphin I or II (Erspamer et al, 1989), SNC80 (Bilsky et al, 1995) U69593 (Lahti et al, 1985), CI977 (Hunter et al, 1990), Salvinorin A (Roth et al, 2002) Endomorphin-1 and -2 (Zadina et al, 1997), morphine (Goldstein and Naidu, 1989), DAMGO (Handa et al, 1981), sufentanil (Yeadon and Kitchen, 1988), PL017 (Costa et al, 1992) N/OFQ, N/OFQ-(1-13)-NH 2 (Guerrini et al, 1997), Ro646198 (Jenck et al, 2000), UFP-112 (Rizzi et al, 2007) Selective antagonists Naltrindole (Portoghese et al, 1988), naltriben (Sofuoglu et al, 1991) Nor-binaltorphimine (Portoghese et al, 1987), GNTI (Stevens et al, 2000) CTAP (Pelton et al, 1986) …”

Section: Citation Informationmentioning

confidence: 99%

7TM Receptors

Alexander¹,

Mathie²,

Peters³

2008

British J Pharmacology

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Overview: Alongside the 7-transmembrane receptors listed in the Guide to Receptors and Channels, IUPHAR recognises a number of genes, which sequence analysis suggests code for 7-transmembrane receptors and for which an endogenous ligand has yet to be identified (Foord et al., 2006). Below are listed a number of these genes, for which preliminary evidence for an endogenous ligand has been published. Further Reading Citation InformationWe recommend that any citations to information in the Guide are presented in the following format:Alexander SPH, . Guide to Receptors and Channels (GRAC), 3rd edn. Br J Pharmacol 153 (Suppl. 2): S1-S209. GPR1 ENSG00000183671 GPR3 ENSG00000181773 ACCA GPR4 ENSG00000177464 Proton-sensing, sphingosylphosphorylcholine GPR6 ENSG00000146360 GPR10 ENSG00000119973 GPR12 ENSG00000132975 GPCR21 GPR15 ENSG00000154165 GPR19 ENSG00000183150 GPR20 ENSG00000204882 GPR21 ENSG00000188394 GPR22 ENSG00000172209 GPR25 ENSG00000170128 GPR26 ENSG00000154478 GPR27 ENSG00000170837 SREB1 GPR31 ENSG00000120436 GPR32 ENSG00000142511 GPR33 ENSMUSG00000035148 Pseudogene in man GPR37 ENSG00000170775 PAELR, EDNRLB GPR45 ENSG00000135973 PSP24 GPR48 ENSG00000205213 Leucine-rich repeat-containing G-protein coupled receptor 4 GPR49 ENSG00000139292LGR5, GPR67, FEX, HG38 , MGC117008 GPR50 ENSG00000102195 H9 GPR52 ENSG00000203737 GPR56 ENSG00000205336 TM7LN4, TM7XN1 GPR61 ENSG00000156097 BALGR GPR62 ENSG00000180929 GPR63 ENSG00000112218 PSP24B GPR64 ENSG00000173698 HE6 GPR65 ENSG00000140030 TDAG8 GPR68 ENSG00000119714 OGR1, Proton-sensing GPR70 ENSG00000173662 TAS1R1 GPR71 ENSG00000179002 TAS1R2 GPR72 ENSG00000123901 GPR83 GPR75 ENSG00000119737 WI31133 GPR77 ENSG00000134830 C5L2 GPR78 ENSG00000155269 GPR81 ENSG00000196917 TAGPCR, GPR104 GPR82 ENSG00000171657 GPR84 ENSG00000139572 EX33 GPR85 ENSG00000164604 SREB2 GPR87 ENSG00000138271 GPR95 GPR88 ENSG00000181656 STRG GPR90 ENSMUSG00000059408 Mas-related GPR, member H GPR97 ENSG00000182885 Pb99, PGR26 GPR98 ENSG00000164199 VLGR1 GPR101 ENSG00000165370 GPR107 ENSG00000148358 KIAA1624, RP11-88G17, FLJ20998, LUSTR1 GPR110 ENSG00000153292 hGPCR36, PGR19 GPR111 ENSG00000164393 hGPCR35, PGR20 GPR112 ENSG00000156920 RP1-299I16, PGR17 GPR113 ENSG00000173567 hGPCR37, PGR23 GPR114 ENSG00000159618 PGR27 Symbol Ensembl ID Other names GPR115 ENSG00000153294 FLJ38076, PGR18 GPR116 ENSG00000069122 DKFZp564O1923, KIAA0758 GPR123 ENSG00000197177 KIAA1828 GPR124 ENSG00000020181 Tumour endothelial marker 5 GPR126 ENSG00000112414 FLJ14937 GPR127 ENSG00000186629 PGR16, EMR4 GPR128 ENSG00000144820 FLJ14454 GPR132 ENSG00000183484 G2A GPR133 ENSG00000111452 PGR25 GPR136 ENSG00000124818 OPN5, neuropsin, PGR14 GPR137 ENSG00000173264 GPR137A, TM7SF1L1 GPR139 ENSG00000180269 PGR3 GPR140 ENSG00000172935MRGPRF, GPR168, RTA GPR141 ENSG00000187037 PGR13 GPR142 ENSG00000196169 PGR2, KIF19 GPR143 ENSG00000101850 OA1 GPR144 ENSG00000180264 PGR24 GPR146 ENSG0000016...

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“…Selective agonists DPDPE (Mosberg et al, 1983), DSBULET (Delay-Goyet et al, 1988), [DAla 2 ]deltorphin I or II (Erspamer et al, 1989), SNC80 (Bilsky et al, 1995) U69593 (Lahti et al, 1985), CI977 (Hunter et al, 1990), Salvinorin A (Roth et al, 2002) Endomorphin-1 and 2 (Zadina et al, 1997), morphine (Goldstein and Naidu, 1989), DAMGO (Handa et al, 1981), sufentanil (Yeadon and Kitchen, 1988), PL017 (Costa et al, 1992) N/OFQ, N/OFQ-(1-13)-NH2 (Guerrini et al, 1997), Ro646198 (Jenck et al, 2000), UFP112 (Rizzi et al, 2007) Selective antagonists Naltrindole (Portoghese et al, 1988), naltriben (Sofuoglu et al, 1991) Nor-binaltorphimine (Portoghese et al, 1987), GNTI (Stevens et al, 2000) CTAP (Pelton et al, 1986) J113397 (8. 3, Kawamoto et al, 1999) (Hawkins et al, 1987) [ 3 H]-N/OFQ (Dooley and Houghten, 1996), Subtypes of m (m1, m2), d (d1, d2) and k (k1, k2, k3) receptor have been proposed based primarily on binding studies with poorly selective ligands or results from in vivo studies.…”

Section: Opioid and Opioid-like Bph_501_46 7879mentioning

confidence: 99%

7tm Receptors

2009

British Journal of Pharmacology

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Overview:The completion of the Human Genome Project allowed the identification of a large family of proteins with a common motif of seven groups of 20-24 hydrophobic amino acids arranged as a helices. Approximately 800 of these seven transmembrane (7TM) receptors have been identified of which over 300 are non-olfactory receptors (see Fredriksson et al., 2003; Lagerstrom and Schioth, 2008). Subdivision on the basis of sequence homology allows the definition of rhodopsin, secretin, adhesion, glutamate and Frizzled receptor families. NC-IUPHAR recognizes Classes A, B, and C, which equate to the rhodopsin, secretin and glutamate receptor families.The nomenclature of 7TM receptors is commonly used interchangeably with G protein-coupled receptors, although the former nomenclature allows for signalling of 7TM receptors through pathways not involving G proteins. For example, adiponectin and membrane progestin receptors appear to signal independently of G proteins and appear to reside in membranes in an inverted fashion compared with conventional 7TM receptors. Additionally, the NPR3 natriuretic peptide receptor has a single transmembrane domain structure, but appears to couple to G proteins to generate cellular responses. The 300+ non-olfactory 7TM receptors are the targets for the majority of drugs in clinical usage (Overington et al., 2006), although only a minority of these receptors are exploited therapeutically. Further ReadingFoord SM, Bonner TI, Neubig RR, Rosser EM, Pin JP, Davenport AP et al. (2005) . Preliminary pairingsWhile the remainder of this section focuses on those 7TM receptors for which there is substantial pharmacological information, or interest, listed below are a number of putative 7TM receptors identified by IUPHAR , for which only preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. Gene SymbolEnsembl ID Other names Putative endogenous ligand Comment GPR1 ENSG00000183671 -Appears to act as a co-receptor for HIV (Shimizu et al., 1999) GPR3 ENSG00000181773 ACCA Fails to respond to a variety of lipid-derived agents (Yin et al., 2009) Has been reported to activate adenylyl cyclase constitutively through Gs (Eggerickx et al., 1995). Gene disruption results in premature ovarian aging (Ledent et al., 2005) and reduced b-amyloid deposition (Thathiah et al., 2009) in mice GPR4 ENSG00000177464 Protons (Ludwig et al., 2003; Tobo et al., 2007) An initial report suggesting activation by lysophosphatidylcholine, sphingosylphosphorylcholine (Zhu et al., 2001) has been retracted (Zhu et al., 2005). Gene disruption is associated with increased perinatal mortality and impaired vascular proliferation (Yang et al., 2007 Has also been reported to respond to the phosphodiesterase inhibitor zaprinast (Taniguchi et al., 2006) and the chloride channel blocker 5-nitro-2-(3-phenylpropylamino) benzoic acid (Taniguchi et al., 2008) GPR37 ENSG00000170775 PAELR, EDNRLB Head activator peptide (Rezgaoui et al., 2006) Reported to a...

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Comparative binding of μ and δ selective ligands in whole brain and pons/medulla homogenates from rat: Affinity profiles of fentanyl derivatives

Cited by 52 publications

References 14 publications

Antagonism of swim‐stress‐induced antinociception by the δ‐opioid receptor antagonist naltrindole in adult and young rats

Antagonism of swim‐stress‐induced antinociception by the δ‐opioid receptor antagonist naltrindole in adult and young rats

7TM Receptors

7tm Receptors

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