Inverse agonism at G protein‐coupled receptors: (patho)physiological relevance and implications for drug discovery

Inverse agonism at G protein‐coupled receptors: (patho)physiological relevance and implications... Abbreviations: Ado adenosine AM630 6‐iodopravadoline AR adrenoceptor BK bradykinin CAM constitutively active mutant CB cannabinoid CHO Chinese hamster ovary COS African green monkey kidney fibroblast‐like cell line CP‐55940 (−)‐3‐[2‐hydroxy‐4‐(1,1‐dimethylhyptyl)phenyl]‐4(3‐hydroxypropyl)cyclohexan‐1‐ol CT calcitonin 5‐CT 5‐carboxamidotryptamine D dopamine DMCM methyl 6,7‐dimethoxy‐4‐ethyl‐β‐carboline‐e‐carboxylate DOI (±)‐1‐(2,5‐dimethoxy‐4‐iodophenyl)‐2‐aminopropane DPCPX 1,3‐DiPropyl‐8‐cyclopentyladenosine F314 [Mpa, D‐Tyr(Ethyl),Thr, Orn]‐oxytocin FMLP N ‐formyl‐ L ‐methionyl‐ L ‐leucyl‐ L ‐phenylalanine FP formyl peptide FSH follicle‐stimulating hormone GLP‐1 glucagon‐like peptide‐1 GPCR G protein‐coupled receptor GTP guanosine‐5′‐triPhosphate GTPase guanosine‐5′‐triphosphatase [ 35 S]‐GTPγS ‐[ 35 S] guanosine 5′‐ 0 ‐(thiotriphosphate) H histamine HEK293 human embryonic kidney H.E.L. 92.1.17 human erythroleukemia HL‐60 human leukemia I Ca L‐type calcium currents ICI‐118,551 (±)‐1‐(2,3‐[dihydro‐7‐methyl‐1 H ‐inden‐4‐yl]oxy)‐3‐([1‐methylethyl]‐amino)‐2‐butanol ICI‐174,864 N ‐ N ‐diallyl‐Tyr‐Aib‐Aib‐Phe‐Thr IP inositol phosphates IP‐10 interferon‐γ‐inducible protein 10 LH luteinizing hormone M muscarinic MAPK mitogen‐activated protein kinase MC melanocortin Mig monokine induced by interferon‐γ α‐MSH melanocyte stimulating hormone NG108‐15 neuroblastoma X glioma hybrid O opioid P purinergic PTH parathyroid hormone PTHrP parathyroid hormone‐related peptide QNB R (−)‐quinuclidinylbenzilate RIN5AH rat insulinoma‐derived Sf9 Spodoptera frugiperda 9 SB206553 N ‐3‐pyridinyl‐3,5‐dihydro‐5‐methylbenzo[1,2‐b:4,5‐b′]dipyrrole‐1(2H)‐carboxamide hydrochloride SDF‐1α stromal cell‐derived factor 1α SR141,716A N ‐(piperidino‐1‐yl)‐5‐(4‐chlorophenyl)‐1‐(2,4‐dichlorophenyl)‐4‐methyl‐pyrazole‐3‐carboxamide SR144,528 N ‐([1s]‐endo‐1,3,3‐trimethylbicyclo[2.2.1]heptan‐2‐yl)‐5‐(4‐chloro‐3‐methylphenyl)‐1‐(4‐methylbenzyl)‐pyrazole‐3‐carboxamide vMIP‐II viral macrophage inflammatory protein‐II WAY100,635 N‐{2‐[4‐(2‐methoxyphenyl)‐1‐piperazinyl]ethyl}‐N‐(2‐pyridinyl)‐cyclohexane‐carboxamide WIN55,212‐2 R(+)‐[2,3‐dihydro‐5‐methyl‐3‐[(morpholinyl)methyl]pyrrolo[1,2,3‐ de ]‐1,4‐benzoxazin‐yl]‐(1‐napthalenyl)methanone mesylate WB4101 2‐(2,6‐dimethoxyphenoxyethyl)aminomethyl‐1,4‐benzodioxane XAC xanthin amino congener Introduction The largest http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png British Journal of Pharmacology Wiley

Inverse agonism at G protein‐coupled receptors: (patho)physiological relevance and implications for drug discovery

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Publisher
Wiley
Copyright
2000 Nature Publishing Group
ISSN
0007-1188
eISSN
1476-5381
DOI
10.1038/sj.bjp.0703311
pmid
10780991
Publisher site
See Article on Publisher Site

Abstract

Abbreviations: Ado adenosine AM630 6‐iodopravadoline AR adrenoceptor BK bradykinin CAM constitutively active mutant CB cannabinoid CHO Chinese hamster ovary COS African green monkey kidney fibroblast‐like cell line CP‐55940 (−)‐3‐[2‐hydroxy‐4‐(1,1‐dimethylhyptyl)phenyl]‐4(3‐hydroxypropyl)cyclohexan‐1‐ol CT calcitonin 5‐CT 5‐carboxamidotryptamine D dopamine DMCM methyl 6,7‐dimethoxy‐4‐ethyl‐β‐carboline‐e‐carboxylate DOI (±)‐1‐(2,5‐dimethoxy‐4‐iodophenyl)‐2‐aminopropane DPCPX 1,3‐DiPropyl‐8‐cyclopentyladenosine F314 [Mpa, D‐Tyr(Ethyl),Thr, Orn]‐oxytocin FMLP N ‐formyl‐ L ‐methionyl‐ L ‐leucyl‐ L ‐phenylalanine FP formyl peptide FSH follicle‐stimulating hormone GLP‐1 glucagon‐like peptide‐1 GPCR G protein‐coupled receptor GTP guanosine‐5′‐triPhosphate GTPase guanosine‐5′‐triphosphatase [ 35 S]‐GTPγS ‐[ 35 S] guanosine 5′‐ 0 ‐(thiotriphosphate) H histamine HEK293 human embryonic kidney H.E.L. 92.1.17 human erythroleukemia HL‐60 human leukemia I Ca L‐type calcium currents ICI‐118,551 (±)‐1‐(2,3‐[dihydro‐7‐methyl‐1 H ‐inden‐4‐yl]oxy)‐3‐([1‐methylethyl]‐amino)‐2‐butanol ICI‐174,864 N ‐ N ‐diallyl‐Tyr‐Aib‐Aib‐Phe‐Thr IP inositol phosphates IP‐10 interferon‐γ‐inducible protein 10 LH luteinizing hormone M muscarinic MAPK mitogen‐activated protein kinase MC melanocortin Mig monokine induced by interferon‐γ α‐MSH melanocyte stimulating hormone NG108‐15 neuroblastoma X glioma hybrid O opioid P purinergic PTH parathyroid hormone PTHrP parathyroid hormone‐related peptide QNB R (−)‐quinuclidinylbenzilate RIN5AH rat insulinoma‐derived Sf9 Spodoptera frugiperda 9 SB206553 N ‐3‐pyridinyl‐3,5‐dihydro‐5‐methylbenzo[1,2‐b:4,5‐b′]dipyrrole‐1(2H)‐carboxamide hydrochloride SDF‐1α stromal cell‐derived factor 1α SR141,716A N ‐(piperidino‐1‐yl)‐5‐(4‐chlorophenyl)‐1‐(2,4‐dichlorophenyl)‐4‐methyl‐pyrazole‐3‐carboxamide SR144,528 N ‐([1s]‐endo‐1,3,3‐trimethylbicyclo[2.2.1]heptan‐2‐yl)‐5‐(4‐chloro‐3‐methylphenyl)‐1‐(4‐methylbenzyl)‐pyrazole‐3‐carboxamide vMIP‐II viral macrophage inflammatory protein‐II WAY100,635 N‐{2‐[4‐(2‐methoxyphenyl)‐1‐piperazinyl]ethyl}‐N‐(2‐pyridinyl)‐cyclohexane‐carboxamide WIN55,212‐2 R(+)‐[2,3‐dihydro‐5‐methyl‐3‐[(morpholinyl)methyl]pyrrolo[1,2,3‐ de ]‐1,4‐benzoxazin‐yl]‐(1‐napthalenyl)methanone mesylate WB4101 2‐(2,6‐dimethoxyphenoxyethyl)aminomethyl‐1,4‐benzodioxane XAC xanthin amino congener Introduction The largest

Journal

British Journal of PharmacologyWiley

Published: May 1, 2000

References

  • Histamine H 1 ‐receptor binding sites in guinea pig brain membranes: regulation of agonist interactions by guanine nucleotides and cations
    CHANG, CHANG; SYNDER, SYNDER
  • High prevalence of antibodies against beta 1‐ and beta 2‐adrenoceptors in patients with primary electrical cardiac abnormalities
    CHIALE, CHIALE; ROSENBAUM, ROSENBAUM; ELIZARI, ELIZARI; HJALMARSON, HJALMARSON; MAGNUSSON, MAGNUSSON; WALLUKAT, WALLUKAT; HOEBEKE, HOEBEKE
  • Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB 1 and CB 2 receptors
    MACLENNAN, MACLENNAN; REYNEN, REYNEN; KWAN, KWAN; BONHAUS, BONHAUS
  • Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with beta2‐adrenoceptor activation
    NAGARAJA, NAGARAJA; IYER, IYER; LIU, LIU; EICHBERG, EICHBERG; BOND, BOND
  • Inhibition of the constitutive activity of human 5‐HT 1A receptors by the inverse agonist, spiperone but not the neutral antagonist, WAY 100,635
    NEWMAN‐TANCREDI, NEWMAN‐TANCREDI; CONTE, CONTE; CHAPUT, CHAPUT; SPEDDING, SPEDDING; MILLAN, MILLAN
  • Functional evidence of inverse agonism in vascular smooth muscle
    NOGUERA, NOGUERA; IVORRA, IVORRA; D'OCON, D'OCON
  • SR 141716A, a cannabinoid receptor antagonist, produces hyperalgesia in untreated mice
    RICHARDSON, RICHARDSON; AANONSEN, AANONSEN; HARGREAVES, HARGREAVES
  • Defects in G protein‐coupled signal transduction in human disease
    SPIEGEL, SPIEGEL
  • A 1 adenosine receptor‐G protein coupling in bovine brain membranes: effects of guanine nucleotides, salt, and solubilization
    STILES, STILES

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