Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T01777
|
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Former ID |
TTDR01180
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Target Name |
Alpha-2C adrenergic receptor
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Gene Name |
ADRA2C
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Synonyms |
Alpha-2C adrenoceptor; Alpha-2C adrenoreceptor; Subtype C4; ADRA2C
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Target Type |
Successful
|
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Disease | Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | ||||
Alcohol use disorders [ICD9: 303; ICD10: F10.2] | |||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Asthma [ICD10: J45] | |||||
Contusion [ICD10: S36.220S] | |||||
Depression [ICD9: 311; ICD10: F30-F39] | |||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Dementia; Obesity [ICD9:290-294, 278; ICD10: F01-F07, E66] | |||||
Diabetic nephropathy; Fibromyalgia [ICD9:250.4, 729.1; ICD10: E11.21, M79.7] | |||||
Erythema [ICD9: 695; ICD10: L51-L54] | |||||
Fibromyalgia [ICD9: 729.1; ICD10: M79.7] | |||||
Glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Hypotension [ICD9: 458, 796.3; ICD10: I95] | |||||
Heart arrhythmia [ICD10: I47-I49] | |||||
Heart failure [ICD9: 428; ICD10: I50] | |||||
Male sexual disorders [ICD10: F52] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Ocular disease [ICD10: H00-H59] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Ocular hypertension [ICD9: 365.04; ICD10: H40.0] | |||||
Prostate disease [ICD10: N42.9] | |||||
Poison intoxication [ICD10: T36-T50] | |||||
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Sexual dysfunction [ICD9: 302.7; ICD10: F52] | |||||
Function |
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins.
|
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BioChemical Class |
GPCR rhodopsin
|
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Target Validation |
T01777
|
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UniProt ID | |||||
Sequence |
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGF
LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA VISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR TRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGA LRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRR RRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFK FFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ |
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Structure |
1HLL; 1HO9; 1HOD; 1HOF
|
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Drugs and Mode of Action | |||||
Drug(s) | Amezinium | Drug Info | Approved | Hypotension | [1] |
Amosulalol | Drug Info | Approved | Hypertension | [2] | |
Brimonidine | Drug Info | Approved | Ocular hypertension | [3], [4] | |
Dihydroergocristine | Drug Info | Approved | Alcohol use disorders | [5], [6] | |
MOXONIDINE | Drug Info | Approved | Alcohol use disorders | [7] | |
Propylhexedrine | Drug Info | Approved | Obesity | [1] | |
Rilmenidine | Drug Info | Approved | Hypertension | [1] | |
Tetrahydrozoline | Drug Info | Approved | Ocular disease | [8] | |
Xylometazoline | Drug Info | Phase 4 | Allergic rhinitis | [9], [10] | |
IDAZOXAN HYDROCHLORIDE | Drug Info | Phase 3 | Neurological disease | [11] | |
TNX-102 | Drug Info | Phase 3 | Fibromyalgia | [12] | |
AGN-XX/YY | Drug Info | Phase 2 | Diabetic nephropathy; Fibromyalgia | [13] | |
MEDETOMIDINE | Drug Info | Phase 2 | Pain | [14] | |
ORM-12741 | Drug Info | Phase 2 | Alzheimer disease | [15] | |
V-101 | Drug Info | Phase 2 | Erythema | [16] | |
INDORAMIN | Drug Info | Withdrawn from market | Hypertension | [17], [1] | |
Ecabapide | Drug Info | Discontinued in Preregistration | Peptic ulcer | [18] | |
Delequamine hydrochloride | Drug Info | Discontinued in Phase 3 | Male sexual disorders | [19] | |
FLUPAROXAN | Drug Info | Discontinued in Phase 3 | Depression | [20], [21] | |
NOLOMIROLE HYDROCHLORIDE | Drug Info | Discontinued in Phase 3 | Heart failure | [22] | |
Deriglidole | Drug Info | Discontinued in Phase 2 | Diabetes | [23] | |
Fadolmidine | Drug Info | Discontinued in Phase 2 | Pain | [24] | |
GYKI-16084 | Drug Info | Discontinued in Phase 2 | Prostate disease | [25] | |
JTH-601 | Drug Info | Discontinued in Phase 2 | Prostate disease | [26] | |
MAZAPERTINE | Drug Info | Discontinued in Phase 2 | Discovery agent | [27] | |
MK-912 | Drug Info | Discontinued in Phase 2 | Discovery agent | [28] | |
NMI-870 | Drug Info | Discontinued in Phase 2 | Sexual dysfunction | [29] | |
SGB-1534 | Drug Info | Discontinued in Phase 2 | Hypotension | [30] | |
GYKI-12743 | Drug Info | Discontinued in Phase 1 | Hypertension | [31] | |
A-75169 | Drug Info | Terminated | Glaucoma | [32] | |
A-80426 | Drug Info | Terminated | Discovery agent | [33] | |
ARC239 | Drug Info | Terminated | Discovery agent | [34], [35] | |
F-14413 | Drug Info | Terminated | Alzheimer disease | [36] | |
Midaglizole | Drug Info | Terminated | Asthma | [37] | |
SK&F-104078 | Drug Info | Terminated | Discovery agent | [38] | |
SNAP-5089 | Drug Info | Terminated | Heart arrhythmia | [39], [40] | |
WB-4101 | Drug Info | Terminated | Discovery agent | [41], [42] | |
Inhibitor | (+/-)-nantenine | Drug Info | [43] | ||
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol | Drug Info | [44] | |||
(1H-Benzoimidazol-5-yl)-(1H-imidazol-2-yl)-amine | Drug Info | [45] | |||
(1H-Imidazol-2-yl)-quinoxalin-6-yl-amine | Drug Info | [45] | |||
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [45] | |||
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [45] | |||
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine | Drug Info | [46] | |||
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine | Drug Info | [46] | |||
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine | Drug Info | [46] | |||
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [47] | |||
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [47] | |||
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline | Drug Info | [48] | |||
1,2,3,4,5,6-Hexahydro-benzo[c]azocine | Drug Info | [47] | |||
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol | Drug Info | [49] | |||
1,2,3,4-Tetrahydro-isoquinolin-7-ol | Drug Info | [49] | |||
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole | Drug Info | [50] | |||
1,2,3,4-tetrahydroisoquinoline | Drug Info | [51] | |||
1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [52] | |||
2,3,4,5-Tetrahydro-1H-benzo[c]azepine | Drug Info | [47] | |||
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine | Drug Info | [47] | |||
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine | Drug Info | [47] | |||
2,3-Dihydro-1H-isoindole | Drug Info | [47] | |||
2-BFi | Drug Info | [53] | |||
3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [54] | |||
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [44] | |||
3-Methyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [47] | |||
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole | Drug Info | [55] | |||
4-(4-Methyl-indan-1-yl)-1H-imidazole | Drug Info | [56] | |||
5-Aminomethyl-naphthalen-2-ol | Drug Info | [49] | |||
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene | Drug Info | [47] | |||
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [57] | |||
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline | Drug Info | [49] | |||
A-80426 | Drug Info | [58] | |||
Butyl-indol-1-yl-pyridin-4-yl-amine | Drug Info | [46] | |||
C-(6-Methoxy-naphthalen-1-yl)-methylamine | Drug Info | [49] | |||
C-Naphthalen-1-yl-methylamine | Drug Info | [49] | |||
CONESSINE | Drug Info | [59] | |||
Ethyl-indol-1-yl-pyridin-4-yl-amine | Drug Info | [46] | |||
GNF-PF-2857 | Drug Info | [60] | |||
GNF-PF-3427 | Drug Info | [60] | |||
GNF-PF-3878 | Drug Info | [60] | |||
Indol-1-yl-methyl-pyridin-4-yl-amine | Drug Info | [46] | |||
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine | Drug Info | [46] | |||
Indol-1-yl-propyl-pyridin-4-yl-amine | Drug Info | [46] | |||
Indol-1-yl-pyridin-4-yl-amine | Drug Info | [46] | |||
INDORAMIN | Drug Info | [61] | |||
MAZAPERTINE | Drug Info | [62] | |||
MEDETOMIDINE | Drug Info | [55] | |||
METHYLNORADRENALINE | Drug Info | [63] | |||
MEZILAMINE | Drug Info | [64] | |||
MOXONIDINE | Drug Info | [65] | |||
PIPEROXAN | Drug Info | [63] | |||
R-226161 | Drug Info | [66] | |||
RX-821002 | Drug Info | [67] | |||
S-34324 | Drug Info | [58] | |||
SK&F-104078 | Drug Info | [61] | |||
SK&F-64139 | Drug Info | [51] | |||
SNAP-5089 | Drug Info | [68] | |||
SNAP-5150 | Drug Info | [68] | |||
TRACIZOLINE | Drug Info | [57] | |||
TRAMAZOLINE | Drug Info | [63] | |||
TRYPTOLINE | Drug Info | [57] | |||
WB-4101 | Drug Info | [63] | |||
Modulator (allosteric modulator) | 5-(N,N-hexamethylene)-amiloride | Drug Info | [69] | ||
Antagonist | 5-methylurapidil | Drug Info | [70] | ||
all-trans-4-oxo-retinoic acid | Drug Info | [71] | |||
ARC239 | Drug Info | [72] | |||
Ciproxifan | Drug Info | [73] | |||
F-14413 | Drug Info | [74] | |||
GYKI-16084 | Drug Info | [75] | |||
JP1302 | Drug Info | [76] | |||
JTH-601 | Drug Info | [77] | |||
MK-912 | Drug Info | [78] | |||
ORM-12741 | Drug Info | [79] | |||
piribedil | Drug Info | [80] | |||
spiroxatrine | Drug Info | [81] | |||
TNX-102 | Drug Info | [82] | |||
[125I]BE-2254 | Drug Info | [83] | |||
[3H]MK-912 | Drug Info | [84] | |||
[3H]rauwolscine | Drug Info | [85] | |||
[3H]RX821002 | Drug Info | [86] | |||
Agonist | 6-fluoro-noradrenaline | Drug Info | [87] | ||
A61603 | Drug Info | [88] | |||
AGN-XX/YY | Drug Info | [89] | |||
amidephrine | Drug Info | [87] | |||
Chloroethylclonidine | Drug Info | [90] | |||
cirazoline | Drug Info | [87] | |||
Fadolmidine | Drug Info | [91] | |||
indanidine | Drug Info | [87] | |||
SKF 89748 | Drug Info | [87] | |||
V-101 | Drug Info | [92] | |||
xylazine | Drug Info | [93] | |||
[125I]HEAT | Drug Info | [94] | |||
Modulator | A-75169 | Drug Info | [95] | ||
Amezinium | Drug Info | [96], [1] | |||
Amosulalol | Drug Info | [2], [1] | |||
Brimonidine | Drug Info | [3] | |||
Delequamine hydrochloride | Drug Info | [97] | |||
Deriglidole | Drug Info | [98] | |||
Dihydroergocristine | Drug Info | [5], [1] | |||
Ecabapide | Drug Info | [99] | |||
ETHOXY-IDAZOXAN | Drug Info | [100] | |||
FLUPAROXAN | Drug Info | [101] | |||
GYKI-12743 | Drug Info | [102] | |||
IDAZOXAN HYDROCHLORIDE | Drug Info | [103] | |||
Midaglizole | Drug Info | [104] | |||
NMI-870 | Drug Info | [105] | |||
NOLOMIROLE HYDROCHLORIDE | Drug Info | [106] | |||
Propylhexedrine | Drug Info | [107], [1] | |||
Rilmenidine | Drug Info | [108], [1] | |||
SGB-1534 | Drug Info | [109] | |||
Tetrahydrozoline | Drug Info | [8], [1] | |||
V-103 | Drug Info | [110] | |||
Xylometazoline | Drug Info | [111], [1] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | cGMP-PKG signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
PANTHER Pathway | Alpha adrenergic receptor signaling pathway | ||||
Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
Reactome | Adrenoceptors | ||||
Adrenaline signalling through Alpha-2 adrenergic receptor | |||||
Adrenaline,noradrenaline inhibits insulin secretion | |||||
G alpha (i) signalling events | |||||
G alpha (z) signalling events | |||||
Surfactant metabolism | |||||
WikiPathways | Monoamine GPCRs | ||||
GPCRs, Class A Rhodopsin-like | |||||
Platelet Aggregation (Plug Formation) | |||||
Integration of energy metabolism | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
REF 2 | Effects of amosulalol, a combined alpha 1- and beta-adrenoceptor-blocking agent, on ischemic myocardial energy metabolism in dogs. J Pharm Sci. 1993 Mar;82(3):291-5. | ||||
REF 3 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 520). | ||||
REF 4 | ClinicalTrials.gov (NCT00675207) Comparison of Brimonidine Purite, Dorzolamide, and Brinzolamide as Adjunctive Therapy to Prostaglandin Analogs. U.S. National Institutes of Health. | ||||
REF 5 | Effect of dihydroergocristine on blood pressure and activity at peripheral alpha-adrenoceptors in pithed rats. Eur J Pharmacol. 1984 Jan 13;97(1-2):21-7. | ||||
REF 6 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 278). | ||||
REF 7 | The role of I(1)-imidazoline and alpha(2)-adrenergic receptors in the modulation of glucose metabolism in the spontaneously hypertensive obese rat model of metabolic syndrome X. J Pharmacol Exp Ther.2003 Aug;306(2):646-57. Epub 2003 May 19. | ||||
REF 8 | Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline. Clin Toxicol (Phila). 2008 Feb;46(2):171-2. | ||||
REF 9 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 517). | ||||
REF 10 | ClinicalTrials.gov (NCT00630474) Nasal Decongestion and Obstructive Sleep Apnea. U.S. National Institutes of Health. | ||||
REF 11 | ClinicalTrials.gov (NCT00294944) The Effectiveness of Idazoxan in Treating TRD. U.S. National Institutes of Health. | ||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017946) | ||||
REF 13 | Clinical pipeline report, company report or official report of ACADIA Pharmaceuticals. | ||||
REF 14 | Sedative and cardiopulmonary effects of medetomidine hydrochloride and xylazine hydrochloride and their reversal with atipamezole hydrochloride in calves. Am J Vet Res. 2008 Mar;69(3):319-29. | ||||
REF 15 | ClinicalTrials.gov (NCT02471196) Efficacy of ORM-12741 on Agitation/Aggression Symptoms in Alzheimer's Disease. | ||||
REF 16 | ClinicalTrials.gov (NCT01186068) Dose Response Study of Patients With Erythematous Rosacea. U.S. National Institutes of Health. | ||||
REF 17 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 501). | ||||
REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000582) | ||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008832) | ||||
REF 20 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 41). | ||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000678) | ||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003364) | ||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000010) | ||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013220) | ||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010746) | ||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010685) | ||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662) | ||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000716) | ||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014166) | ||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000148) | ||||
REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002059) | ||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003469) | ||||
REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006017) | ||||
REF 34 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 524). | ||||
REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000266) | ||||
REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019997) | ||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000085) | ||||
REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000354) | ||||
REF 39 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 498). | ||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006771) | ||||
REF 41 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 499). | ||||
REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004048) | ||||
REF 43 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. | ||||
REF 44 | J Med Chem. 1999 Jun 3;42(11):1982-90.3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor. | ||||
REF 45 | J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. | ||||
REF 46 | J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. | ||||
REF 47 | J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase. | ||||
REF 48 | J Med Chem. 1998 Oct 8;41(21):4165-70.N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies. | ||||
REF 49 | J Med Chem. 1997 Dec 5;40(25):3997-4005.Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. | ||||
REF 50 | Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands. | ||||
REF 51 | J Med Chem. 2006 Sep 7;49(18):5424-33.Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamineN-methyltransferase. | ||||
REF 52 | J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. | ||||
REF 53 | Bioorg Med Chem Lett. 2000 Mar 20;10(6):605-7.Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand. | ||||
REF 54 | J Med Chem. 2005 Jan 13;48(1):134-40.3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity. | ||||
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