Detail of "4507-84-0"

CAS Number:
4507-84-0
Name:
1-Naphthalenecarboxylicacid, 3-nitro-
Superlist Name:
3-Nitro-1-naphthoic acid
Molecular Structure:
Formula:
C₁₁H₇NO₄
Molecular Weight:
217.18
Synonyms:
1-Naphthoicacid, 3-nitro- (6CI,7CI,8CI);3-Nitro-1-naphthalenecarboxylic acid;3-Nitro-1-naphthoic acid;NSC 26051;
Density:
1.468 g/cm³
Boiling Point:
445.2 °C at 760 mmHg
Flash Point:
197.4 °C

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Discovery of novel, orally active dual NK1/NK2 antagonists: Discovery of novel, orally active dual NK1/NK2 antagonists. Bernstein, P. R.; Aharony, D.; Albert, J. S.; Andisik, D.; Barthlow, H. G.; Bialecki, R.; Davenport, T.; Dedinas, R. F.; Dembofsky, B. T.; Koether, G.; Kosmider, B. J.In this study，4507-84-0 is also used.; Kirkland, K.; Ohnmacht, C. J.; Potts, W.; Rumsey, W. L.; Shen, L.; Shenvi, A.Several substances like 4507-84-0 may be metioned in this study.; Sherwood, S.; Stollman, D.; Russell, K. ( AstraZeneca Pharmaceuticals LP, CNS Discovery Research, Wilmington, DE 19850-5437, USA). Bioorganic & Medicinal Chemistry Letters, 11(20), 2769-2773 (English) 2001 Elsevier Science Ltd. CODEN: BMCLE8. ISSN: 0960-894X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 27, 63 Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogs provide potent dual NK1 and NK2 antagonists. ZD6021 inhibited binding of [3H]-NKA or [3H]-SP to human NK1 and NK2 receptors, with high-affinity (Ki=0.12 and 0.62 nM, resp.). In functional assays ZD6021 had, at 10-7 M, in human pulmonary artery pKB=8.9 and in human bronchus pKB=7.3, for NK1 and NK2, resp. Oral administration of ZD6021 to guinea pigs dose-dependently attenuated ASMSP induced extravasation of plasma proteins, ED50=0.5 mg/kg, and NK2 mediated bronchoconstriction, ED50=13 mg/kg. ..

Discovery of novel, orally active dual NK1/NK2 antagonists: Discovery of novel, orally active dual NK1/NK2 antagonists. Bernstein, P. R.; Aharony, D.; Albert, J. S.; Andisik, D.; Barthlow, H. G.; Bialecki, R.; Davenport, T.; Dedinas, R. F.; Dembofsky, B. T.; Koether, G.; Kosmider, B. J.In this study，4507-84-0 is also used.; Kirkland, K.; Ohnmacht, C. J.; Potts, W.; Rumsey, W. L.; Shen, L.; Shenvi, A.Several substances like 4507-84-0 may be metioned in this study.; Sherwood, S.; Stollman, D.; Russell, K. ( AstraZeneca Pharmaceuticals LP, CNS Discovery Research, Wilmington, DE 19850-5437, USA). Bioorganic & Medicinal Chemistry Letters, 11(20), 2769-2773 (English) 2001 Elsevier Science Ltd. CODEN: BMCLE8. ISSN: 0960-894X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 27, 63 Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogs provide potent dual NK1 and NK2 antagonists. ZD6021 inhibited binding of [3H]-NKA or [3H]-SP to human NK1 and NK2 receptors, with high-affinity (Ki=0.12 and 0.62 nM, resp.). In functional assays ZD6021 had, at 10-7 M, in human pulmonary artery pKB=8.9 and in human bronchus pKB=7.3, for NK1 and NK2, resp. Oral administration of ZD6021 to guinea pigs dose-dependently attenuated ASMSP induced extravasation of plasma proteins, ED50=0.5 mg/kg, and NK2 mediated bronchoconstriction, ED50=13 mg/kg. ..