LF 16-0687

a potent non-peptide bradykinin B2 receptor antagonist; structure in first source

Also Known As:

1-((2,4-dichloro-3-(((2,4-dimethylquinolin-8-yl)oxy) methyl)phenyl)sulfonyl)-N-(3-((4-(aminoimethyl) phenyl) carbonylamino)propyl)-2(S)-pyrrolidinecarboxamide; Anatibant; LF16-0687; LF16-0687Ms

Networked: 19 relevant articles (4 outcomes, 6 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Quinolines: 146
      - LF 16-0687: 19

Experts

1.	Pruneau, D: 6 articles (01/2006 - 01/2000)
2.	Pruneau, Didier: 5 articles (05/2006 - 08/2002)
3.	Baethmann, A: 4 articles (01/2006 - 01/2000)
4.	Plesnila, N: 4 articles (01/2006 - 01/2000)
5.	Artru, Alan A: 3 articles (05/2003 - 08/2002)
6.	Asa, Ilia: 3 articles (05/2003 - 08/2002)
7.	Ivashkova, Yulia: 3 articles (05/2003 - 08/2002)
8.	Shapira, Yoram: 3 articles (05/2003 - 08/2002)
9.	Couture, Réjean: 2 articles (05/2006 - 12/2005)
10.	Marchand-Verrecchia, Catherine: 2 articles (05/2006 - 08/2003)

Related Diseases

1.	Brain Edema (Cerebral Edema) 01/01/2000 - "No significant reduction of hemispheric brain swelling (+7.4 +/- 2.9%) was found in animals receiving high-dose LF16-0687 as compared to the untreated controls. " 01/01/2018 - "Both the cPLA2 inhibitor and the LF16-0687 improved CCI rat outcomes by decreasing neuron death and reducing brain edema. " 09/01/2003 - "LF 16-0687 Ms given 30 min after injury reduced the neurological deficit by 26% and the cerebral edema by 22% when evaluated 4 h after CHT. " 11/01/2001 - "To examine the latter possibility we studied a surrogate condition for the earliest possible administration of LF 16-0687 Ms after CHT, e.g., we examined brain edema and NSS when LF 16-0687 Ms was given 15 min before CHT in rats. " 10/01/2001 - "Pretreatment with 10 microg/kg/min LF 16-0687 decreased brain swelling significantly to 6.4 +/- 1.3% (p < 0.05). "
2.	Infarction (Infarctions) 09/20/2002 - "All treated animals showed tendency to exhibit improved neurological recovery throughout the observation period as compared to the vehicle-treated controls, while this improvement was only significant within the low dose group from postischemic days 3 to 4. Low dose LF 16-0687 Ms significantly attenuated the total and cortical infarct volume by 50 and 80%, respectively. " 08/01/2003 - "3. When given at 0.25 and 6.25 h after MCAO, LF 16-0687 Ms (1.5, 3 and 6 mg kg(-1)) decreased the infarct volume by a maximum of 25% and improved the neurological score. " 01/19/2006 - "In order to assess the potential clinical value of this approach, we evaluated the effect of LF 16-0687 Ms given at reperfusion following focal cerebral ischemia on local cerebral blood flow (LCBF), neurological outcome, and infarct size. " 08/01/2003 - "2. LF 16-0687 Ms (1, 2 and 4 mg kg(-1)) administered 0.5 h before and, 1.25 and 6 h after MCAO, decreased the infarct volume by a maximum of 33% and significantly improved the neurological recovery. " 09/20/2002 - "We have investigated the influence of LF 16-0687 Ms on the edema formation, neurological outcome, and infarct size in temporary focal cerebral ischemia in rats. "
3.	Stroke (Strokes) 09/20/2002 - "Accordingly, specific inhibition of bradykinin B(2) receptors by LF 16-0687 Ms attenuated postischemic brain swelling, improved the functional neurological recovery, and limited ischemic tissue damage, raising its potential for clinical evaluation in patients with acute stroke."
4.	Traumatic Brain Injuries (Traumatic Brain Injury) 12/03/2009 - "Adults with traumatic brain injury and a Glasgow Coma Scale score of 12 or less, who had a CT scan showing an intracranial abnormality consistent with trauma, and were within eight hours of their injury were randomly allocated to low, medium or high dose Anatibant or to placebo. " 12/03/2009 - "The BRAIN TRIAL: a randomised, placebo controlled trial of a Bradykinin B2 receptor antagonist (Anatibant) in patients with traumatic brain injury." 12/03/2009 - "A response to and comment on The BRAIN TRIAL: a randomised, placebo controlled trial of a Bradykinin B2 receptor antagonist (Anatibant) in patients with traumatic brain injury, by Haleema Shakur, Ian Roberts, et al." 12/03/2009 - "Response to: The BRAIN TRIAL: a randomised, placebo controlled trial of a Bradykinin B2 receptor antagonist (Anatibant) in patients with traumatic brain injury." 12/01/2005 - "A single dose, three-arm, placebo-controlled, phase I study of the bradykinin B2 receptor antagonist Anatibant (LF16-0687Ms) in patients with severe traumatic brain injury."
5.	Closed Head Injuries 09/01/2003 - "Using the non-peptide B2R antagonist LF 16-0687 Ms and B2R null (B2R-/-) mice, we investigated the role of B2R in a model of closed head trauma (CHT). " 08/01/2002 - "LF 16-0687 Ms, a bradykinin B2 receptor antagonist, reduces brain edema and improves long-term neurological function recovery after closed head trauma in rats." 11/01/2001 - "Giving LF 16-0687 Ms (a bradykinin B2 receptor antagonist) 1 hour after closed head trauma (CHT) previously was reported to decrease brain edema at 24 hours and improve neurologic severity score (NSS) at 7 days. " 02/01/2003 - "This study examined the effect of LF 16-0687 Ms, a new B(2) receptor antagonist, on brain tissue PGE(2) after closed head trauma (CHT). " 05/01/2006 - "Autoradiographic analysis of mouse brain kinin B1 and B2 receptors after closed head trauma and ability of Anatibant mesylate to cross the blood-brain barrier."

Related Drugs and Biologics

1.	2,5-dichloro-4-bromophenol (B 2)
2.	Bradykinin
3.	MS 1-2
4.	Bradykinin B2 Receptor
5.	Prostaglandins E
6.	N- (4'- fluorobutyrophenone)- 4- (4- chlorophenyl)pyridinium (HPP(+))
7.	icatibant
8.	Kinins
9.	Peptides (Polypeptides)
10.	Dinoprostone (PGE2)

Related Therapies and Procedures

1.	Ligation