Target Information

Target General Information

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Target ID

T87023 (Former ID: TTDR01165)

Target Name

Platelet-activating factor receptor (PTAFR)

Synonyms

PTAFR; PAF-R

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Gene Name

PTAFR

Target Type

Successful target

[1]

Disease

[+] 1 Target-related Diseases

Ischaemic/haemorrhagic stroke [ICD-11: 8B20]

Function

Receptor for platelet activating factor, a chemotactic phospholipid mediator that possesses potent inflammatory, smooth- muscle contractile and hypotensive activity. Seems to mediate its action via a G protein that activates a phosphatidylinositol- calcium second messenger system.

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BioChemical Class

GPCR rhodopsin

UniProt ID

PTAFR_HUMAN

Sequence

MEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLT
MADMLFLITLPLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVT
RPIKTAQANTRKRGISLSLVIWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKG
SVPVLIIHIFIVFSFFLVFLIILFCNLVIIRTLLMQPVQQQRNAEVKRRALWMVCTVLAV
FIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLCLLSTNCVLDPVIYCFLTKKF
RKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

ADReCS ID

BADD_A00264

HIT2.0 ID

T72IYV

Drugs and Modes of Action

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Approved Drug(s)

[+] 1 Approved Drugs

Ticlopidine

Drug Info

Approved

Stroke

[2], [3]

Clinical Trial Drug(s)

[+] 7 Clinical Trial Drugs

ISRAPAFANT

Drug Info

Phase 3

Asthma

[4], [5]

60P002

Drug Info

Phase 2

Dengue

[6]

CMI-392

Drug Info

Phase 2

Psoriasis vulgaris

[7]

Dersalazine

Drug Info

Phase 2

Inflammatory bowel disease

[8]

Lexipafant

Drug Info

Phase 2

Nerve injury

[9]

YM-264

Drug Info

Phase 2

Sepsis

[10]

PegCNTF

Drug Info

Phase 1

Obesity

[11]

Discontinued Drug(s)

[+] 31 Discontinued Drugs

BN 50730

Drug Info

Discontinued in Phase 3

Asthma

[12]

FOROPAFANT

Drug Info

Discontinued in Phase 3

Asthma

[13], [14]

BN50727

Drug Info

Discontinued in Phase 2

Inflammatory bowel disease

[15]

DE-081

Drug Info

Discontinued in Phase 2

Conjunctivitis

[16]

E-6123

Drug Info

Discontinued in Phase 2

Asthma

[17]

Minopafant

Drug Info

Discontinued in Phase 2

Sepsis

[18]

MK-287

Drug Info

Discontinued in Phase 2

Sepsis

[19]

Ro-24-4736

Drug Info

Discontinued in Phase 2

Sepsis

[20]

SM-10661

Drug Info

Discontinued in Phase 2

Sepsis

[21]

TCV-309

Drug Info

Discontinued in Phase 2

Sepsis

[22]

UK-74505

Drug Info

Discontinued in Phase 2

Sepsis

[23]

ABT-299

Drug Info

Discontinued in Phase 1

Sepsis

[24], [25]

AGN-191743

Drug Info

Discontinued in Phase 1

Allergy

[26]

DACOPAFANT

Drug Info

Discontinued in Phase 1

Sepsis

[27]

DF-1111301

Drug Info

Discontinued in Phase 1

Allergy

[28]

SDZ-62-434

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[29]

Bepafant

Drug Info

Terminated

Sepsis

[30], [31]

BN-50726

Drug Info

Terminated

Nerve injury

[32]

BN50739

Drug Info

Terminated

Cerebral infarction

[33], [34]

CL-184005

Drug Info

Terminated

Sepsis

[35]

CMI-206

Drug Info

Terminated

Inflammation

[36]

CV 6209

Drug Info

Terminated

Asthma

[37], [38]

FR-128998

Drug Info

Terminated

Thrombocytopenia

[39]

KC-11404

Drug Info

Terminated

Asthma

[40]

KC-11425

Drug Info

Terminated

Asthma

[41]

Ro-24-0238

Drug Info

Terminated

Sepsis

[42]

Sch-40338

Drug Info

Terminated

Allergy

[43], [44]

TIAPAFANT

Drug Info

Terminated

Sepsis

[45], [46]

TULOPAFANT

Drug Info

Terminated

Cardiac arrhythmias

[47]

UR-12460

Drug Info

Terminated

Thrombosis

[48]

WEB-2347

Drug Info

Terminated

Allergy

[49]

Mode of Action

[+] 4 Modes of Action

Modulator

[+] 28 Modulator drugs

Ticlopidine

Drug Info

[1]

CMI-392

Drug Info

[7]

Lexipafant

Drug Info

[54]

PegCNTF

Drug Info

[44]

BN 50730

Drug Info

[56], [57]

BN50727

Drug Info

[60]

DE-081

Drug Info

[61], [62], [63]

E-6123

Drug Info

[64]

TCV-309

Drug Info

[69]

AGN-191743

Drug Info

[72]

BN50739

Drug Info

[78], [79]

CL-184005

Drug Info

[80]

CMI-206

Drug Info

[81]

CV 6209

Drug Info

[82]

FR-128998

Drug Info

[83]

KC-11404

Drug Info

[40]

Sch-40338

Drug Info

[87]

UR-12460

Drug Info

[91]

WEB-2347

Drug Info

[92]

A 137491

Drug Info

[94]

BB-823

Drug Info

[91]

FR-900452

Drug Info

[96]

KO-286011

Drug Info

[97]

SRI-63-675

Drug Info

[104]

UR-10324

Drug Info

[105]

UR-11353

Drug Info

[105]

UR-12510

Drug Info

[106]

UR-12519

Drug Info

[107]

Inhibitor

[+] 7 Inhibitor drugs

RUPATADINE

Drug Info

[50]

Dersalazine

Drug Info

[8]

L-659989

Drug Info

[85]

Ro-24-0238

Drug Info

[86]

SDZ-64-412

Drug Info

[88]

L-652731

Drug Info

[85]

VERAGUENSIN

Drug Info

[85]

Antagonist

[+] 34 Antagonist drugs

ISRAPAFANT

Drug Info

[51], [52]

60P002

Drug Info

[53]

YM-264

Drug Info

[55]

FOROPAFANT

Drug Info

[52], [58], [59]

Minopafant

Drug Info

[65]

MK-287

Drug Info

[66], [52]

Ro-24-4736

Drug Info

[67]

SM-10661

Drug Info

[68], [52]

UK-74505

Drug Info

[70]

ABT-299

Drug Info

[71]

DACOPAFANT

Drug Info

[73], [52]

DF-1111301

Drug Info

[74], [52]

SDZ-62-434

Drug Info

[75], [52]

Bepafant

Drug Info

[76]

BN-50726

Drug Info

[77]

KC-11425

Drug Info

[84]

TIAPAFANT

Drug Info

[89], [52]

TULOPAFANT

Drug Info

[90], [52]

10-OBn-7alpha-F-gingkolide B

Drug Info

[93]

10-OBn-epi-ginkgolide C

Drug Info

[93]

10-OBn-ginkgolide B

Drug Info

[93]

10-OBn-ginkgolide C

Drug Info

[93]

7-epi-ginkgolide C

Drug Info

[93]

7alpha-Cl-ginkgolide B

Drug Info

[93]

7alpha-F-ginkgolide B

Drug Info

[93]

7alpha-N3-ginkgolide B

Drug Info

[93]

7alpha-NH2-ginkgolide B

Drug Info

[93]

7alpha-NHEt-ginkgolide B

Drug Info

[93]

7alpha-NHMe-ginkgolide B

Drug Info

[93]

7alpha-OAc-ginkgolide B

Drug Info

[93]

7alpha-OCOCH2Ph-ginkgolide B

Drug Info

[93]

CV-3988

Drug Info

[95]

LAU-0901

Drug Info

[98], [99]

RP-52770

Drug Info

[103]

Agonist

[+] 5 Agonist drugs

2-O-ethyl-PAF C-16

Drug Info

[62]

2-O-methyl-PAF C-18

Drug Info

[62]

enantio PAF C-16

Drug Info

[62]

methylcarbamyl PAF

Drug Info

[100]

PAF

Drug Info

[101], [102]

Cell-based Target Expression Variations

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Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Human Similarity Proteins Human Pathway Affiliation

Different Human System Profiles of Target

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Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Human Similarity Proteins

Human Pathway Affiliation

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 11G2 (OR11G2)	PF13853	21.359 (66/309)	6.79E-04
Olfactory receptor 52E4 (OR52E4)	PF13853	23.899 (76/318)	8.57E-04
Olfactory receptor 6C68 (OR6C68)	PF13853	26.178 (50/191)	5.00E-03

KEGG Pathway	Pathway ID	Affiliated Target
Calcium signaling pathway	hsa04020	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Neuroactive ligand-receptor interaction	hsa04080	Affiliated Target
Class: Environmental Information Processing => Signaling molecules and interaction	Pathway Hierarchy

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

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Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

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KEGG Pathway

[+] 3 KEGG Pathways

Calcium signaling pathway

Neuroactive ligand-receptor interaction

Staphylococcus aureus infection

NetPath Pathway

[+] 2 NetPath Pathways

IL5 Signaling Pathway

Leptin Signaling Pathway

Reactome

[+] 3 Reactome Pathways

Class A/1 (Rhodopsin-like receptors)

G alpha (q) signalling events

Interferon gamma signaling

WikiPathways

[+] 6 WikiPathways

GPCRs, Class A Rhodopsin-like

Gastrin-CREB signalling pathway via PKC and MAPK

Small Ligand GPCRs

Interferon gamma signaling

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

Top

REF 1

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 2

URL: 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: 7307).

REF 3

Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.

REF 4

REF 5

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001699)

REF 6

ClinicalTrials.gov (NCT02569827) Celgosivir or Modipafant as Treatment for Adult Participants With Uncomplicated Dengue Fever in Singapore. U.S. National Institutes of Health.

REF 7

Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20.

REF 8

The intestinal anti-inflammatory effect of dersalazine sodium is related to a down-regulation in IL-17 production in experimental models of rodent colitis. Br J Pharmacol. 2012 February; 165(3): 729-740.

REF 9

Randomized, double-blind phase II trial of Lexipafant, a platelet-activating factor antagonist, in human acute pancreatitis. Br J Surg. 1995 Oct;82(10):1414-20.

REF 10

Current Pharmaceutical Design. Page(175).

REF 11

Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.

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 800001346)

REF 13

REF 14

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002078)

REF 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005290)

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000113)

REF 17

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001351)

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 800002131)

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 800001713)

REF 20

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001180)

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 800004382)

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 800002130)

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 800001719)

REF 24

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 800005514)

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 800003636)

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 800000051)

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 800003701)

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 800002021)

REF 30

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 800000108)

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 800001821)

REF 33

REF 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002032)

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 800001674)

REF 36

Cmi206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor. Bioorganic & Medicinal Chemistry Letters. 03/1995; 5(6):643-648.

REF 37

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 800001311)

REF 39

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004313)

REF 40

Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995 Feb 17;38(4):669-85.

REF 41

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005461)

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 800003729)

REF 43

REF 44

Sch 37370: a new drug combining antagonism of platelet-activating factor (PAF) with antagonism of histamine. Agents Actions Suppl. 1991;34:313-21.

REF 45

REF 46

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001989)

REF 47

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001254)

REF 48

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005037)

REF 49

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001720)

REF 50

Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.

REF 51

Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor. J Biol Chem. 2010 Feb 19;285(8):5931-40.

REF 52

Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.

REF 53

Clinical pipeline report, company report or official report of 60 Degrees Pharmaceuticals.

REF 54

Lexipafant and acute pancreatitis: a critical appraisal of the clinical trials.Eur J Surg.2002;168(4):215-9.

REF 55

Effects of YM264, a novel PAF antagonist, on puromycin aminonucleoside-induced nephropathy in the rat. Biochem Biophys Res Commun. 1991 Apr 30;176(2):781-5.

REF 56

Platelet-activating factor antagonist BN 50730 attenuates hypoxic-ischemic brain injury in neonatal rats. Pediatr Res. 2001 Jun;49(6):804-11.

REF 57

Effects of BN-50730 (PAF receptor antagonist) and physostigmine (AChE inhibitor) on learning and memory in mice. Methods Find Exp Clin Pharmacol. 1997 Nov;19(9):585-8.

REF 58

Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist. J Pharmacol Exp Ther. 1991 Oct;259(1):44-51.

REF 59

In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist, on the PAF-induced bovine platelet aggregation. Vet Res. 2000 Mar-Apr;31(2):267-72.

REF 60

Platelet-activating factor preferentially stimulates the phospholipase A2/cyclooxygenase cascade in the rabbit cornea. Curr Eye Res. 1995 Sep;14(9):769-75.

REF 61

Characterization of [3H]apafant binding to PAF receptor on rabbit platelet membranes: a comparison of a microplate filtration system and a standard... J Pharmacol Toxicol Methods. 1996 Sep;36(1):53-62.

REF 62

A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor. J Immunol Methods. 1995 Oct 26;186(2):225-31.

REF 63

Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.

REF 64

Inhibitory effects of a novel PAF antagonist E6123 on anaphylactic responses in passively and actively sensitized guinea pigs and passively sensiti... Prostaglandins. 1991 Dec;42(6):541-55.

REF 65

Formation of spherical micelles composed of the novel platelet activating factor receptor antagonist, E5880. Pharm Dev Technol. 2005;10(1):11-6.

REF 66

MK 287: a potent, specific, and orally active receptor antagonist of platelet-activating factor. J Lipid Mediat. 1993 Jun;7(2):115-34.

REF 67

Pharmacology of a potent platelet-activating factor antagonist: Ro 24-4736. J Pharmacol Exp Ther. 1991 Oct;259(1):78-85.

REF 68

Effect of the PAF-receptor antagonist SM-12502 on human platelets. Inflammation. 1996 Feb;20(1):71-85.

REF 69

Inhibitory effect of TCV-309, a novel platelet activating factor (PAF) antagonist, on endotoxin-induced disseminated intravascular coagulation in r... Thromb Res. 1993 May 15;70(4):281-93.

REF 70

Differential effects of the PAF receptor antagonist UK-74,505 on neutrophil and eosinophil accumulation in guinea-pig skin. Br J Pharmacol. 1994 Oct;113(2):513-21.

REF 71

ABT-299, a novel PAF antagonist, attenuates multiple effects of endotoxemia in conscious rats. Shock. 1996 Aug;6(2):112-7.

REF 72

US patent application no. 6,274,627, Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor.

REF 73

RP 55778, a PAF receptor antagonist, prevents and reverses LPS-induced hemoconcentration and TNF release. J Lipid Mediat. 1989 Nov-Dec;1(6):349-60.

REF 74

US patent application no. 2007,0196,421, Soft tissue implants and drug combination compositions, and use thereof.

REF 75

In vitro antitumour activity of the novel imidazoisoquinoline SDZ 62-434. Br J Cancer. 1993 May;67(5):989-95.

REF 76

Pharmacologic activity of bepafant (WEB 2170), a new and selective hetrazepinoic antagonist of platelet activating factor. J Pharmacol Exp Ther. 1990 Dec;255(3):962-8.

REF 77

Effects of the PAF antagonists BN50726 and BN50739 on arrhythmogenesis and extent of necrosis during myocardial ischaemia/reperfusion in rabbits. Br J Pharmacol. 1992 Nov;107(3):705-9.

REF 78

Effect of the platelet-activating factor antagonist BN 50739 and its diluents on mitochondrial respiration and membrane lipids during and following... J Neurochem. 1994 May;62(5):1929-38.

REF 79

Pharmacologic profile of BN 50739, a new PAF antagonist in vitro and in vivo. Prostaglandins. 1990 May;39(5):469-80.

REF 80

Studies of the effect of a platelet-activating factor antagonist, CL 184,005, in animal models of gram-negative bacterial sepsis. Antimicrob Agents Chemother. 1992 Sep;36(9):1971-7.

REF 81

DOI: 10.1016/0960-894X(95)00088-B

REF 82

CV-6209, a highly potent antagonist of platelet activating factor in vitro and in vivo. J Pharmacol Exp Ther. 1987 Jul;242(1):263-8.

REF 83

Effect of FR128998, a novel PAF receptor antagonist, on endotoxin-induced disseminated intravascular coagulation. Eur J Pharmacol. 1994 Jun 13;258(3):239-46.

REF 84

WO patent application no. 2002,01223,5, 1,4-dihydropyridines as bradykinin antagonists.

REF 85

Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,... J Med Chem. 1992 Sep 18;35(19):3474-82.

REF 86

Pentadienyl carboxamide derivatives as antagonists of platelet-activating factor. J Med Chem. 1989 Aug;32(8):1820-35.

REF 87

Conformational considerations in the design of dual antagonists of platelet-activating factor (PAF) and histamine. Bioorg Med Chem. 1999 Jul;7(7):1413-23.

REF 88

Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists. J Med Chem. 1993 Oct 15;36(21):3098-102.

REF 89

PCA-4248, a PAF receptor antagonist, inhibits PAF-induced phosphoinositide turnover. Eur J Pharmacol. 1995 Aug 15;290(3):183-8.

REF 90

Tulopafant, a PAF receptor antagonist, increases capillary patency and prolongs survival in discordant cardiac xenotransplants. J Lipid Mediat. 1993 May;7(1):79-84.

REF 91

Platelet-activating factor: the effector of protein-rich plasma extravasation and nitric oxide synthase induction in rat immune complex peritonitis. Br J Pharmacol. 1995 Feb;114(4):895-901.

REF 92

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