Hydrocarbon molar water solubility predicts NMDA vs. GABAA receptor modulation

Brosnan, Robert J; Pham, Trung L

doi:10.1186/2050-6511-15-62

BMC Pharmacology and Toxicology

Table 2 Mean responses (±SEM) produced by 14 different functional groups on NMDA and GABA _A receptor modulation, expressed as a percent of the control agonist peak, using standard two-electrode voltage clamp techniques with 5–6 oocytes each

From: Hydrocarbon molar water solubility predicts NMDA vs. GABA_A receptor modulation

Compound	NMDA			GABA_A
Compound	% Direct effect	% Agonist effect	Drug response	% Direct effect	% Agonist effect	Drug response
Alcohols
1-decanol	None	70 ± 3	-	None	386 ± 20	+
1-undecanol	None	101 ± 2	0	None	181 ± 13	+
1-dodecanol	None	98 ± 1	0	None	177 ± 4	+
Alkanes
butane	None	7 ± 2	-	None	623 ± 68	+
pentane	None	94 ± 3	0	None	321 ± 10	+
hexane	None	100 ± 1	0	None	129 ± 5	+
Aldehydes
octanal	None	71 ± 3	-	6 ± 3	357 ± 20	+
nonanal	None	104 ± 2	0	None	219 ± 29	+
decanal	None	97 ± 3	0	None	159 ± 5	+
undecanal	None	97 ± 8	0	None	299 ± 29	+
Alkenes
1-pentene	None	69 ± 1	-	2 ± 3	453 ± 38	+
1-hexene	None	97 ± 0	0	None	132 ± 2	+
Alkynes
1-hexyne	None	41 ± 6	-	5 ± 2	418 ± 21	+
1-heptyne	None	68 ± 10	-	None	172 ± 8	+
1-octyne	None	96 ± 2	0	None	259 ± 11	+
Amines
1-octadecanamine	None	73 ± 4	-	None	146 ± 5	+
1-eicosanamine	None	108 ± 1	0	None	166 ± 7	+
Benzenes
1,3-dimethylbenzene	None	58 ± 3	-	None	366 ± 21	+
1,3-diethylbenzene	None	101 ± 2	0	None	305 ± 24	+
Cycloalkanes
cyclopentane	None	83 ± 2	-	3 ± 2	196 ± 11	+
cyclohexane	None	101 ± 2	0	None	421 ± 17	+
Ethers
dibutylether	None	59 ± 4	-	14 ± 13	347 ± 33	+
dipentylether	None	97 ± 2	0	None	211 ± 9	+
dihexylether	None	112 ± 4	0	None	113 ± 1	+
Esters
ethyl heptanoate	None	78 ± 3	-	None	370 ± 34	+
ethyl octanoate	None	90 ± 1	-	None	285 ± 18	+
ethyl decanoate	None	98 ± 1	0	None	137 ± 2	+
Haloalkanes
1-fluoropentane	None	76 ± 2	-	None	539 ± 35	+
1-fluorohexane	None	101 ± 1	0	11 ± 4	207 ± 13	+
1-fluoroctane	None	98 ± 1	0	None	182 ± 18	+
Ketones
2-decaNone	None	81 ± 1	-	None	476 ± 52	+
2-undecaNone	None	98 ± 2	0	None	230 ± 16	+
2-dodecaNone	None	97 ± 3	0	None	325 ± 30	+
Sulfides
1-(ethylthio)-hexane	None	87 ± 1	-	None	350 ± 57	+
1-(ethylthio)-octane	None	101 ± 1	0	None	120 ± 3	+
Thiols
1-pentanethiol	None	85 ± 4	-	22 ± 8	466 ± 57	+
1-hexanethiol	None	102 ± 3	0	8 ± 2	290 ± 41	+

The % Direct Effect is the drug response without co-administration of the receptor agonist. The % Agonist Effect is the drug response with co-administration of agonist (glutamate and glycine for NMDA receptors; γ-aminobutyric acid for GABA_A receptors). The Drug Response denotes inhibition (−) for drug + agonist responses less than the control agonist peak, potentiation (+) for drug + agonist responses greater than the control agonist peak, and no response (0) for drug + agonist responses that differ by <10% from the control agonist peak.

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ISSN: 2050-6511

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